SSR504734

Chemical Structure : SSR504734

CAS No.: 615571-23-8

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货号: PC-24091Not For Human Use, Lab Use Only.

SSR504734 is a potent, selective and reversible inhibitor of glycine transporter-1 (GlyT1) with 8, 15, and 38 nM for human, rat, and mouse GlyT1 respectively.

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5 mg	￥1180	In stock
10 mg	￥1880	In stock
25 mg	￥2980	In stock
50 mg		Get quote
100 mg		Get quote

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生物&药学活性

SSR504734 is a potent, selective and reversible inhibitor of glycine transporter-1 (GlyT1) with 8, 15, and 38 nM for human, rat, and mouse GlyT1 respectively.
SSR504734 has no effect (IC50>1 μM) on human GlyT2 and D-serine transporters, and on murine proline, glutamate, and GABA transporters.
SSR504734 blocks reversibly the ex vivo uptake of glycine (mouse cortical homogenates: ID50: 5 mg/kg i.p.), rapidly and for a long duration.
SSR504734 increases extracellular levels of glycine in the rat prefrontal cortex (PFC), potentiates NMDA-mediated excitatory postsynaptic currents (EPSCs) in rat hippocampal slices (MEC=0.5 uM) and intrastriatal glycine-induced rotations in mice (MED: 1 mg/kg i.p.).
SSR504734 prevented ketamine-induced metabolic activation in mice limbic areas and reversed MK-801-induced hyperactivity and increase in EEG spectral energy in mice and rats, respectively (MED: 10-30 mg/kg i.p.).
SSR504734 shows activity in schizophrenia, anxiety and depression models.

物理化学性质&存储条件

分子量	433.30
分子式	C20H21Cl2F3N2O
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-Chloro-N-((S)-phenyl((S)-piperidin-2-yl)methyl)-3-(trifluoromethyl)benzamide hydrochloride

参考文献

1. Depoortère R, et al. Neuropsychopharmacology. 2005 Nov;30(11):1963-85.

2. Leonetti M, et al. Neuroscience. 2006;137(2):555-64.

SSR504734

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SSR504734

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