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.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|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.
|CAS Number||230299-95-3 (free base)|
Molecular properties of apelin: tissue distribution and receptor binding
Y Kawamata, et al. Biochim Biophys Acta. 2001 Apr 23;1538(2-3):162-71. PMID: 11336787.
Apelin peptides block the entry of human immunodeficiency virus (HIV)
M X Zou, et al. FEBS Lett. 2000 May 4;473(1):15-8. PMID: 10802050.
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|HIV-1 TAT Peptide TFA
TAT TFA is a cell-penetrating peptide which derived from the transactivator of transcription (TAT) of human immunodeficiency virus (HIV-1).
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