Bms-986122 is a selective and effective positive allosteric regulator of μ -opioid receptor (µ-OR). Bms-986122 showed enhancement of β -inhibitory protein recruitment, adenylate cyclase inhibition and G-protein activation mediated by normal agonists. Bms-986122 enhances damGO-mediated [35S]GTPγS binding in mouse meninges.
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.
Molecular Weight | 448.78 |
Formula | C16H15BrClNO3S2 |
CAS Number | 313669-88-4 |
Purity | >98% |
Solubility | DMSO ≥ 60 mg/mL |
Storage | 2-8°C |
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