Apelin-36(rat, mouse) TFA is an endogenous orphan G protein-coupled receptor APJ agonist. Apelin-36(rat, mouse) TFA blocks entry of some HIV-1 and HIV-2 strains into NP-2/CD4 cells expressing APJ. Apelin-36(rat, mouse) TFA binds to APJ receptors with an IC50 of 5.4 nM, and potently inhibits cAMP production with an EC50 of 0.52 nM.
| Molecular Weight | 4314.91 |
| Formula | C187H305N68F3O45S |
| CAS Number | 230299-95-3 (free base) |
| Solubility (25°C) | Water |
| Storage | -20°C, sealed |
| 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.
[2] M X Zou, et al. FEBS Lett. Apelin peptides block the entry of human immunodeficiency virus (HIV)
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