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| | RIPA-56 Basic information |
| Product Name: | RIPA-56 | | Synonyms: | RIPA-56;RIPA56; RIPA 56;Butanamide, N-hydroxy-2,2-dimethyl-N-(phenylmethyl)-;RIPA-56 >=98% (HPLC);N-Benzyl-N-hydroxy-2,2-dimethylbutanamide;RIPA-56,inhibit,Receptor-interacting protein kinases,RIP kinase,RIPK,Inhibitor,RIPA 56,RIPA56 | | CAS: | 1956370-21-0 | | MF: | C13H19NO2 | | MW: | 221.3 | | EINECS: | | | Product Categories: | | | Mol File: | 1956370-21-0.mol |  |
| | RIPA-56 Chemical Properties |
| Boiling point | 346.0±35.0 °C(Predicted) | | density | 1.070±0.06 g/cm3(Predicted) | | storage temp. | -20°C | | solubility | Soluble in DMSO (up to 50 mg/ml) or in Ethanol (up to 50 mg/ml) | | form | solid | | pka | 9.42±0.50(Predicted) | | color | White | | Stability: | Stable for 1 year from date of purchase as supplied. Solutions in DMSO or ethanol may be stored at -20°C for up to 3 months. |
| | RIPA-56 Usage And Synthesis |
| Description | RIPA-56 (1956370-21-0) is a potent (IC50?= 13 nM, EC50?= 28nM for HT-29 cells) and selective inhibitor of Receptor-Interacting Protein 1 (RIP1) kinase with significant metabolic stability (t1/2?= 128min human liver microsomal stability assay).? RIPA-56 showed excellent kinase selectivity and did not inhibit IDO at 200 μM.?It was able to block the progression of multiple sclerosis in an immune-induced demyelination model.2 | | 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. | | storage | Store at -20°C | | References | 1) Ren?et al.?(2017),?Discovery of a Highly Potent, Selective, and Metabolically Stable Inhibitor of Receptor-Interacting Protein 1 (RIP1) for the Treatment of Systemic Inflammatory Response Syndrome; J. Med. Chem.?60?972 |
| | RIPA-56 Preparation Products And Raw materials |
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