Ertugliflozin L-pyroglutamic acid

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Chemical Structure| 1210344-83-4 同义名 : PF-04971729 L-pyroglutamic acid; MK-8835 L-pyroglutamic acid
CAS号 : 1210344-83-4
货号 : A1006406
分子式 : C27H32ClNO10
纯度 : 99%
分子量 : 566.0
MDL号 : MFCD27956909
存储条件：

Pure form Inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(212.02 mM)，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 5 mg/mL(8.83 mM)，配合低频超声，并水浴加热至45℃助溶
生物活性
描述 Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) is a potent, selective, and orally administered inhibitor of the sodium-dependent glucose cotransporter 2 (SGLT2), exhibiting an IC50 of 0.877 nM against h-SGLT2[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.77mL

0.35mL

0.18mL

8.83mL

1.77mL

0.88mL

17.67mL

3.53mL

1.77mL
参考文献

[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]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.