| Identification | Back Directory | [Name]
Carbamic acid, N-[5-[2-[(cyclopropylcarbonyl)amino]-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, tetrahydro-2H-pyran-4-yl ester | [CAS]
2173557-02-1 | [Synonyms]
RIPK1-IN-11
Carbamic acid, N-[5-[2-[(cyclopropylcarbonyl)amino]-6-benzothiazolyl]-2-methyl-3-pyridinyl]-, tetrahydro-2H-pyran-4-yl ester | [Molecular Formula]
C23H24N4O4S | [MOL File]
2173557-02-1.mol | [Molecular Weight]
452.53 |
| Hazard Information | Back Directory | [Uses]
RIPK1-IN-11 is a potent and orally active RIPK1 inhibitor (Kd=9.2 nM; IC50=67 nM). RIPK1-IN-11 inhibits necroptosis in both human and mouse cells (EC50=17-30 nM). Anti-inflammatory activity[1]. | [in vivo]
RIPK1-IN-11 (3 mg/kg; i.p. for 30 min, followed by injection with TNFα) blocks hypothermia and death in mice in the TNFα-induced SIRS model[1].
RIPK1-IN-11 (5 mg/kg, 25 mg/kg; p.o.; 7 days; C57BL/6 mouse) exhibits no obvious toxicity in mice[1]. | Animal Model: | C57BL/6 female mice (TNF-induced systemic inflammatory response syndrome)[1] | | Dosage: | 3 mg/kg | | Administration: | i.p. for 30 min, followed by injection with TNFα (0.25 μg/g) | | Result: | Significantly reduced TNFα-induced temperature loss and ameliorated lethal shock in mice.
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| [IC 50]
RIPK1 | [References]
[1] Li Z, Hao Y, Yang C, et al. Design, synthesis, and evaluation of potent RIPK1 inhibitors with in vivo anti-inflammatory activity. Eur J Med Chem. 2022;228:114036. DOI:10.1016/j.ejmech.2021.114036 |
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