We produce Sotagliflozin,LX4211,1018899-04-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok

Name: Sotagliflozin
CAS#: 1018899-04-1
Chemical Formula: C21H25ClO5S
Exact Mass: 424.11112
Molecular Weight: 424.94
Elemental Analysis: C, 59.36; H, 5.93; Cl, 8.34; O, 18.83; S, 7.55


We produce Sotagliflozin,LX4211,1018899-04-1 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Sotagliflozin,LX4211,1018899-04-1 Intermediates, we have 8; Sotagliflozin,LX4211,1018899-04-1 Impurity we have 10, all from GMP, FDA plant.
Now Sotagliflozin,LX4211,1018899-04-1 DMF document is preparing.
Until 2016, Aug, Sotagliflozin,LX4211,1018899-04-1 more than produced 25kg API, 120kg Intermediates

Sotagliflozin LP-802034;LX-4211; 1018899-04-1
Sotagliflozin Intermediates ((3aS,5R,6S,6aS)-6-hydroxy-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-5-yl)(morpholino)methanone 1103738-19-7
Sotagliflozin Intermediates (3aS,5R,6S,6aS)-6-hydroxy-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxole-5-carboxylic acid 1103738-20-0
Sotagliflozin Intermediates (3aS,5S,6R,6aS)-5-(hydroxymethyl)-2,2-dimethyltetrahydrofuro[2,3-d][1,3]dioxol-6-ol 114861-22-2
Sotagliflozin Intermediates (3aS,3bR,7aS,8aS)-2,2,5,5-tetramethyltetrahydro-3aH-[1,3]dioxolo[4',5':4,5]furo[3,2-d][1,3]dioxine 131156-47-3

GMP PRODUCE:

Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib 

2016 Mumbai CPHI, Hope to meet!

2016 Barcelona CPHI, Hope to meet!

2016 Korea(한국) CPHI, C40, Welcome!

2016 Shanghai CPHI, W5C47, Welcome!

EOS Med Chem, Medchem is Big

執大象，天下往，往而無害，安平泰

網址: www.eosmedchem.com 

郵箱: gutian@eosmedchem.com; eosmedchem@gmail.com 

辦公室: 0086-531-69905422-806(直通)

攜帶番號 & WhatsApp: +8618653174435

Skype: willgutian

Description: Sotagliflozin, also known as LX4211, is an orally active and a dual SGLT1/SGLT2 inhibitor, which improves glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. LX4211 increases serum glucagon-like peptide 1 and peptide YY levels by reducing sodium/glucose cotransporter 1 (SGLT1)-mediated absorption of intestinal glucose. Sotagliflozin is currently being developed by Lexicon for the treatment of type 1 and type 2 diabetes mellitus. Sotagliflozin may be an effective and promising medication for treating not only Type 2 diabetes (the common target for non-insulin medications for diabetes), but also Type 1 as well.
Synonym: LX4211; LX 4211; LX 4211; Sotagliflozin
IUPAC/Chemical Name: (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(methylthio)tetrahydro-2H-pyran-3,4,5-triol
SMILES Code: O[C@@H]([C@@H]([C@H]([C@H](C1=CC=C(Cl)C(CC2=CC=C(OCC)C=C2)=C1)O3)O)O)[C@H]3SC

