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1361224-53-4

中文名稱(chēng) AMG-3969
英文名稱(chēng) AMG-3969
CAS 1361224-53-4
更新日期 2026/06/01 10:25:42
分子式 C21H20F6N4O3S
分子量 522.46
MOL 文件 1361224-53-4.mol
1361224-53-4 結(jié)構(gòu)式 1361224-53-4 結(jié)構(gòu)式

基本信息

中文別名
化合物AMG-3969
AMG-3969游離態(tài)
4-[(2S)-4-[(6-氨基-3-吡啶基)磺?;鵠-2-(1-丙炔-1-基)-1-哌嗪基]-Α,Α-雙(三氟甲基)-苯甲醇
(S)-2-(4-(4-((6-氨基吡啶-3-基)磺?;?-2-(丙-1-炔-1-基)哌嗪-1-基)苯基)-1,1,1,3,3-六氟丙烷-2-醇
英文別名
AMG-3969
所屬類(lèi)別
生物化工:激動(dòng)劑抑制劑

物理化學(xué)性質(zhì)

沸點(diǎn)648.8±65.0 °C(Predicted)
密度1.56±0.1 g/cm3(Predicted)
儲(chǔ)存條件2-8°C(protect from light)
溶解度DMSO:100.0(Max Conc. mg/mL);191.4(Max Conc. mM)
酸度系數(shù)(pKa)10.12±0.15(Predicted)
形態(tài)Solid
顏色White to off-white

安全數(shù)據(jù)

危險(xiǎn)性符號(hào)(GHS)有害 (GHS07)
GHS07
警示詞警告
危險(xiǎn)性描述H302-H315-H319-H335
防范說(shuō)明P261-P305+P351+P338
海關(guān)編碼2935909099
AMG-3969價(jià)格(試劑級(jí))
報(bào)價(jià)日期產(chǎn)品編號(hào)產(chǎn)品名稱(chēng)CAS號(hào)包裝價(jià)格
2026/06/05HY-12411AMG-3969
AMG-3969
1361224-53-41mg993元
2026/06/05HY-12411AMG-3969
AMG-3969
1361224-53-45mg2320元
2026/06/05HY-12411AMG-3969
AMG-3969
1361224-53-410mM * 1mLin DMSO2667元

常見(jiàn)問(wèn)題列表

生物活性
AMG-3969是有效的葡萄糖激酶-葡糖激酶調(diào)節(jié)蛋白(GK-GKRP)相互作用的干擾物,IC50值為4 nM。
靶點(diǎn)

IC50: 4 nM (GK-GKRP)

體外研究

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).

體內(nèi)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.

"1361224-53-4" 相關(guān)產(chǎn)品信息
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