MK-5046, a potent, selective small molecule agonist of BRS-3 (bombesin receptor subtype-3). In pharmacological testing using diet-induced obese mice, MK-5046 caused mechanism-based, dose-dependent reductions in food intake and body weight. MK-5046 was a full agonist for activation of MAPK, FAK, Akt, and paxillin.
| Molecular Weight | 444.37 |
| Formula | C20H18F6N4O |
| CAS Number | 1022152-70-0 |
| Solubility (25°C) | DMSO 10 mM |
| 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.
| Related Bombesin Receptor Products |
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| (D-Phe6, Leu-NHEt13, des-Met14)-Bombesin (6-14)
(D-Phe6,Leu-NHEt13,des-Met14)-Bombesin (6-14) is a bombesin (BBN) antagonist and can be used for the research of cancer. |
| BIM 23042
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| BIM-26226
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