1: Zambrowicz B, Lapuerta P, Strumph P, Banks P, Wilson A, Ogbaa I, Sands A, Powell D. LX4211 Therapy Reduces Postprandial Glucose Levels in Patients With Type 2 Diabetes Mellitus and Renal Impairment Despite Low Urinary Glucose Excretion. Clin Ther. 2014 Dec 16. pii: S0149-2918(14)00699-7. doi: 10.1016/j.clinthera.2014.10.026. [Epub ahead of print] PubMed PMID: 25529979.
2: Rosenstock J, Cefalu WT, Lapuerta P, Zambrowicz B, Ogbaa I, Banks P, Sands A. Greater Dose-Ranging Effects on A1C Levels Than on Glucosuria With LX4211, a Dual Inhibitor of Sodium Glucose Transporters SGLT1 and SGLT2, in Type 2 Diabetes on Metformin Monotherapy. Diabetes Care. 2014 Sep 11. pii: DC_140890. [Epub ahead of print] PubMed PMID: 25216510.
3: Powell DR, DaCosta CM, Smith M, Doree D, Harris A, Buhring L, Heydorn W, Nouraldeen A, Xiong W, Yalamanchili P, Mseeh F, Wilson A, Shadoan M, Zambrowicz B, Ding ZM. Effect of LX4211 on glucose homeostasis and body composition in preclinical models. J Pharmacol Exp Ther. 2014 Aug;350(2):232-42. doi: 10.1124/jpet.114.214304. Epub 2014 May 21. PubMed PMID: 24849925.
4: Mauricio D. [Sodium-glucose co-transporter-2 inhibitors: from the bark of apple trees and familial renal glycosuria to the treatment of type 2 diabetes mellitus]. Med Clin (Barc). 2013 Sep;141 Suppl 2:31-5. doi: 10.1016/S0025-7753(13)70061-7. Review. Spanish. PubMed PMID: 24444522.
5: Kanwal A, Banerjee SK. SGLT inhibitors: a novel target for diabetes. Pharm Pat Anal. 2013 Jan;2(1):77-91. doi: 10.4155/ppa.12.78. Review. PubMed PMID: 24236972.
6: Zambrowicz B, Ogbaa I, Frazier K, Banks P, Turnage A, Freiman J, Boehm KA, Ruff D, Powell D, Sands A. Effects of LX4211, a dual sodium-dependent glucose cotransporters 1 and 2 inhibitor, on postprandial glucose, insulin, glucagon-like peptide 1, and peptide tyrosine tyrosine in a dose-timing study in healthy subjects. Clin Ther. 2013 Aug;35(8):1162-1173.e8. doi: 10.1016/j.clinthera.2013.06.011. Epub 2013 Jul 31. PubMed PMID: 23911260.
7: Bloomgarden Z. Sodium glucose transporter 2 inhibition: a new approach to diabetes treatment. J Diabetes. 2013 Sep;5(3):225-7. doi: 10.1111/1753-0407.12065. Epub 2013 Jul 1. PubMed PMID: 23714218.
8: Lapuerta P, Rosenstock J, Zambrowicz B, Powell DR, Ogbaa I, Freiman J, Cefalu WT, Banks P, Frazier K, Kelly M, Sands A. Study design and rationale of a dose-ranging trial of LX4211, a dual inhibitor of SGLT1 and SGLT2, in type 2 diabetes inadequately controlled on metformin monotherapy. Clin Cardiol. 2013 Jul;36(7):367-71. doi: 10.1002/clc.22125. Epub 2013 Apr 29. PubMed PMID: 23630033.
9: Powell DR, Smith M, Greer J, Harris A, Zhao S, DaCosta C, Mseeh F, Shadoan MK, Sands A, Zambrowicz B, Ding ZM. LX4211 increases serum glucagon-like peptide 1 and peptide YY levels by reducing sodium/glucose cotransporter 1 (SGLT1)-mediated absorption of intestinal glucose. J Pharmacol Exp Ther. 2013 May;345(2):250-9. doi: 10.1124/jpet.113.203364. Epub 2013 Mar 13. PubMed PMID: 23487174.
10: Zambrowicz B, Ding ZM, Ogbaa I, Frazier K, Banks P, Turnage A, Freiman J, Smith M, Ruff D, Sands A, Powell D. Effects of LX4211, a dual SGLT1/SGLT2 inhibitor, plus sitagliptin on postprandial active GLP-1 and glycemic control in type 2 diabetes. Clin Ther. 2013 Mar;35(3):273-285.e7. doi: 10.1016/j.clinthera.2013.01.010. Epub 2013 Feb 21. PubMed PMID: 23433601.
11: Zambrowicz B, Freiman J, Brown PM, Frazier KS, Turnage A, Bronner J, Ruff D, Shadoan M, Banks P, Mseeh F, Rawlins DB, Goodwin NC, Mabon R, Harrison BA, Wilson A, Sands A, Powell DR. LX4211, a dual SGLT1/SGLT2 inhibitor, improved glycemic control in patients with type 2 diabetes in a randomized, placebo-controlled trial. Clin Pharmacol Ther. 2012 Aug;92(2):158-69. doi: 10.1038/clpt.2012.58. Epub 2012 Jul 4. PubMed PMID: 22739142; PubMed Central PMCID: PMC3400893.

We produce Dapagliflozin , BMS-512148-05, 461432-26-8 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok

Name: Dapagliflozin

CAS#: 461432-26-8

Chemical Formula: C21H25ClO6

Exact Mass: 408.13397

Molecular Weight: 408.87

Elemental Analysis: C, 61.69; H, 6.16; Cl, 8.67; O, 23.48

Dapagliflozin BMS-512148-05;Forxiga 461432-26-8(free base)

Dapagliflozin BMS-512148-05;Forxiga 960404-48-2(Propanediol Monohydrate)

Dapagliflozin Intermediates (2R,3R,4R,5S,6S)-2-(acetoxymethyl)-6-(4-chloro-3-(4-ethoxybenzyl)phenyl)tetrahydro-2H-pyran-3,4,5-triyl triacetate 461432-25-7

We produce Dapagliflozin , BMS-512148-05, 461432-26-8 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Dapagliflozin , BMS-512148-05, 461432-26-8 Intermediates, we have 8; Dapagliflozin , BMS-512148-05, 461432-26-8 Impurity we have 10, all from GMP, FDA plant.

Now Dapagliflozin , BMS-512148-05, 461432-26-8 DMF document is preparing.

