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Ertugliflozin

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Chemical Structure| 1210344-57-2 同义名 : PF-04971729;MK-8835
CAS号 : 1210344-57-2
货号 : A191432
分子式 : C22H25ClO7
纯度 : 98%
分子量 : 436.883
MDL号 : MFCD21609259
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(572.24 mM)，配合低频超声助溶，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
动物实验配方：
生物活性
描述 Type 2 diabetes mellitus (T2DM) is a growing and serious global health problem. Pharmacological inhibition of the sodium–glucose cotransporter-2 (SGLT2) increases urinary glucose excretion, decreasing plasma glucose levels in an insulin-independent manner. PF-04971729 is a potent and selective SGLT2 inhibitor with IC50 value of 0.877 nM for h-SGLT2 and it has a 2000-fold increase in selectivity for human SGLT2 over SGLT1 in vitro. Diseases or conditions that can be ameliorated by inhibition of SGLT2 with PF-04971729 include: Type II diabetes, diabetic nephropathy, insulin resistance syndrome, hyperglycemia, hyperinsulinemia, hyperlipidemia, impaired glucose tolerance, obesity (including weight control or weight maintenance), hypertension and reducing the level of blood glucose. PF-04971729 can also be used for treating analogous diseases or conditions in animals. PF-04971729 is rapidly absorbed in preclinical species after oral administration, and it is characterized by low clearance and a moderate steady-state distribution volume. PF-04971729 is well absorbed in humans and eliminated largely via glucuronidation. PF-04971729 improved glycemic control, body weight and blood pressure in 328 patients with T2DM suboptimally controlled on metformin, and was well-tolerated[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.29mL

0.46mL

0.23mL

11.44mL

2.29mL

1.14mL

22.89mL

4.58mL

2.29mL
参考文献

[1]Miao Z, Nucci G, 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.

[2]Mascitti V, Maurer TS, Robinson RP, Bian J, Boustany-Kari CM, Brandt T, Collman BM, Kalgutkar AS, Klenotic MK, Leininger MT, Lowe A, Maguire RJ, Masterson VM, Miao Z, Mukaiyama E, Patel JD, Pettersen JC, Preville C, Samas B, She L, Sobol Z, 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.

[3]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):1349-1352.