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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 |
| Related Opioid Receptor Products |
|---|
| Dermorphin
Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Dermorphin can be used to suppress neuralgia. |
| SR17018
SR17018 is an mu-opioid-receptor (MOR) agonist, EC50 is 97 nM for binding with GTPγS. |
| Adrenorphin (Metorphamide)
Adrenorphin (Metorphamide) is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM. |
| CYT-1010
CYT-1010 is a mu-opioid receptor agonist with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively. |
| Dynorphin A (1-8)
Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. Dynorphin A (1-8) inhibited 3H-Bremazocine binding to the purified kappa receptor with IC50 of 303 nM. |
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