Until 2016, Aug, Dapagliflozin , BMS-512148-05, 461432-26-8 more than produced 25kg API, 120kg Intermediates

GMP PRODUCE:

Alectinib;Veliparib;Acalabrutinib;Venetoclax;Sotagliflozin;Ledipasvir;LX1606;Anacetrapib;Abemaciclib 

2016 Mumbai CPHI, Hope to meet!

2016 Barcelona CPHI, Hope to meet!

2016 Korea(한국) CPHI, C40, Welcome!

2016 Shanghai CPHI, W5C47, Welcome!

EOS Med Chem, Medchem is Big

執大象，天下往，往而無害，安平泰

網址: www.eosmedchem.com 

郵箱: gutian@eosmedchem.com; eosmedchem@gmail.com 

辦公室: 0086-531-69905422-806(直通)

攜帶番號 & WhatsApp: +8618653174435

Skype: willgutian

Description: Dapagliflozin, also known as BMS-512148, is a drug used to treat type 2 diabetes approved in 2012 by FDA. Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2) which are responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter mechanism causes blood glucose to be eliminated through the urine. In clinical trials, dapagliflozin lowered HbA1c by 0.6 versus placebo percentage points when added to metformin.

Synonym: BMS512148; BMS-512148; BMS 512148; Dapagliflozin; trade name Farxiga in the US and Forxiga in the EU.

IUPAC/Chemical Name: (2S,3R,4R,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol

SMILES Code: O[C@H]1[C@H](C2=CC=C(Cl)C(CC3=CC=C(OCC)C=C3)=C2)O[C@H](CO)[C@@H](O)[C@@H]1O

Dapagliflozin inhibits subtype 2 of the sodium-glucose transport proteins (SGLT2), which is responsible for at least 90% of the glucose reabsorption in the kidney. Blocking this transporter causes blood glucose to be eliminated through the urine. The efficacy of the this medication class has yet to be determined, but in initial clinical trials, dapagliflozin lowers HbA1c by 0.90 percentage points when added to metformin.

1: Hinnen D. Glucuretic effects and renal safety of dapagliflozin in patients with type 2 diabetes. Ther Adv Endocrinol Metab. 2015 Jun;6(3):92-102. doi: 10.1177/2042018815575273. Review. PubMed PMID: 26137213; PubMed Central PMCID: PMC4480550.

2: Liakos A, Karagiannis T, Bekiari E, Boura P, Tsapas A. Update on long-term efficacy and safety of dapagliflozin in patients with type 2 diabetes mellitus. Ther Adv Endocrinol Metab. 2015 Apr;6(2):61-7. doi: 10.1177/2042018814560735. Review. PubMed PMID: 25941564; PubMed Central PMCID: PMC4406879.

3: Vivian EM. Dapagliflozin: a new sodium-glucose cotransporter 2 inhibitor for treatment of type 2 diabetes. Am J Health Syst Pharm. 2015 Mar 1;72(5):361-72. doi: 10.2146/ajhp140168. Review. PubMed PMID: 25694411.

4: Filippatos TD, Liberopoulos EN, Elisaf MS. Dapagliflozin in patients with type 2 diabetes mellitus. Ther Adv Endocrinol Metab. 2015 Feb;6(1):29-41. doi: 10.1177/2042018814558243. Review. PubMed PMID: 25678954; PubMed Central PMCID: PMC4321869.

5: Sposetti G, MacKinnon I, Barengo NC. Dapagliflozin: drug profile and its role in individualized treatment. Expert Rev Cardiovasc Ther. 2015 Feb;13(2):129-39. doi: 10.1586/14779072.2015.995636. Epub 2015 Jan 6. Review. PubMed PMID: 25560982.

6: Anderson SL. Dapagliflozin efficacy and safety: a perspective review. Ther Adv Drug Saf. 2014 Dec;5(6):242-54. doi: 10.1177/2042098614551938. Review. PubMed PMID: 25436106; PubMed Central PMCID: PMC4232499.

7: Maranghi M, Carnovale A, Durante C, Tarquini G, Tiseo G, Filetti S. Pharmacokinetics, pharmacodynamics and clinical efficacy of dapagliflozin for the treatment of type 2 diabetes. Expert Opin Drug Metab Toxicol. 2015 Jan;11(1):125-37. doi: 10.1517/17425255.2015.986457. Epub 2014 Nov 24. Review. PubMed PMID: 25418019.

8: Plosker GL. Dapagliflozin: a review of its use in patients with type 2 diabetes. Drugs. 2014 Dec;74(18):2191-209. doi: 10.1007/s40265-014-0324-3. Review. PubMed PMID: 25389049.

9: Thomas MC. Renal effects of dapagliflozin in patients with type 2 diabetes. Ther Adv Endocrinol Metab. 2014 Jun;5(3):53-61. doi: 10.1177/2042018814544153. Review. PubMed PMID: 25126408; PubMed Central PMCID: PMC4132377.

