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AMG 837 is a potent, orally bioavailable GPR40 agonist with EC50 of 14 nM.
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Source | Physiol Rep (2015). Figure 3. AMG-837 |
| Method | Hormone measurement | |
| Cell Lines | rat small intestine | |
| Concentrations | 10 μmol/L | |
| Incubation Time | - | |
| Results | Intergroup comparisons between LA, TAK-875, AMG 837, and DMSO stimulations showed that only the GLP-1 response induced by vascular AMG 837 was significantly different from the vehicle control |
| Molecular Weight | 438.44 |
| Formula | C26H21F3O3 |
| CAS Number | 865231-46-5 |
| Solubility (25°C) | DMSO |
| 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.
[3] Jonathan B Houze, et al. AMG 837: a potent, orally bioavailable GPR40 agonist
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