RG7713 (RO5028442) is a highly effective and selective brain-osmotic vasopressin 1A (V1a) receptor antagonist with Ki values of 1 nM (hV1a) and 39 nM (mV1a).
|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 ≥ 10 mg/mL|
|Related Vasopressin Receptor Products|
Desmopressin is a synthetic octapeptide that is an analogue of the human hormone arginine vasopressin and has antidiuretic and procoagulant effects.
D[LEU4,LYS8]-VP TFA is a selective agonist of vasopressin V1b receptors, with Ki values of 0.16 nM, 0.52 nM and 1.38 nM for rat, human and mouse V1b receptors, respectively. D[LEU4,LYS8]-VP TFA showed weak antidiuretic, vasopressor and oxytocin activity in vitro.
Terlipressin acetate is a vasopressin analogue and a highly selective vasopressin V1 receptor agonist that reduces visceral blood flow and portal vein pressure and controls acute varicose rupture bleeding. Terlipressin acetate has anti-inflammatory and antioxidant effects and can be used to study hepatorenal syndrome and norepinephrine-resistant septic shock.
Lixivaptan (VPA-985, WAY-VPA 985) is an orally active, selective vasopressin receptor V2 antagonist with IC50 values of 1.2 nM in humans and 2.3 nM in rats.
Felypressin (PLV-2) is a non-catecholamine vasoconstrictor and a vasopressin 1 (Vasopressin 1) agonist. Felypressin is widely used in dental surgery.
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