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Ertugliflozin L-pyroglutamic acid {[allProObj[0].p_purity_real_show]}

货号:A1006406 同义名: PF-04971729 L-pyroglutamic acid;MK-8835 L-pyroglutamic acid

Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) 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]. A drug for the treatment of type 2 diabetes mellitus[2].

Ertugliflozin L-pyroglutamic acid 化学结构 CAS号:1210344-83-4
Ertugliflozin L-pyroglutamic acid 化学结构
CAS号:1210344-83-4
Ertugliflozin L-pyroglutamic acid 3D分子结构
CAS号:1210344-83-4
Ertugliflozin L-pyroglutamic acid 化学结构 CAS号:1210344-83-4
Ertugliflozin L-pyroglutamic acid 3D分子结构 CAS号:1210344-83-4
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Ertugliflozin L-pyroglutamic acid 纯度/质量文件 产品仅供科研

货号:A1006406 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 SGLT1 SGLT2 其他靶点 纯度
Phloretin 98%
Canagliflozin +++

hSGLT2, IC50: 3.7 nM

mSGLT2, IC50: 2 nM

95%
Empagliflozin ++

SGLT2, IC50: 3.1 nM

98%
Dapagliflozin ++++

hSGLT2, EC50: 1.1 nM

97%
Tofogliflozin (hydrate) +++

hSGLT2, IC50: 2.9 nM

99%+
Sotagliflozin +

SGLT1, IC50: 36 nM

++++

SGLT2, IC50: 1.8 nM

98%
Ipragliflozin ++

hSGLT2, IC50: 7.4 nM

98%
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Ertugliflozin L-pyroglutamic acid 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].
体内研究

Ertugliflozin L-pyroglutamic acid induces a dose-dependent increase in glucose excretion in the urine following its oral delivery to rats, demonstrating its effectiveness in promoting glucosuria[3].

体外研究

In vitro, Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) [3].

Ertugliflozin L-pyroglutamic acid 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.

Ertugliflozin L-pyroglutamic acid 实验方案

计算器
存储液制备 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

Ertugliflozin L-pyroglutamic acid 技术信息

CAS号1210344-83-4
分子式C27H32ClNO10
分子量 565.997
别名 PF-04971729 L-pyroglutamic acid;MK-8835 L-pyroglutamic acid
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C

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

动物实验配方
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