CAS NO: | 1622848-92-3 |
包装 | 价格(元) |
10 mM * 1 mL in DMSO | 电议 |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
100mg | 电议 |
生物活性 | GSK2982772 is a potent, orally active and ATP competitiveRIP1kinase inhibitor withIC50values of 16 nM and 20 nM for human and monkey RIP1, respectively[1]. | ||||||||||||||||
IC50& Target | 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)[1] | ||||||||||||||||
体外研究 (In Vitro) | 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 IC50of 195 μM, and also shows a weak activation of the human Pregnane X receptor (hPXR) with an EC50of 13 μM[1]. | ||||||||||||||||
体内研究 (In Vivo) | 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 (21×10-6cm/s)[1]. | ||||||||||||||||
Clinical Trial | |||||||||||||||||
分子量 | 377.40 | ||||||||||||||||
性状 | Solid | ||||||||||||||||
Formula | C20H19N5O3 | ||||||||||||||||
CAS 号 | 1622848-92-3 | ||||||||||||||||
运输条件 | Room temperature in continental US; may vary elsewhere. | ||||||||||||||||
储存方式 |
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溶解性数据 | In Vitro: DMSO : 250 mg/mL(662.43 mM;Need ultrasonic) H2O :< 0.1 mg/mL (ultrasonic;warming;heat to 60℃)(insoluble) 配制储备液
* 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。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用;
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