- 产品详情
- 产品参数
- 产品评论
产品属性：
产品名称 | 2,6-Dichloro-N-(2-(cyclopropanecarboxamido)pyridin-4-yl)benzamide |
规格 | 10mM*1 mL in DMSO、5 mg、10 mg、25 mg |
货号 | EY-01Y17049 |
Cas No.: 1258292-64-6
别名: N/A
化学名: N/A
分子式: C16H13Cl2N3O2
分子量: 350.2
溶解度: DMSO : 62.5 mg/mL (178.47 mM; Need ultrasonic)
储存条件: 4°C, protect from light
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述：
GDC-046 is a potent, selective, and orally bioavailable TYK2 inhibitor with Kis of 4.8, 0.7, 0.7, and 0.4 nM for TYK2, JAK1, JAK2, and JAK3, respectively[1].In cell-based assays, GDC-046 demonstrates reasonable potency in blocking the IL-12 pathway (IL-12 pSTAT4 EC50=380 nM) while displaying less activity in the EPO (JAK2) pathway (EPO pSTAT5 EC50=1700 nM) and IL-6 (JAK1) pathway (IL-6 pSTAT3 EC50=2000 nM)[1].In mice, GDC-046 exhibits relatively high clearance (65 mL/min/kg) when dosed intravenously (i.v. 1 mg/kg) and exhibits modest oral exposure (AUC=2.6 μM.h at p.o. 5 mg/kg)[1].[1]. Jun Liang, et al. Lead Optimization of a 4-aminopyridine Benzamide Scaffold to Identify Potent, Selective, and Orally Bioavailable TYK2 Inhibitors. J Med Chem. 2013 Jun 13;56(11):4521-36.
特别提醒公司产品仅供科研使用