10: Orme M, Fenici P, Lomon ID, Wygant G, Townsend R, Roudaut M. A systematic review and mixed-treatment comparison of dapagliflozin with existing anti-diabetes treatments for those with type 2 diabetes mellitus inadequately controlled by sulfonylurea monotherapy. Diabetol Metab Syndr. 2014 Jun 11;6:73. doi: 10.1186/1758-5996-6-73. eCollection 2014. Review. PubMed PMID: 25006351; PubMed Central PMCID: PMC4085736.

11: Aylsworth A, Dean Z, VanNorman C, Nkemdirim Okere A. Dapagliflozin for the Treatment of Type 2 Diabetes Mellitus. Ann Pharmacother. 2014 Jun 20;48(9):1202-1208. [Epub ahead of print] Review. PubMed PMID: 24951310.

12: Salvo MC, Brooks AD, Thacker SM. Patient considerations in the management of type 2 diabetes - critical appraisal of dapagliflozin. Patient Prefer Adherence. 2014 Apr 22;8:493-502. doi: 10.2147/PPA.S59169. eCollection 2014. Review. PubMed PMID: 24790417; PubMed Central PMCID: PMC4003262.

13: Balakumar P, Sundram K, Dhanaraj SA. Dapagliflozin: glucuretic action and beyond. Pharmacol Res. 2014 Apr;82:34-9. doi: 10.1016/j.phrs.2014.03.008. Epub 2014 Apr 3. Review. PubMed PMID: 24705156.

14: Albarrán OG, Ampudia-Blasco FJ. [Dapagliflozin, the first SGLT-2 inhibitor in the treatment of type 2 diabetes]. Med Clin (Barc). 2013 Sep;141 Suppl 2:36-43. doi: 10.1016/S0025-7753(13)70062-9. Review. Spanish. PubMed PMID: 24444523.

15: Goring S, Hawkins N, Wygant G, Roudaut M, Townsend R, Wood I, Barnett AH. Dapagliflozin compared with other oral anti-diabetes treatments when added to metformin monotherapy: a systematic review and network meta-analysis. Diabetes Obes Metab. 2014 May;16(5):433-42. doi: 10.1111/dom.12239. Epub 2013 Dec 16. Review. PubMed PMID: 24237939.

16: Kilov G, Leow S, Thomas M. SGLT2 inhibition with dapagliflozin -- a novel approach for the management of type 2 diabetes. Aust Fam Physician. 2013 Oct;42(10):706-10. Review. PubMed PMID: 24130972.

17: Zhang M, Zhang L, Wu B, Song H, An Z, Li S. Dapagliflozin treatment for type 2 diabetes: a systematic review and meta-analysis of randomized controlled trials. Diabetes Metab Res Rev. 2014 Mar;30(3):204-21. doi: 10.1002/dmrr.2479. Review. PubMed PMID: 24115369.

18: Kasichayanula S, Liu X, Lacreta F, Griffen SC, Boulton DW. Clinical pharmacokinetics and pharmacodynamics of dapagliflozin, a selective inhibitor of sodium-glucose co-transporter type 2. Clin Pharmacokinet. 2014 Jan;53(1):17-27. doi: 10.1007/s40262-013-0104-3. Review. PubMed PMID: 24105299.

19: Kleefstra N, Drion I, van Hateren KJ, Holleman F, Goudswaard AN, Bilo HJ. [SGLT-2 inhibitors: diabetes treatment by glycosuria; literature review on the effect of dapagliflozin]. Ned Tijdschr Geneeskd. 2013;157(38):A5969. Review. Dutch. PubMed PMID: 24050445.

20: Abdul-Ghani MA, DeFronzo RA. Dapagliflozin for the treatment of type 2 diabetes. Expert Opin Pharmacother. 2013 Aug;14(12):1695-703. doi: 10.1517/14656566.2013.812632. Epub 2013 Jun 26. Review. PubMed PMID: 23800130.

We produce Ipragliflozin, ASP1941, 761423-87-4 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok

Name: Ipragliflozin

CAS#: 761423-87-4

Chemical Formula: C21H21FO5S

Exact Mass: 404.1094

Molecular Weight: 404.4524

Elemental Analysis: C, 62.36; H, 5.23; F, 4.70; O, 19.78; S, 7.93

We produce Ipragliflozin, ASP1941, 761423-87-4 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Ipragliflozin, ASP1941, 761423-87-4 Intermediates, we have 8; Ipragliflozin, ASP1941, 761423-87-4 Impurity we have 10, all from GMP, FDA plant.

Now Ipragliflozin, ASP1941, 761423-87-4 DMF document is preparing.

