RIPA-56 is a highly potent, selective, and metabolically stable inhibitor of receptor-interacting protein 1 (RIP1) with an IC50 of 13 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 is potent in both human and murine cells, is much more stable in vivo, and is efficacious in animal model studies. In the SIRS mice disease model, RIPA-56 efficiently reduces tumor necrosis factor alpha (TNFα)-induced mortality and multi-organ damage.
| Molecular Weight | 221.30 |
| Formula | C13H19NO2 |
| CAS Number | 1956370-21-0 |
| Solubility (25°C) | DMSO ≥ 30 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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RIPK1-IN-12 is a potent RIPK1 inhibitor. |
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| DNL104
DNL104 is a RIPK1 inhibitor that can be used in Alzheimer's disease related studies. |
| mRNA-0184
mRNA-0184 is a relaxin mimetic and also a relaxin receptor-1 (RXFP1) agonist. |
| AZD-3427
AZD-3427 is an RXFP1 agonist that may be used in studies related to cardiovascular disease. |
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