MK-8189 | PDE10A inhibitor | Probechem Biochemicals

Chemical Structure : MK-8189

CAS No.: 1424371-93-6

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MK-8189 (MK8189)

货号: PC-49494Not For Human Use, Lab Use Only.

MK-8189 (MK8189) is a highly potent, selective PDE10A inhibitor with Ki of 29 pM, 500,000-fold selectivity over the other PDE enzyme families (PDE1-PDE11).

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5 mg	￥2780	In stock
10 mg	￥4580	In stock
25 mg	￥7580	In stock
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生物&药学活性

MK-8189 (MK8189) is a highly potent, selective PDE10A inhibitor with Ki of 29 pM, 500,000-fold selectivity over the other PDE enzyme families (PDE1-PDE11).
MK-8189 shows an IC50 of 1.6 nM in cells recombinantly expressing full-length human PDE10A.
MK-8189 has an excellent profile against ion channels (Iks, Cav1.2, and Nav1.5 >30 μM, and functional hERG Ikr IC50=33 μM). One off-target activity was identified in a broad Panlabs panel (somatostatin receptor type 2 (SSTR2) IC50=2.8 μM in a radioligand binding assay).
MK-8189 (0.25 mg/kg, oral) attenuates MK-801-induced locomotor activity in rats.

物理化学性质&存储条件

分子量	382.49
分子式	C19H22N6OS
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	2-Methyl-N-((5-methyl-1,3,4-thiadiazol-2-yl)methyl)-6-(((1S,2S)-2-(5-methylpyridin-2-yl)cyclopropyl)methoxy)pyrimidin-4-amine

参考文献

1. Layton ME, et al. J Med Chem. 2023 Jan 9. doi: 10.1021/acs.jmedchem.2c01521.

MK-8189 (MK8189)

生物&药学活性

物理化学性质&存储条件

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MK-8189 (MK8189)

生物&药学活性

物理化学性质&存储条件

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