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MK-8617

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。

CAS号

1187990-87-9

分子式

C24H21N5O4

主要靶点

HIF/HIF Prolyl-Hydroxylase

仅限科研使用

Cat No : CM04470

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Synonyms

MK8617

验证数据展示

  • CAS No.: 1187990-87-9

    MK-8617
    CAS#: 1187990-87-9

产品信息

MK-8617 is an orally available HIF PHD1 3 pan-inhibitor, inhibiting PHD1/2/3 (IC50: 1.0/1.0/14 nM).

CAS号 1187990-87-9
分子式 C24H21N5O4
主要靶点 HIF/HIF Prolyl-Hydroxylase
主要通路 表观遗传|代谢
分子量 443.45
纯度 99.50%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名 MK8617

靶点活性

PHD1:1 nM|PHD3:14 nM|PHD2:1 nM

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.

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.

溶解度

DMSO:16 mg/mL (36.1 mM)

参考文献

1.John S. Debenham, et al. J Med Chem. 2016, 59 (24):11039-11049.

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2

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