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 resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 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 resveratrol of 11.2 mg/kg.
|Solubility||DMSO 80 mg/mL|
|Related Angiotensin Receptor Products|
A-779 is a specific antagonist of G-protein coupled receptor (Mas receptor).
Angiotensin (1-7) is a synthetic heptapeptide identical to endogenous angiotensin-(1-7), inhibits purified canine angiotensin converting enzyme (ACE) activity with an IC50 of 0.65 μM.
Losartan is an angiotensin II receptor antagonist, competing with the binding of angiotensin II to AT1 receptors with IC50 of 20 nM.
EMA401 (also known as Olodanrigan and PD-126055) is a highly selective angiotensin AT2 antagonist.
|Angiotensin II human
Angiotensin II human is converted by Angiotensin I through removal of two C-terminal residues by the enzyme angiotensin-converting enzyme (ACE). Angiotensin II is mediated by AT1 and AT2 receptors, which are seven transmembrane glycoproteins with 30% sequence similarity.
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