Until 2016, Aug, Ipragliflozin, ASP1941, 761423-87-4 more than produced 25kg API, 120kg Intermediates

Ipragliflozin Suglat;ASP-1941 761423-87-4(free base)

Ipragliflozin Suglat;ASP-1941 951382-34-6(L-Proline)

Ipragliflozin Intermediates (2S,3R,4S,5S,6R)-2-(3-(benzo[b]thiophen-2-ylmethyl)-4-fluorophenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol 1034305-23-1

Ipragliflozin Intermediates (2S,3R,4S,5S,6R)-2-(3-(benzo[b]thiophen-2-ylmethyl)phenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol

Ipragliflozin Intermediates 2-(3-bromobenzyl)benzo[b]thiophene 898538-24-4

Ipragliflozin Intermediates benzo[b]thiophen-2-yl(5-bromo-2-fluorophenyl)methanol 1034305-11-7

Ipragliflozin Intermediates 2-(5-bromo-2-fluorobenzyl)benzo[b]thiophene 1034305-17-3

Ipragliflozin Intermediates (2S,3R,4R,5S,6R)-2-(3-(benzo[b]thiophen-2-ylmethyl)phenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol 761424-02-6

Description: Ipragliflozin, also known as ASP1941, is a potent and selective SGLT2 inhibitor for treatment of type 2 diabetes. Ipragliflozin treatment improved glycaemic control when added to metformin therapy and may be associated with weight loss and reductions in blood pressure compared to placebo. Ipragliflozin improves not only hyperglycemia but also diabetes/obesity-associated metabolic abnormalities in type 2 diabetic mice. It was approved for use in Japan in 2014.

Synonym: ASP1941; ASP-1941; ASP 1941; Ipragliflozin. Trade name: Suglat.

IUPAC/Chemical Name: (2S,3R,4R,5S,6R)-2-[3-(1-benzothiophen-2-ylmethyl)-4-fluorophenyl]-6-(hydroxymethyl)oxane-3,4,5-triol

SMILES Code: O[C@H]1[C@H](C2=CC=C(F)C(CC3=CC4=CC=CC=C4S3)=C2)O[C@H](CO)[C@@H](O)[C@@H]1O

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

21: Kashiwagi A, Kazuta K, Goto K, Yoshida S, Ueyama E, Utsuno A. Ipragliflozin in combination with metformin for the treatment of Japanese patients with type 2 diabetes: ILLUMINATE, a randomized, double-blind, placebo-controlled study. Diabetes Obes Metab. 2015 Mar;17(3):304-8. doi: 10.1111/dom.12331. Epub 2014 Jul 31. PubMed PMID: 24919820; PubMed Central PMCID: PMC4342773.

22: Poole RM, Dungo RT. Ipragliflozin: first global approval. Drugs. 2014 Apr;74(5):611-7. doi: 10.1007/s40265-014-0204-x. PubMed PMID: 24668021.

23: Tahara A, Kurosaki E, Yokono M, Yamajuku D, Kihara R, Hayashizaki Y, Takasu T, Imamura M, Li Q, Tomiyama H, Kobayashi Y, Noda A, Sasamata M, Shibasaki M. Effects of sodium-glucose cotransporter 2 selective inhibitor ipragliflozin on hyperglycaemia, oxidative stress, inflammation and liver injury in streptozotocin-induced type 1 diabetic rats. J Pharm Pharmacol. 2014 Jul;66(7):975-87. doi: 10.1111/jphp.12223. Epub 2014 Feb 17. PubMed PMID: 24533859.

24: Yokono M, Takasu T, Hayashizaki Y, Mitsuoka K, Kihara R, Muramatsu Y, Miyoshi S, Tahara A, Kurosaki E, Li Q, Tomiyama H, Sasamata M, Shibasaki M, Uchiyama Y. SGLT2 selective inhibitor ipragliflozin reduces body fat mass by increasing fatty acid oxidation in high-fat diet-induced obese rats. Eur J Pharmacol. 2014 Mar 15;727:66-74. doi: 10.1016/j.ejphar.2014.01.040. Epub 2014 Jan 30. PubMed PMID: 24486393.

25: Zhang W, Smulders R, Abeyratne A, Dietz A, Krauwinkel W, Kadokura T, Keirns J. Ipragliflozin does not prolong QTc interval in healthy male and female subjects: a phase I study. Clin Ther. 2013 Aug;35(8):1150-1161.e3. doi: 10.1016/j.clinthera.2013.06.009. Epub 2013 Aug 2. PubMed PMID: 23910665.

26: Zhang W, Krauwinkel WJ, Keirns J, Townsend RW, Lasseter KC, Plumb L, Kadokura T, Ushigome F, Smulders R. The effect of moderate hepatic impairment on the pharmacokinetics of ipragliflozin, a novel sodium glucose co-transporter 2 (SGLT2) inhibitor. Clin Drug Investig. 2013 Jul;33(7):489-96. doi: 10.1007/s40261-013-0089-6. PubMed PMID: 23733389.

