Valsartan (Diovan) is an angiotensin II receptor antagonist with IC50 of ranging from 39.5 to116 uM. By blocking the action of angiotensin, valsartan dilates blood vessels and reduces blood pressure. In the Value trial, the angiotensin II receptor blocker valsartan produced a statistically significant 19% (p=0.02) relative increase in the prespecified secondary end point of myocardial infarction (fatal and non-fatal) compared with amlodipine. The CHARM-alternative trial showed a significant +52% (p=0.025) increase in myocardial infarction with candesartan (versus placebo) despite a reduction in blood pressure.
|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.
|Solubility||DMSO 77 mg/mL|
|Related Angiotensin Receptor Products|
|C-Type Natriuretic Peptide (CNP) (1-22), human
C-Type Natriuretic Peptide (CNP) (1-22), human is the 1-22 fragment of C-Type Natriuretic Peptide.
AVE 0991 is an orally active agonist of angiotensin-(1-7) receptor with IC50 of 21 nM.
TRV-120027 (also known as TRV027) is an angiotensin II receptor type 1 (AT1R) antagonist and engages ß-arrestins while blocking G-protein signaling.
BIBS39 is a new nonpeptide angiotensin II (AII) receptor antagonist.
A-779 is a specific antagonist of G-protein coupled receptor (Mas receptor).
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