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RLX-33 is a potent and selective blood-brain barrier permeable relaxin family peptide 3 (RXFP3) antagonist that also blocks relaxin 3 (Relaxin 3) -induced ERK1/2 phosphorylation. The IC50 phosphorylated RXFP3, ERK1 and ERK2 were 2.36μM, 7.82μM and 13.86μM, respectively. RLX-33 can block the increase of food intake in rats induced by RXFP3 selective agonist R3/I5. RLX-33 can be used in the study of metabolic syndrome.
| Molecular Weight | 462.89 |
| Formula | C24H19ClN4O4 |
| CAS Number | 2784577-71-3 |
| Solubility (25°C) | DMSO ≥ 100 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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