AMG 579
AMG579是有效，选择性的磷酸二酯酶10A(PDE10A)抑制剂，IC50值为0.1nM。
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包装价格促销价数量
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250mg￥0.000.00- +
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500mg￥0.000.00- +
- 货号: ajcx12532
- CAS: 1227067-61-9
- 别名:
- 分子式: C25H23N5O3
- 分子量: 441.48
- 纯度: ＞98%
- 溶解度: DMSO: 41.67 mg/mL (94.39 mM)
- 储存: Store at -20°C
- 库存: 现货
Background
AMG 579 is a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A) with an IC50 of 0.1 nM.
AMG 579 shows statistically significant reduction of PCP induced behavior in rats over the 2 h period. Minimum effective doses for efficacy in PCP-LMA model is determined to be 0.3 mg/kg for AMG 579. In dog, 5 exhibits superior oral bioavailability of 72%[1].
[1]. Hu E,et al. Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A). J Med Chem. 2014 Aug 14;57(15):6632-41.
Protocol
Animal experiment: | Rats[1]Adult male Sprague?Dawley rats (250?280 g) are dosed at 0.1, 0.3, 1, and 3 mg/kg PO 1 h prior to administration of PCP. The magnitude of rat locomotor activity is quantified as number of beam breaks over a 2 h period[1]. |
参考文献: [1]. Hu E,et al. Discovery of clinical candidate 1-(4-(3-(4-(1H-benzo[d]imidazole-2-carbonyl)phenoxy)pyrazin-2-yl)piperidin-1-yl)ethanone (AMG 579), a potent, selective, and efficacious inhibitor of phosphodiesterase 10A (PDE10A). J Med Chem. 2014 Aug 14;57(15):6632-41. | |
