RS 504393 is a extremely selective CCR2 chemokine receptor antagonist (IC50 values are 98 nM and > 100 μM for inhibition of human recombinant CCR2b and CCR1 receptors respectively). RS 504393 inhibits MCP-1 chemotaxis (IC50 = 330 nM) and ischemia-reperfusion injury in kidneys.
Int Immunopharmacol. 2021 Oct;99:107947.
The roles of MCP-1/CCR2 mediated macrophage recruitment and polarization in bladder outlet obstruction (BOO) induced bladder remodeling
RS 504393 purchased from AbMole
| Molecular Weight | 417.5 |
| Formula | C25H27N3O3 |
| CAS Number | 300816-15-3 |
| Solubility (25°C) | DMSO ≥ 5 mg/mL (May need ultrasonic) |
| 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.
[4] Kiyoki Kitagawa, et al. Am J Pathol. Blockade of CCR2 ameliorates progressive fibrosis in kidney
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