27: Tahara A, Kurosaki E, Yokono M, Yamajuku D, Kihara R, Hayashizaki Y, Takasu T, Imamura M, Li Q, Tomiyama H, Kobayashi Y, Noda A, Sasamata M, Shibasaki M. Effects of SGLT2 selective inhibitor ipragliflozin on hyperglycemia, hyperlipidemia, hepatic steatosis, oxidative stress, inflammation, and obesity in type 2 diabetic mice. Eur J Pharmacol. 2013 Sep 5;715(1-3):246-55. doi: 10.1016/j.ejphar.2013.05.014. Epub 2013 May 23. PubMed PMID: 23707905.

28: Kurosaki E, Ogasawara H. Ipragliflozin and other sodium-glucose cotransporter-2 (SGLT2) inhibitors in the treatment of type 2 diabetes: preclinical and clinical data. Pharmacol Ther. 2013 Jul;139(1):51-9. doi: 10.1016/j.pharmthera.2013.04.003. Epub 2013 Apr 4. Review. PubMed PMID: 23563279.

29: Fonseca VA, Ferrannini E, Wilding JP, Wilpshaar W, Dhanjal P, Ball G, Klasen S. Active- and placebo-controlled dose-finding study to assess the efficacy, safety, and tolerability of multiple doses of ipragliflozin in patients with type 2 diabetes mellitus. J Diabetes Complications. 2013 May-Jun;27(3):268-73. doi: 10.1016/j.jdiacomp.2012.11.005. Epub 2012 Dec 29. PubMed PMID: 23276620.

30: Wilding JP, Ferrannini E, Fonseca VA, Wilpshaar W, Dhanjal P, Houzer A. Efficacy and safety of ipragliflozin in patients with type 2 diabetes inadequately controlled on metformin: a dose-finding study. Diabetes Obes Metab. 2013 May;15(5):403-9. doi: 10.1111/dom.12038. Epub 2012 Dec 7. PubMed PMID: 23163880.

31: Tahara A, Kurosaki E, Yokono M, Yamajuku D, Kihara R, Hayashizaki Y, Takasu T, Imamura M, Qun L, Tomiyama H, Kobayashi Y, Noda A, Sasamata M, Shibasaki M. Antidiabetic effects of SGLT2-selective inhibitor ipragliflozin in streptozotocin-nicotinamide-induced mildly diabetic mice. J Pharmacol Sci. 2012;120(1):36-44. Epub 2012 Aug 23. PubMed PMID: 22971845.

32: Veltkamp SA, van Dijk J, Collins C, van Bruijnsvoort M, Kadokura T, Smulders RA. Combination treatment with ipragliflozin and metformin: a randomized, double-blind, placebo-controlled study in patients with type 2 diabetes mellitus. Clin Ther. 2012 Aug;34(8):1761-71. doi: 10.1016/j.clinthera.2012.06.027. Epub 2012 Jul 15. PubMed PMID: 22795925.

33: Smulders RA, Zhang W, Veltkamp SA, van Dijk J, Krauwinkel WJ, Keirns J, Kadokura T. No pharmacokinetic interaction between ipragliflozin and sitagliptin, pioglitazone, or glimepiride in healthy subjects. Diabetes Obes Metab. 2012 Oct;14(10):937-43. doi: 10.1111/j.1463-1326.2012.01624.x. Epub 2012 Jun 7. PubMed PMID: 22587345.

34: Imamura M, Nakanishi K, Suzuki T, Ikegai K, Shiraki R, Ogiyama T, Murakami T, Kurosaki E, Noda A, Kobayashi Y, Yokota M, Koide T, Kosakai K, Ohkura Y, Takeuchi M, Tomiyama H, Ohta M. Discovery of Ipragliflozin (ASP1941): a novel C-glucoside with benzothiophene structure as a potent and selective sodium glucose co-transporter 2 (SGLT2) inhibitor for the treatment of type 2 diabetes mellitus. Bioorg Med Chem. 2012 May 15;20(10):3263-79. doi: 10.1016/j.bmc.2012.03.051. Epub 2012 Mar 29. PubMed PMID: 22507206.

35: Tahara A, Kurosaki E, Yokono M, Yamajuku D, Kihara R, Hayashizaki Y, Takasu T, Imamura M, Qun L, Tomiyama H, Kobayashi Y, Noda A, Sasamata M, Shibasaki M. Pharmacological profile of ipragliflozin (ASP1941), a novel selective SGLT2 inhibitor, in vitro and in vivo. Naunyn Schmiedebergs Arch Pharmacol. 2012 Apr;385(4):423-36. doi: 10.1007/s00210-011-0713-z. Epub 2011 Dec 3. PubMed PMID: 22139434.

36: Veltkamp SA, Kadokura T, Krauwinkel WJ, Smulders RA. Effect of Ipragliflozin (ASP1941), a novel selective sodium-dependent glucose co-transporter 2 inhibitor, on urinary glucose excretion in healthy subjects. Clin Drug Investig. 2011 Dec 1;31(12):839-51. doi: 10.2165/11594330-000000000-00000. PubMed PMID: 21877761.

