GlpBio

AMG 579

目录号: GC31213纯度: >99.50%
AMG579是有效，选择性的磷酸二酯酶10A(PDE10A)抑制剂，IC50值为0.1nM。
AMG 579
Cas No.: 1227067-61-9
规格价格库存数量操作
250mg询价现货
1
500mg询价现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
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    187(9):2288-2304 (2024)
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    183(7):1867-1883 (2020)
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产品描述 Description

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.

实验参考方法 Experimental Reference Method

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].

References:

[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.

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1227067-61-9
SMILES
CC(N1CCC(C2=NC=CN=C2OC3=CC=C(C(C4=NC5=CC=CC=C5N4)=O)C=C3)CC1)=O
分子式
C25H23N5O3
分子量
441.48 g/mol
溶解性
DMSO: 41.67 mg/mL (94.39 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol