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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phosphodiesterase (PDE)-MT-3014
MT-3014

Chemical Structure : MT-3014

CAS No.: 2296808-72-3

MT-3014 (MT3014)

货号: PC-26398Not For Human Use, Lab Use Only.

MT-3014 is a potent, highly selective PDE10A inhibitor with IC50 of 0.062 nM and 0.090 nM for human and bovine PDE10A, >1000-fold selective over other PDEs.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

MT-3014 is a potent, highly selective PDE10A inhibitor with IC50 of 0.062 nM and 0.090 nM for human and bovine PDE10A, >1000-fold selective over other PDEs.
Oral administration of MT-3014 (1.0-10 mg/kg) significantly increased the levels of cAMP, cGMP and cAMP response element-binding protein (CREB) phosphorylation in the rat striatum.
MT-3014 decreased MK-801 (0.075 mg/kg)-induced hyperactivity (ED50 = 0.30 mg/kg) in a dose-dependent manner.
MT-3014 (0.3-3.0 mg/kg and 0.2 mg/kg) attenuated MK-801-induced prepulse inhibition deficits and cognitive deficits in rats, respectively.
MT-3014 suppressed the conditioned avoidance response (ID50 = 0.32 mg/kg).

物理化学性质&存储条件

分子量 489.96
分子式 C23H26ClF2N7O
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

1-({2-(7-Fluoro-3-methylquinoxalin-2-yl)-5-[(3R)-3-fluoropyrrolidin-1-yl]pyrazolo[1,5-a]pyrimidin-7-yl}amino)-2-methylpropan-2-ol hydrochloride

参考文献

1. Koizumi Y, et al. Bioorg Med Chem. 2019 Aug 1;27(15):3440-3450.

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