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SSR504734 是一种具有口服活性、选择性和可逆性的 GlyT1抑制剂 (hGlyT1,rGlyT1,mGlyT1IC50分别为 18、15 和 38 nM)。SSR504734 在精神分裂症、焦虑症和抑郁症模型中表现出活性。
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SSR504734 是一种具有口服活性、选择性和可逆性的 GlyT1抑制剂 (hGlyT1,rGlyT1,mGlyT1IC50分别为 18、15 和 38 nM)。SSR504734 在精神分裂症、焦虑症和抑郁症模型中表现出活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 619 | 现货 | |
5 mg | ¥ 1,230 | 现货 | |
10 mg | ¥ 1,880 | 现货 | |
25 mg | ¥ 3,360 | 现货 | |
50 mg | ¥ 4,930 | 现货 | |
100 mg | ¥ 7,270 | 现货 |
产品描述 | SSR504734 is an orally active, selective and reversible inhibitor of human, rat, and mouse GlyT1 ( IC 50 =18, 15, and 38 nM, respectively). SSR504734 exhibits activity in schizophrenia, anxiety and depression models [1]. |
体外活性 | SSR504734 (15 nM-86 μM; 10 min) inhibits the ex vivo uptake of glycine in human SK-N-MC and rat C6 cells [1]. Cell Viability Assay [1] Cell Line: Human neuroblastoma (SK-N-MC) and rat astrocytoma (C6) cells Concentration: 15 nM-86 μM Incubation Time: 10 min Result: Showed IC 50 values of 18 and 15 nM for human SK-N-MC and rat C6 cells, respectively. |
体内活性 | SSR504734 (i.p. and p.o.; 1-100 mg/kg; once) treatment demonstrates good oral bioavailability [1]. SSR504734 (i.p.; 30 mg/kg; once) induces a rapid and significant decrease of specific glycine uptake [1]. SSR504734 (i.p.; 10 mg/kg; once) increases extracellular levels of Glycine in the prefrontal cortex (PFC) of freely moving rats [1]. Animal Model: Male Sprague-Dawley rats [1] Dosage: 1-100 mg/kg Administration: Intraperitoneal injection and oral gavage.; 1-100 mg/kg; once Result: Showed ID 50 values of 5.0 and 4.6 mg/kg for i.p. and p.o. treatments, respectively. Animal Model: Male Sprague-Dawley rats [1] Dosage: 30 mg/kg Administration: Intraperitoneal injection; 30 mg/kg; once Result: Maintained at about 80% inhibition from 1 to 7 h after administration. Animal Model: Male Sprague-Dawley rats [1] Dosage: 10 mg/kg Administration: Intraperitoneal injection; 10 mg/kg; once Result: Produced a rapid and sustained increase in PFC extracellular levels of glycine. |
分子量 | 433.30 |
分子式 | C20H21Cl2F3N2O |
CAS No. | 615571-23-8 |
Smiles | Cl.[H][C@]1(CCCCN1)[C@@H](NC(=O)c1cccc(c1Cl)C(F)(F)F)c1ccccc1 |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
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