RIPA-56是一种高效力、代谢稳定的选择性RIP1 (RIPK1)抑制剂。 应用： RIPA-56 是一种高效选择和代谢稳定的受体相互作用蛋白 1 (RIP1) 抑制剂，IC50 为 13 nM。RIPA-56 可用于研究全身炎症反应综合征。 Information RIPA-56 RIPA-56 is a highly-potent, selective, and metabolically stable RIP1 (RIPK1) inhibitor. Targets RIP1 (Cell-free) 13 nM In vitro RIPA-56 shows efficient inhibition of RIP1 kinase activity, with an IC50 of 13 nM. It showed no inhibition of RIP3 kinase activity at a 10 µM concentration. RIPA-56 does not inhibit IDO activity at a concentration of 200 µM, which represents an estimated 10,000-fold selectivity window based on the RIP1 ADP-Glo activity of 13 nM. In vivo RIPA-56 has an impressive PK profile in mice, with a 3.1 h half-life, 22% oral bioavailability (PO), and 100% bioavailability from intraperitoneal injection (IP). RIPA-56 has great ability in transporting across blood brain barrier. In the SIRS mice disease model, RIPA-56 efficiently reduced tumor necrosis factor alpha (TNFα)-induced mortality and multi-organ damage.
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RIPA-56
CAS number：1956370-21-0 molecular formula：C13H19NO2
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| Chinese alias | N-苄基-N-羟基-2,2-二甲基丁酰胺, RIPA56 | ||
| English alias | Butanamide,N-hydroxy-2,2-dimethyl-N-(phenylmethyl)- | ||
| CAS number | 1956370-21-0 | molecular formula | C13H19NO2 |
| molecular weight | 221.3 g/mol | Exact mass | - |
| PSA | 40.500 Ų | logp | 2.500 |
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