GSK481 is a highly effective, selective and specific RIPK1 inhibitor with an IC50 value of 1.3 nM, which can inhibit the phosphorylation of Ser166 in wild-type human RIPK1 (IC50 value of 2.8 nM). The IC50 value of GSK481 against U937 cells was 10 nM.
Molecular Weight | 377.39 |
Formula | C21H19N3O4 |
CAS Number | 1622849-58-4 |
Solubility (25°C) | DMSO 70 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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