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首页-小分子抑制剂&激动剂-GPCR-Orexin Receptor-MK-3697
MK-3697

Chemical Structure : MK-3697

CAS No.: 1224846-01-8

MK-3697 (MK 3697, MK3697)

货号: PC-42964Not For Human Use, Lab Use Only.

MK-3697 is a potent, selective, orally bioavailable Orexin 2 receptor (OX2R) antagonist with Ki of 1.1 nM and IC50 of 16 nM, shows exquisite selectivity over OX1R (Ki=18 uM).

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

MK-3697 is a potent, selective, orally bioavailable Orexin 2 receptor (OX2R) antagonist with Ki of 1.1 nM and IC50 of 16 nM, shows exquisite selectivity over OX1R (Ki=18 uM).
MK-3697 is orally efficacious in sleep experiments across species with high OX2R occupancy and low OX1R blockade.
MK-3697 demonstrated excellent sleep efficacy across species, and shows potential for the treatment of insomnia.

物理化学性质&存储条件

分子量 447.5096
分子式 C23H21N5O3S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 22.5 mg/mL

Chemical Name/SMILES

[2,3'-Bipyridine]-4-carboxamide, N-[(5,6-dimethoxy-2-pyridinyl)methyl]-5'-methyl-5-(2-thiazolyl)-

参考文献

1. Roecker AJ, et al. Bioorg Med Chem Lett. 2014 Oct 15;24(20):4884-90.

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