Powder: -20°C for 3 years | In solvent: -80°C for 1 year
PF-04991532 is an effective, hepatoselective glucokinase activator. It has EC50s of 80 and 100 nM in human and rat, respectively.
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
2 mg | ¥ 534 | 5日内发货 | ||
5 mg | ¥ 977 | 5日内发货 | ||
50 mg | ¥ 5,310 | 6-8周 | ||
100 mg | ¥ 8,980 | 6-8周 | ||
1 mL * 10 mM (in DMSO) | ¥ 987 | 5日内发货 |
产品描述 | PF-04991532 is an effective, hepatoselective glucokinase activator. It has EC50s of 80 and 100 nM in human and rat, respectively. |
靶点活性 | GK (rat):100 nM(EC50), GK (human):(EC50)80 nM |
体外活性 | PF-04991532 is a Phase 2 clinical candidate. PF-04991532 reduces the production of glucose from 1-[14C]-lactate in a dose-dependent manner (EC50?=0.626 μM). PF-04991532 enhances the expression of G6Pase compare to cells treated only with 100 nM glucagon, in isolated rat hepatocytes. The greatest increase in G6Pase mRNA expression is in the presence of 25 mM glucose, 100 nM glucagon, and PF-04991532. Mechanistic experiments conducted in freshly isolated primary rat hepatocytes treated for 1 hour with PF-04991532 display increased 2-[14C]-deoxyglucose uptake (EC50?=1.261 μM) and increased glucose oxidation (EC50=5.769 μM) [1]. |
体内活性 | PF-04991532 (a single dose) enhances the glucose infusion rate in order to maintain hyperglycemia. PF-04991532 (in rats) treatment, there is increased expression of lipogenic gene expression such as acetyl-CoA carboxylase (ACC), ATP citrate lyase (ACLY), and fatty acid synthase (FAS). Despite the elevations in plasma triglycerides, hepatic triglycerides in rats dosed with 19 days of PF-04991532 are identical to vehicle-treated GK rats. Identical hepatic lipid concentrations are observed between vehicle and rats dosed with PF-04991532 (Vehicle: 9.89±0.31; PF-04991532 100 mg/kg: 9.91±0.31), in an additional cohort treated for 28 days [1]. |
分子量 | 396.36 |
分子式 | C18H19F3N4O3 |
CAS No. | 1215197-37-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
PF-04991532 1215197-37-7 Metabolism Glucokinase PF04991532 PF 04991532 Inhibitor inhibitor inhibit