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
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.
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!
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Skype: willgutian
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.
