V2 Receptor  Antagonist

Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V₂R) antagonist with an IC₅₀ of 1.28 μM for the inhibition of arginine vasopressin (AVP)-induced platelet aggregation. Tolvaptan induces cell apoposis and affects cell cycle. Tolvaptan can be used for the research of hyponatremia.

Conivaptan hydrochloride (YM 087) is an orally active dual vasopressin V_1a/V₂ receptor antagonist with K_i values of 0.48 nM and 3.04 nM for vasopressin V_1a receptor and V₂ receptor, respectively. Conivaptan hydrochloride competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan hydrochloride inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan hydrochloride induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan hydrochloride is used for research on hyponatremia and congestive heart failure.

Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V₂ receptor antagonist with an IC₅₀ of 14 nM. Mozavaptan shows ~85-fold selectivity for V₂ receptor over V₁ receptor (IC₅₀ of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.

Mozavaptan hydrochloride (OPC-31260 hydrochloride) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V₂ receptor antagonist with an IC₅₀ of 14 nM. Mozavaptan hydrochloride shows ~85-fold selectivity for V₂ receptor over V₁ receptor (IC₅₀ of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan hydrochloride has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.

Conivaptan-d₄ (YM 087-d₄) is the deuterated-labeled Conivaptan (HY-18347). Conivaptan (YM 087 free base) is an orally active dual vasopressin V_1a/V₂ receptor antagonist with K_i values of 0.48 nM and 3.04 nM for vasopressin V_1a receptor and V₂ receptor, respectively. Conivaptan competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan is used for research on hyponatremia and congestive heart failure.

Lixivaptan (VPA-985, WAY-VPA 985) is an orally active and selective vasopressin receptor V2 antagonist, with IC₅₀ values of 1.2 and 2.3 nM for human and rat V2, respectively.

Vasopressin V2 receptor antagonist 1 is a vasopressin V2 receptor (V₂R) antagonist with a K_i value of 3.8 nM. Vasopressin V2 receptor antagonist 1 inhibits renal cyst formation in embryonic renal cyst models and mouse models. Vasopressin V2 receptor antagonist 1 can be used in research related to autosomal dominant polycystic kidney disease.

V1a/V2 antagonist 1 (Compound 18j) is an orally active dual V1a and V2 receptor antagonist with high binding affinity for both receptors (K_i: 0.13 nM for hV1a, 0.53 nM for hV2 and 0.5 nM for mV1a; IC₅₀: 2.2 nM for hV1a). V1a/V2 antagonist 1 inhibits Oxytocin (HY-17571)-induced scratching behavior in mice.

XYDC2050 (Compound 29) is a selective vasopressin V2 receptor (V2R) antagonist with an IC₅₀ of 27 nM and a K_i of 2.8 nM. XYDC2050 shows a K_i of 420.7 nM (SI = 162 fold) for V1R. XYDC2050 can inhibit Vasopressin (HY-B1811)-induced intracellular cyclic adenosine monophosphate (cAMP) accumulation with an IC₅₀ of 12 nM. XYDC2050 can inhibit the growth of renal cysts, reduce the ratio of kidney weight to body weight and decrease the area of cysts and the cystic index. XYDC2050 can be used for the research of autosomal dominant polycystic kidney disease (ADPKD).

Mozavaptan-d6 (OPC-31260-d6) is the deuterium labeled Mozavaptan. Mozavaptan (OPC-31260) is a benzazepine derivative and a potent, selective, competitive and orally active vasopressin V₂ receptor antagonist with an IC₅₀ of 14 nM. Mozavaptan shows ~85-fold selectivity for V₂ receptor over V₁ receptor (IC₅₀ of 1.2 μM), and can antagonize the antidiuretic action of arginine vasopressin (AVP) in vivo. Mozavaptan has the potential for hyponatremia, syndrome of inappropriate antidiuretic hormone (SIADH), and congestive heart failure treatment.

Conivaptan (YM 087 free base) is an orally active dual vasopressin V_1a/V₂ receptor antagonist with K_i values of 0.48 nM and 3.04 nM for vasopressin V_1a receptor and V₂ receptor, respectively. Conivaptan competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan is used for research on hyponatremia and congestive heart failure.

L-364918 is a potent and selective oxytocin and arginine vasopressin antagonist with K_i values of 30, 1300, 2400 nM for OT, AVP-V1, AVP-V2, respectively. L-364918 has the potential for the research of preterm labor and disturbances in water balance.

YM218 free base is an orally active non-peptide vasopressin (AVP) receptor antagonist. YM218 free base has a high affinity for rat liver V1A receptors with a K_i value of 0.50 nM; it has a lower affinity for rat pituitary V1B, kidney V2, and uterine oxytocin receptors with K_i values of 1510 nM, 72.2 nM, and 150 nM, respectively. YM218 free base can be used in the study of diabetes and kidney disease.

Conivaptan hydrochloride (Standard) (YM 087 (Standard)) is the analytical standard of Conivaptan hydrochloride (HY-18347A). This product is intended for research and analytical applications. Conivaptan hydrochloride is an orally active dual vasopressin V_1a/V₂ receptor antagonist with K_i values of 0.48 nM and 3.04 nM for vasopressin V_1a receptor and V₂ receptor, respectively. Conivaptan hydrochloride competitively and reversibly blocks vasopressin-mediated antidiuresis, vasoconstriction, and cellular hypertrophy, while inhibiting CYP3A4. Conivaptan hydrochloride inhibits vasopressin-induced intracellular calcium, cAMP, and mitogen-activated kinase activation in vascular smooth muscle cells and cardiomyocytes. Conivaptan hydrochloride induces water diuresis while improving hemodynamics in heart failure models, reducing left ventricular end-diastolic pressure, vascular resistance, and organ weight. Conivaptan hydrochloride is used for research on hyponatremia and congestive heart failure.

Tolvaptan-d₇ is the deuterium labeled Tolvaptan. Tolvaptan is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC₅₀ of 1.28μM for the inhibition of AVP-induced platelet aggregation.