1361224-53-4

中文名称 AMG-3969

英文名称 AMG-3969

CAS 1361224-53-4

更新日期 2024/07/04 11:32:51

分子式 C21H20F6N4O3S

分子量 522.46

MOL 文件 1361224-53-4.mol

1361224-53-4 结构式

基本信息物理化学性质安全数据 AMG-3969价格(试剂级) 常见问题列表

基本信息

中文别名

化合物AMG-3969
AMG-3969游离态
4-[(2S)-4-[(6-氨基-3-吡啶基)磺酰基]-2-(1-丙炔-1-基)-1-哌嗪基]-Α,Α-双(三氟甲基)-苯甲醇
(S)-2-(4-(4-((6-氨基吡啶-3-基)磺酰基)-2-(丙-1-炔-1-基)哌嗪-1-基)苯基)-1,1,1,3,3-六氟丙烷-2-醇

英文别名

AMG-3969

所属类别

生物化工：激动剂抑制剂

物理化学性质

沸点648.8±65.0 °C(Predicted)

密度1.56±0.1 g/cm3(Predicted)

储存条件2-8°C(protect from light)

溶解度DMSO:100.0(Max Conc. mg/mL);191.4(Max Conc. mM)

酸度系数(pKa)10.12±0.15(Predicted)

形态Solid

颜色White to off-white

安全数据

危险性符号(GHS)

GHS07

警示词警告

危险性描述H302-H315-H319-H335

防范说明P261-P305+P351+P338

海关编码2935909099

AMG-3969价格(试剂级)

报价日期	产品编号	产品名称	CAS号	包装	价格
2024/04/30	HY-12411	AMG-3969 AMG-3969	1361224-53-4	1mg	1200元
2024/04/30	HY-12411	AMG-3969 AMG-3969	1361224-53-4	5mg	2800元
2024/04/30	HY-12411	AMG-3969 AMG-3969	1361224-53-4	10mM * 1mLin DMSO	3218元

常见问题列表

生物活性

AMG-3969是有效的葡萄糖激酶-葡糖激酶调节蛋白(GK-GKRP)相互作用的干扰物，IC50值为4 nM。

靶点

IC50: 4 nM (GK-GKRP)

体外研究

AMG-3969 exhibits potent cellular activity with an EC ₅₀ of 0.202 μM and IC ₅₀ of 4 nM, . It potently reverses the inhibitory effect of GKRP on GK activity and promotes GK translocation in vitro (isolated hepatocytes).

体内研究

AMG-3969 has good in vivo pharmacokinetic (PK) properties in rats (75%) and significantly lowers blood glucose levels in a dose-dependent manner db/db mice. AMG-3969 (100 mg/kg) demonstrates significant reductions in blood glucose with robust efficacy (56% reduction) observed at the 8 h time point. AMG-3969 demonstrates dose-dependent efficacy in three models of diabetes: diet induced obese (DIO), ob/ob and db/db mice; however,AMG-3969 is ineffective in lowering blood glucose in normoglycaemic C57BL/6 (B6) mice. AMG-3969 is highly effective in promoting carbohydrate substrate. AMG-3969 exhibits extended changes to carbohydrate oxidation as observed by increased respiratory exchange ratio into the next night and day after a single dose.