Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MK-8617 是一种口服具有活力的低氧诱导因子脯氨酰羟化酶 1-3 (HIF PHD1-3) 泛抑制剂,对于PHD2的IC50=1 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 248 | 现货 | ||
2 mg | ¥ 368 | 现货 | ||
5 mg | ¥ 638 | 现货 | ||
10 mg | ¥ 887 | 现货 | ||
25 mg | ¥ 1,720 | 现货 | ||
50 mg | ¥ 3,260 | 现货 | ||
100 mg | ¥ 4,770 | 现货 | ||
200 mg | ¥ 6,780 | 现货 | ||
500 mg | ¥ 9,870 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 759 | 现货 |
产品描述 | MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM). |
靶点活性 | PHD3:14 nM, PHD1:1 nM, PHD2:1 nM |
体外活性 | In vitro, MK-8617 hasn't markedly inhibitory for CYP1A2, 3A4, 2B6, 2C9, 2C19, or 2D6 (IC50>60 μM), and is a moderate reversible inhibitor of CYP2C8 (IC50: 1.6 μM). MK-8617 (10 μM) is inactive against a general panel of 171 radioligand binding and enzymatic assays. |
体内活性 | In liver microsomes (+NADPH) from rat, dog, and monkey, tritiated MK-8617 exhibits minimal metabolic turnover (<10%), but the significant turnover (34%) in HLMs after 60 min (10 μM compound, 1 mg/mL microsomal protein). MK-8617 has good oral bioavailability across species (36?71%), with low clearance and volume of distribution. Increases in circulating reticulocytes are observed at 5 and 15 mg/kg 3 days after challenge and at the 15 mg/kg 4 days after challenge. |
别名 | MK8617 |
分子量 | 443.45 |
分子式 | C24H21N5O4 |
CAS No. | 1187990-87-9 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 16 mg/mL (36.1 mM)
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 2.255 mL | 11.2752 mL | 22.5505 mL | 56.3761 mL |
5 mM | 0.451 mL | 2.255 mL | 4.5101 mL | 11.2752 mL | |
10 mM | 0.2255 mL | 1.1275 mL | 2.255 mL | 5.6376 mL | |
20 mM | 0.1128 mL | 0.5638 mL | 1.1275 mL | 2.8188 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。
MK-8617 1187990-87-9 Chromatin/Epigenetic Metabolism HIF/HIF Prolyl-Hydroxylase MK 8617 HIF-PH inhibit Hypoxia-inducible factors MK8617 HIFs Inhibitor inhibitor