您好,欢迎来到试剂仪器网! [登录] [免费注册]
试剂仪器网
位置:首页 > 产品库 > MK-8617
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
MK-8617
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
MK-8617图片
CAS NO:1187990-87-9
规格:98%
分子量:443.45
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议
100mg电议

产品介绍
MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.
CAS:1187990-87-9
分子式:C24H21N5O4
分子量:443.45
纯度:98%
存储:Store at -20°C

Background:

MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2.


MK-8617 is an orally active pan-inhibitor of hypoxia-inducible factor prolyl hydroxylase 1-3 (HIF PHD1-3) with an IC50 of 1 nM for PHD2. MK-8617 is not a significant inhibitor of the cytochrome p450 enzymes in vitro (IC50), CYP1A2, 3A4, 2B6, 2C9, 2C19, or 2D6, >60 uM, and is a moderate reversible inhibitor of CYP2C8 at 1.6 uM in vitro. The IC50 of MK-8617 is determined for factor inhibiting HIF (FIH) to be 18 uM[1].


Tritiated MK-8617 exhibits minimal metabolic turnover in liver microsomes from rat, dog, and monkey (<10% turover) but significant turnover in human liver microsomes (34% turnover) after 60 min (10 uM MK-8617, 1 mg/mL microsomal protein). In terms of its pharmacokinetic profile, MK-8617 shows good oral bioavailability across species (36 to 71%), with low clearance and volume of distribution. After 48 h treatment of MK-8617, postdose recovery of the radioactivity is about 26% bile, 12% urine, and 38% in feces, indicating that