37: Schwartz SL, Akinlade B, Klasen S, Kowalski D, Zhang W, Wilpshaar W. Safety, pharmacokinetic, and pharmacodynamic profiles of ipragliflozin (ASP1941), a novel and selective inhibitor of sodium-dependent glucose co-transporter 2, in patients with type 2 diabetes mellitus. Diabetes Technol Ther. 2011 Dec;13(12):1219-27. doi: 10.1089/dia.2011.0012. Epub 2011 Aug 19. PubMed PMID: 21854192.

We produce Ertugliflozin,PF-04971729,1210344-57-2 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Name: Ertugliflozin

CAS#: 1210344-57-2

Chemical Formula: C22H25ClO7

Exact Mass: 436.1289

Molecular Weight: 436.885

Elemental Analysis: C, 60.48; H, 5.77; Cl, 8.11; O, 25.63

We produce Ertugliflozin,PF-04971729,1210344-57-2 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Ertugliflozin,PF-04971729,1210344-57-2 Intermediates, we have 8; Ertugliflozin,PF-04971729,1210344-57-2 Impurity we have 10, all from GMP, FDA plant.

Now Ertugliflozin,PF-04971729,1210344-57-2 DMF document is preparing.

Until 2016, Aug, Ertugliflozin,PF-04971729,1210344-57-2 more than produced 25kg API, 120kg Intermediates

Ertugliflozin PF 04971729;MK-8835 1210344-57-2

Ertugliflozin Intermediates (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one 32384-65-9

Ertugliflozin Intermediates (2S,3R,4S,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol 714269-57-5

Ertugliflozin Intermediates (2S,3R,4S,5S)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6,6-bis(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol 1528636-39-6

Ertugliflozin Intermediates ((2R,3R,4S,5R,6S)-3,4,5-tris(benzyloxy)-6-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-methoxytetrahydro-2H-pyran-2-yl)methanol

Ertugliflozin Intermediates ((1S,2S,3S,4R,5S)-2,3,4-tris(benzyloxy)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6,8-dioxabicyclo[3.2.1]octan-1-yl)methanol

Ertugliflozin Intermediates 4-bromo-1-chloro-2-(4-ethoxybenzyl)benzene 461432-23-5

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO, not in water

Shelf Life: >2 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Description: Ertugliflozin, also known as also known as PF-04971729, is a potent and selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. clinical study showed that Ertugliflozin (1-25 mg/day) improved glycaemic control, body weight and blood pressure in patients with T2DM suboptimally controlled on metformin, and was well tolerated.

Synonym: PF-04971729; PF 04971729; PF04971729; PF-04971729-00; Ertugliflozin

IUPAC/Chemical Name: (1S,2S,3S,4R,5S)-5-(4-Chloro-3-(4-ethoxybenzyl)phenyl)-1-hydroxymethyl-6,8-dioxabicyclo(3.2.1)octane-2,3,4-triol

SMILES Code: O[C@@H]1[C@](O2)(CO)CO[C@]2(C3=CC=C(Cl)C(CC4=CC=C(C=C4)OCC)=C3)[C@H](O)[C@H]1O

1: Jiang M, Steyger PS. An evaluation of US patent 2015065565 (A1) for a new

class of SGLT2 inhibitors for treatment 1 of type II diabetes mellitus. Expert

Opin Ther Pat. 2015;25(11):1349-52. doi: 10.1517/13543776.2015.1076392. Epub 2015

Aug 6. PubMed PMID: 26291462; PubMed Central PMCID: PMC4635049.

2: Amin NB, Wang X, Mitchell JR, Lee DS, Nucci G, Rusnak JM. Blood

pressure-lowering effect of the sodium glucose co-transporter-2 inhibitor

ertugliflozin, assessed via ambulatory blood pressure monitoring in patients with

type 2 diabetes and hypertension. Diabetes Obes Metab. 2015 Aug;17(8):805-8. doi:

10.1111/dom.12486. Epub 2015 Jun 17. PubMed PMID: 25951755.

3: Amin NB, Wang X, Jain SM, Lee DS, Nucci G, Rusnak JM. Dose-ranging efficacy

and safety study of ertugliflozin, a sodium-glucose co-transporter 2 inhibitor,

in patients with type 2 diabetes on a background of metformin. Diabetes Obes

Metab. 2015 Jun;17(6):591-8. doi: 10.1111/dom.12460. Epub 2015 Mar 31. PubMed

PMID: 25754396.

4: Miao Z, Nucci G, Amin N, Sharma R, Mascitti V, Tugnait M, Vaz AD, Callegari E,

Kalgutkar AS. Pharmacokinetics, metabolism, and excretion of the antidiabetic

agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos.

2013 Feb;41(2):445-56. doi: 10.1124/dmd.112.049551. Epub 2012 Nov 20. PubMed

PMID: 23169609.

