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AMG-3969  ≥98%

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包装规格：1mg 5mg 10mg 50mg 100mg in glass bottle
溶解性：溶于DMSO(≥100mg/ml)
产品描述：基本信息 产品编号： A12361 产品名称： AMG-3969 CAS: 1361224-53-4   储存条件 粉末 -20℃ 四年     分子式： C21H20F6N4O3S 溶于液体 -80℃ 六个月 分子量 522.46 -20℃ 一个月 化学名：  2-[4-[(2S)-4-(6-aminopyridin-3-yl)sulfonyl-2-prop-1-ynylpiperazin-1-yl]phenyl]-1,1,1,3,3,3-hexafluoropropan-2-ol Solubility (25°C)：   体外:   DMSO ≥ 100mg/mL (191.40mM) Ethanol   Water   体内(现配现用): 1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility: ≥ 2.5mg/mL (4.79mM); Clear solution 此⽅案可获得 ≥ 2.5mg/mL (4.79mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 400μL PEG300 中，混合均匀；向上述体系中加⼊ 50μL Tween-80，混合均匀；然后继续加⼊ 450μL ⽣理盐⽔定容⾄ 1mL。 2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility: ≥ 2.5mg/mL (4.79mM); Clear solution 此⽅案可获得 ≥ 2.5mg/mL (4.79mM，饱和度未知) 的澄清溶液。 以 1mL ⼯作液为例，取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 900μL 20% 的 SBE-β-CD ⽣理盐⽔⽔溶液中，混合均匀。 3.请依序添加每种溶剂：10% DMSO→90% corn oil Solubility: ≥ 2.5mg/mL (4.79mM); Clear solution 此⽅案可获得 ≥ 2.5mg/mL (4.79mM，饱和度未知) 的澄清溶液，此⽅案不适⽤于实验周期在半个⽉以上的实验。 以 1mL ⼯作液为例，取 100μL 25.0mg/mL 的澄清 DMSO 储备液加到 900μL ⽟⽶油中，混合均匀。 ＜1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。   制备储备液   浓度   溶液体积 质量   1mg   5mg   10mg 1mM 1.9140mL 9.5701mL 19.1402mL 5mM 0.3828mL 1.9140mL 3.8280mL 10mM 0.1914mL 0.9570mL 1.9140mL   生物活性 产品描述 一种有效的葡萄糖激酶-葡糖激酶调节蛋白(GK-GKRP)相互作用的干扰物，IC50值为4nM。 靶点 IC50: 4nM (GK-GKRP) 体外研究 AMG-3969 exhibits potent cellular activity with an EC50 of 0.202μM and IC50 of 4nM. 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 (100mg/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   推荐实验方法(仅供参考) Animal Administration Mice: Diabetic db/db mice are used in the study. At 8:00 AM, mice are bled via retro-orbital sinus puncture and blood glucose values are determined and used to randomize the animals in which their averages are similar, and only mice with blood glucose ranges between 300 and 500mg/dL are included. Vehicle (2% hydroxypropyl methycellulose, 1% Tween 80, pH 2.2 adjusted with MSA) or AMG-3969 (10, 30, 100mg/kg) are gavaged at 9:00 AM. Blood glucose is measured at 4, 6, or 8 h posttreatment. At each time point, a 15μL sample of whole blood is analyzed for drug exposure
保存条件：-20℃

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