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.
