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首页-小分子抑制剂&激动剂-GPCR-mGluR-MK-8768
MK-8768

Chemical Structure : MK-8768

CAS No.: 1432729-22-0

MK-8768 (MK8768)

货号: PC-21049Not For Human Use, Lab Use Only.

MK-8768 (MK8768) is a potent, selective mGluR2 negative allosteric modulator (NAM) with IC50 of 9.6 nM, shows no activity against mGluR 1,3,4,5,6,8.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MK-8768 (MK8768) is a potent, selective mGluR2 negative allosteric modulator (NAM) with IC50 of 9.6 nM, shows no activity against mGluR 1,3,4,5,6,8.
MK-8768 demonstrates an excellent overall selectivity profile with weak to no activity on the hERG, IKs, and Nav1.5 ion channels and no confirmed activities < 10 μM in a Panlabs screen of >120 off-targets.
MK-8768 exhibits good oral pharmacokinetics and demonstrated efficacy in a rhesus monkey model of executive function and attention.

物理化学性质&存储条件

分子量 433.44
分子式 C21H22F3N5O2
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

10 mM in DMSO

Chemical Name/SMILES

O=C(C1=NC2=CC(CN3C[C@@H](C)O[C@@H](C(F)(F)F)C3)=CC=C2C(C4=CN(C)N=C4)=C1)N

参考文献

1. Michael T Rudd, et al. ACS Med Chem Lett. 2023 Jul 12;14(8):1088-1094.

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