| Bioactivity | Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), with an IC50 of 0.877 nM for h-SGLT2[1]. Has the potential for the treatment of type 2 diabetes mellitus[2]. | ||||||||||||
| Invitro | Ertugliflozin (PF-04971729) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) in vitro[3]. | ||||||||||||
| In Vivo | Ertugliflozin (PF-04971729) reveals a concentration-dependent glucosuria after oral administration to rats[3]. | ||||||||||||
| Name | Ertugliflozin | ||||||||||||
| CAS | 1210344-57-2 | ||||||||||||
| Formula | C22H25ClO7 | ||||||||||||
| Molar Mass | 436.88 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Mascitti V, et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011 Apr 28;54(8):2952-60. [2]. Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56. [3]. Kalgutkar AS, et al. 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. |
Ertugliflozin
CAS: 1210344-57-2 F: C22H25ClO7 W: 436.88
Ertugliflozin (PF-04971729) is a potent, selective and orally active inhibitor of the sodium-dependent glucose cotranspo
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