产品信息
抗原名称
RIP kinase
商品描述
RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interactingprotein 1 (RIP1) with an IC50 of 13 nM.
分子量
221.3
纯度
98%
可溶性
DMSO : ≥ 100 mg/mL (451.88 mM)
外观
White solid
In vitro(体外研究)
RIPA-56 has a half-life of 128 min in human liver microsomal stability assays and an EC50 of 28 nM in TSZ-induced HT-29 necrosis assay. RIPA-56 also demonstrates potency in protection of murine L929 cells from TZ-induced necrosis (EC50=27 nM). RIPA-56 shows efficient inhibition of RIP1 kinase activity, with an IC50 of 13 nM and no inhibition of RIP3 kinase activity at a 10 μM concentration. RIPA-56 could form tight hydrophobic interactions with RIP1 through both the phenyl group and the 2,2-dimethylbutyl group, and form two important hydrogen bonds.
In vivo(体内研究)
In the SIRS mice disease model, RIPA-56 efficiently reduces tumor necrosis factor alpha (TNFα)-induced mortality and multi-organ damage. Compared to known RIP1 inhibitors, RIPA-56 is potent in both human and murine cells, is much more stable in vivo, and is efficacious in animal model studies. RIPA-56 has an impressive PK profile in mice with a 3.1 h half-life, 22% oral bioavailability (P.O.), and 100% bioavailability from intraperitoneal injection (I.P.).
背景
分子式
C13H19NO2
CAS号
1956370-21-0
制备和贮存
保存方式
Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution.
参考图片
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