Powder: -20°C for 3 years | In solvent: -80°C for 1 year
Pemafibrate ((R)-K-13675) 是一种高度特异性的 PPARα 激动剂 (EC50: 1 nM)。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 358 | 现货 | ||
5 mg | ¥ 863 | 现货 | ||
10 mg | ¥ 1,330 | 现货 | ||
25 mg | ¥ 2,580 | 现货 | ||
50 mg | ¥ 3,790 | 现货 | ||
100 mg | ¥ 5,390 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 986 | 现货 |
产品描述 | Pemafibrate ((R)-K-13675) is a highly specific PPARα agonist (EC50: 1 nM). |
靶点活性 | PPARγ (human):1.1 μM (EC50), PPARα (human):1 nM (EC50) |
体外活性 | Pemafibrate是一种强效的PPARα激动剂,对h-PPARα、h-PPARγ和h-PPARδ的EC50分别为1 nM、1.10 μM和1.58 μM。 |
体内活性 | Pemafibrate(3 mg/kg,口服)在人类apoA-I转基因小鼠中增加血浆h-apoA-I的水平,并且与fenofibrate 300 mg/kg相比,显示出更高的血浆h-apoA-I水平[1]。Pemafibrate(0.03 mg/kg)能降低PEMA-L(db/db)小鼠中的甘油三酯和天门冬氨酸转氨酶(AST)水平。Pemafibrate(0.1 mg/kg)不仅展现了上述效果,而且在PEMA-H(db/db)小鼠中增加了肝脏重量。Pemafibrate增强了非酒精性脂肪肝炎(NASH)啮齿动物模型中的病理发展。Pemafibrate显著降低了PEMA-H小鼠中肝细胞球形膨胀的程度[2]。含有Pemafibrate(K-877,0.0005%)的高脂饮食(HFD)抑制了小鼠的体重增加。Pemafibrate显著降低了小鼠餐后血浆中富含甘油三酯(TG)的脂蛋白,包括残留物的丰度。Pemafibrate还降低了小鼠肠道ApoB和Npc1l1的mRNA表达[3]。 |
动物实验 | Mice are fasted for 12?h and fasting blood glucose measured. Nine-week-old db/db mice are used in the assay. After a 2-week acclimatization period, mice are divided into four groups: BD (db/db) mice (fed basal diet (BD) and treated with 0.5% aqueous methylcellulose solution (MC); MCD (db/db) mice (fed methionine choline-deficient (MCD) and treated with 0.5% MC); PEMA-L (db/db) mice (fed MCD and treated with 0.03?mg/kg Pemafibrate); PEMA-H (db/db) mice (fed MCD and treated with 0.1?mg/kg Pemafibrate). The drug-free solvent or the dosing solution is administered to animals (5?mL/kg body weight, p.o.) once daily (in the morning) for 4 consecutive weeks. After a 2-week acclimatization period, BD mice are fed a BD for 20 weeks. CTRL mice are fed D09100301 for 20 weeks. PEMA-L and PEMA-H mice are fed D09100301 for 12 weeks followed by D09100301 with 0.4?mg and 1.3?mg Pemafibrate/kg of the diet for 8 weeks, which corresponds to 0.03?mg/kg/day and 0.1?mg/kg/day, respectively. FENO mice are fed D09100301 for 12 weeks followed by D09100301 with 666.7?mg fenofibrate/kg of the diet for 8 weeks, which corresponds to 50?mg/kg/day. Pemafibrate and fenofibrate are incorporated into the AMLN diet. Animals are housed under conventional conditions with controlled temperature, humidity, and light (12-h light-dark cycle) and provided with food and water [2]. |
别名 | (R)-K-13675 |
分子量 | 490.55 |
分子式 | C28H30N2O6 |
CAS No. | 848259-27-8 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
H2O: Insoluble
DMSO: 100 mg/mL (203.85 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.0385 mL | 10.1926 mL | 20.3853 mL | 50.9632 mL |
5 mM | 0.4077 mL | 2.0385 mL | 4.0771 mL | 10.1926 mL | |
10 mM | 0.2039 mL | 1.0193 mL | 2.0385 mL | 5.0963 mL | |
20 mM | 0.1019 mL | 0.5096 mL | 1.0193 mL | 2.5482 mL | |
50 mM | 0.0408 mL | 0.2039 mL | 0.4077 mL | 1.0193 mL | |
100 mM | 0.0204 mL | 0.1019 mL | 0.2039 mL | 0.5096 mL |
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。
Pemafibrate 848259-27-8 DNA Damage/DNA Repair Metabolism PPAR K13675 K 13675 K-13675 (R)-K-13675 Inhibitor inhibitor inhibit