RIPA-56

RIPA-56

Biochem/physiol Actions

RIPA-56 is a metabolically stable type III kinase inhibitor that targets receptor-interacting protein 1 kinase (RIP1; RIPK1) in a highly potent and selective manner (RIP1 IC50 = 13 nM) by locking RIP1 in its inactive form, exhibiting no inhibitory potency toward RIP3, IDO or a panel of multiple kinases (tested at 10, 200, and 5 µM, respectively). RIPA-56 protects against TNFα-induced necroptosis (necrosis) upon apoptosis/NF-κB pathway blockage (EC50?= 27 nM/murine L929 and 28 nM/human HT-29 cells) in cultures as well as TNFα-induced mortality and multiorgan damage in a murine model of systemic inflammatory response syndrome (SIRS) in vivo (100% survival rate with 3 mg/kg/12 h or single 6 mg/kg i.p.) with good pharmacokinetics and bioavailability (F post 10 mg/kg p.o. or i.p. dosing = 22% and 100%, respectively, of 2 mg/kg i.v.). Long-term daily RIPA-56 supplementation (150 or 300 mg/kg in chow) is reported to prevent aging-associated deterioration of the male reproductive system in mice.

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Code Description Colour Manufacturer Storage Temp. Solubility Form Assay Price Quantity
3575820 RIPA-56 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£214.50 (exc VAT) per 25MG
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3575821 RIPA-56 white to beige SIGMA-ALDRICH 2-8°C DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£75.08 (exc VAT) per 5MG
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