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CAS No.: 1210344-57-2

埃格列净 Catalog No. CSN15831

Synonyms: PF-04971729;PF-4971729;PF-04971729-00

PF-04971729 is a selective sodium-dependent glucose cotransporter (SGLT) inhibitor which selectively targets SGLT2.

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400-920-2911

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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].
临床研究
NCT号适应症或疾病临床期招募状态预计完成时间地点
NCT01958671 - - Completed - -
NCT01999218 Type 2 Diabetes Mellitus Phase 3 Completed - -
NCT02630706 Type 2 Diabetes Mellitus Phase 3 Completed - -
更多
参考文献

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT01958671	-	-	Completed	-	-
NCT01999218	Type 2 Diabetes Mellitus	Phase 3	Completed	-	-
NCT02630706	Type 2 Diabetes Mellitus	Phase 3	Completed	-	-

[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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2889 mL
- 11.4447 mL
- 22.8894 mL
- 5 mM
- 0.4578 mL
- 2.2889 mL
- 4.5779 mL
- 10 mM
- 0.2289 mL
- 1.1445 mL
- 2.2889 mL

技术信息

CAS号

1210344-57-2

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H25ClO7

运输

蓝冰

分子量

436.88

别名

PF-04971729;PF-4971729;PF-04971729-00;Steglatro;埃格列净

溶解度

DMSO	86.0 mg/mL (196.8 mM)
Water	85.0 mg/mL (194.6 mM)
Ethanol	85.0 mg/mL (194.6 mM)

动物实验配方

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