SB290157 is a selective antagonist of complement anaphylatoxin C3a receptor, a 74 amino acid proinflammatory peptide that is a potent chemotaxin for eosinophils, macrophages and mast cells, and has recently been found to be involved in nonimmunological roles in osteoblast differentiation, angiogenesis, and lipid metabolism. SB290157 is selective for C3aR over C5aR or other chemotactic GPCRs with an IC50 of 200 nM. It effectively blocks C3aR in humans, rat, guinea pig, and mouse. SB290157 was found to inhibit diet-induced obesity, metabolic dysfunction, and adipocyte signaling, in addition to inhibiting macrophage signaling.
| Molecular Weight | 526.51 |
| Formula | C22H28N4O4.CF3CO2H |
| CAS Number | 1140525-25-2 |
| Solubility (25°C) | DMSO 100 mg/mL Ethanol 90 mg/mL |
| Storage | -20°C, dry, sealed |
| 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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