- GSK 2982772；GSK-2982772
GSK2982772 is an ATP competitive receptor-interacting protein-1 (RIP1) kinase inhibitor with the IC50 value of 1 nM. It has exquisite kinase specificity and excellent activity in blocking many TNF-dependent cellular responses.
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
DMSO ：75 mg/mL (198.73 mM)
GSK2982772 has excellent activity in both RIP1 cellular systems, preventing TNF induced necrotic cell death, and an ulcerative colitis explant assay blocking spontaneous cytokine release.
GSK2982772 exhibits approximately equivalent RIP1 FP potency against human and monkey RIP1 but was significantly less potent against nonprimate RIP1. 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, it has low brain penetration in rat (4%) despite possessing good cell permeability, which is likely due to active extrusion of GSK2982772 from the brain via the efflux drug transporter. It is predicted that GSK2982772 has high bioavailability, moderate to low clearance with a moderate volume, and a terminal half-life in the order of 12 h.
- 实验方法 实验条件
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