5: Kalgutkar AS, Tugnait M, Zhu T, Kimoto E, Miao Z, Mascitti V, Yang X, Tan B,

Walsky RL, Chupka J, Feng B, Robinson RP. Preclinical species and human

disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose

cotransporter 2 and clinical candidate for the treatment of type 2 diabetes

mellitus. Drug Metab Dispos. 2011 Sep;39(9):1609-19. doi: 10.1124/dmd.111.040675.

Epub 2011 Jun 20. PubMed PMID: 21690265.

GMP: Omarigliptin, MK-3102, 1226781-44-7

Description: Omarigliptin, also known as MK-3102, is a potent and long-acting DPP-4 inhibitor for once-weekly treatment of type 2 diabetes. MK-3102 (omarigliptin), was identified as a potent and selective dipeptidyl peptidase 4 (DPP-4) inhibitor with an excellent pharmacokinetic profile amenable for once-weekly human dosing and selected as a clinical development candidate. Omarigliptin is currently in phase 3 clinical development.

Synonym: MK3102; MK-3102; MK 3102; Omarigliptin

IUPAC/Chemical Name: (2R,3S,5R)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine

SMILES Code: N[C@@H]1[C@@H](C2=CC(F)=CC=C2F)OC[C@H](N3CC4=NN(S(=O)(C)=O)C=C4C3)C1

Name: Omarigliptin 
CAS#: 1226781-44-7 
Chemical Formula: C17H20F2N4O3S 
Exact Mass: 398.12242 
Molecular Weight: 398.43 
Elemental Analysis: C, 51.25; H, 5.06; F, 9.54; N, 14.06; O, 12.05; S, 8.05We produce Omarigliptin, MK-3102, 1226781-44-7 in GMP plant, C-GMP standard, now COA, NMR, HPLC, MS is ok.

Omarigliptin, MK-3102, 1226781-44-7 Intermediates, we have 8; Omarigliptin, MK-3102, 1226781-44-7 Impurity we have 10, all from GMP, FDA plant.

Now Omarigliptin, MK-3102, 1226781-44-7 DMF document is preparing.

Until 2016, Aug, Omarigliptin, MK-3102, 1226781-44-7 more than produced 25kg API, 120kg Intermediates

Omarigliptin	MK-3102;Marizev	1226781-44-7
Omarigliptin Intermediates	(2S,3R,5S)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine	1443380-88-8
Omarigliptin Intermediates	Tert-butyl 4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate	1280210-79-8
Omarigliptin Intermediates	2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole 4-methylbenzenesulfonate	18193664-02-7
Omarigliptin Intermediates	Tert-butyl 2-(methylsulfonyl)-4,6-dihydropyrrolo[3,4-c]pyrazole-5(2H)-carboxylate	1226781-82-3
Omarigliptin Intermediates	(Z)-tert-butyl 3-((dimethylamino)methylene)-4-oxopyrrolidine-1-carboxylate	905274-02-4
Omarigliptin Intermediates	Tert-butyl 6a-hydroxy-1,2,6,6a-tetrahydropyrrolo[3,4-c]pyrazole-5(4H)-carboxylate	1211594-55-6
Omarigliptin Intermediates	2-(methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole	1226781-80-1
Omarigliptin Intermediates	2-(methylsulfonyl)-2,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole benzenesulfonate	1280210-80-1
Omarigliptin Intermediates	Tert-butyl ((2R,3R)-2-(2,5-difluorophenyl)-5-oxotetrahydro-2H-pyran-3-yl)carbamate	1456616-43-5
Omarigliptin Intermediates	Tert-butyl ((2S,3S)-2-(2,5-difluorophenyl)-5-oxotetrahydro-2H-pyran-3-yl)carbamate	1456616-44-6
Omarigliptin Intermediates	(2R,3R,5R)-2-(2,5-difluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine
Omarigliptin Intermediates	(2R,3S,5R)-2-(2,5-difluorophenyl)-5-(pyrrolo[3,4-c]pyrazol-5(1H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine
Omarigliptin Intermediates	Tert-butyl ((2R,3S)-2-(2,5-difluorophenyl)-5-hydroxytetrahydro-2H-pyran-3-yl)carbamate	1172623-99-2
Omarigliptin Intermediates	2-((tert-butoxycarbonyl)amino)pent-4-ynoic acid	61172-66-5
Omarigliptin Intermediates	Tert-butyl (1-(methoxy(methyl)amino)-1-oxopent-4-yn-2-yl)carbamate	172623-95-8
Omarigliptin Intermediates	Tert-butyl (1-(2,5-difluorophenyl)-1-oxopent-4-yn-2-yl)carbamate	1172623-96-9
Omarigliptin Intermediates	(2R,3S,5R)-2-(3-fluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine impurity A
Omarigliptin Intermediates	(2R,3S,5R)-2-(2-fluorophenyl)-5-(2-(methylsulfonyl)pyrrolo[3,4-c]pyrazol-5(2H,4H,6H)-yl)tetrahydro-2H-pyran-3-amine impurity B