| 货号 | 规格 | 价格 | 上海 | 北京 | 珠海 | 重庆 | 武汉 | 购买数量 |
|---|---|---|---|---|---|---|---|---|
S88447-5mg买3赠1 |
99.45% | ￥290.00 |
3 | - | - | - | - |
|
S88447-10mg买3赠1 |
99.45% | ￥500.00 |
4 | - | - | - | - |
|
S88447-25mg买3赠1 |
99.45% | ￥800.00 |
6 | - | - | - | - |
|
S88447-100mg |
≥98% | ￥2260.00 |
货期：2-3天 | - | - | - | - |
|
| 产品描述： | GSK2982772 is a potent, orally active and ATP competitive RIP1 kinase inhibitor with IC50 values of 16 nM and 20 nM for human and monkey RIP1, respectively | ||||||||||||||||||||
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| 靶点： | IC50: 16 nM (human RIP1 FP) IC50: 20 nM (monkey RIP1 FP) IC50: 2 μM (rat RIP1 FP) IC50: 2.5 μM (mouse RIP1 FP);RIPkinase | ||||||||||||||||||||
| 体外研究： | GSK2982772 shows more than 1,000-fold selectivity for ERK5 over a panel of over 339 kinases at 10 μM. In stimulated cellular systems,GSK2982772 is also able to reduce spontaneous production of cytokines (IL-1β and IL-6) in a concentration-dependent fashion from ulcerative colitis explant tissue in overnight incubations. GSK2982772 produces a weak concentration dependent inhibition of hERG in human embryonic kidney (HEK-293) cells, with an estimated IC50 of 195 μM, and also shows a weak activation of the human Pregnane X receptor (hPXR) with an EC50 of 13 μM. | ||||||||||||||||||||
| 体内研究： | GSK2982772 is dosed orally 15 min prior to TNF and shows 68, 80, and 87% protection from temperature loss over 6 h, at doses of 3, 10, and 50 mg/kg, respectively. In the corresponding TNF/zVAD model, GSK2982772 shows 13, 63, and 93% protection from temperature loss over 3 h. GSK2982772 displays a good free fraction in blood in rats (4.2%), dogs (11%), cynomolgus monkeys (11%), and humans (7.4%). The inhibitor has a good pharmacokinetic profile across both rats and monkeys. GSK2982772 distributes into a range of tissues including the colon, liver, kidney, and heart at concentrations comparable to those of blood. However, GSK2982772 has low brain penetration in rat (4%) despite possessing good cell permeability (21×10-6 cm/s). | ||||||||||||||||||||
| 参考文献： | 1. Harris PA, et al. Discovery of a First-in-Class Receptor Interacting Protein 1 (RIP1) Kinase Specific Clinical Candidate (GSK2982772) for the Treatment of Inflammatory Diseases. J Med Chem. 2017 Feb 23;60(4):1247-1261. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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