Tolvaptan - Moligand™, 10mM in DMSO , Vasotocin V2 receptor antagonist, CAS No.150683-30-0, Vasotocin V2 receptor antagonist

CAS: 150683-30-0 Cat. No.: T408595 Molecular Weight: 448.94 EC Number: 691-537-5 PubChem CID: 216237

GRADE & PURITY Moligand™, 10mM in DMSO

Synonyms

OPC-41061 | N-​[4-​[(7-​chloro-​2,​3,​4,​5-​tetrahydro-​5-​hydroxy-​1H-​1-​benzazepin-​1-​yl)​carbonyl]​-​3-​methylphenyl]​-​2-​methyl-benzamide

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Overview

Information

Tolvaptan (OPC-41061) is an orally effective nonpeptide arginineVasotocin V2 receptorantagonist withIC50of 3 nM, used to treat hyponatremia.
In vitro

Tolvaptan blocks the binding of [(3)H]AVP to human V(2) receptors with 29-fold greater selectivity than that for V(1a) receptors, and showed no inhibition of V(1b) receptors. Tolvaptan inhibits not only the binding of [(3)H]AVP but also the AVP-induced production of cyclic AMP in human V(2)-receptor-expressing HeLa cells. Tolvaptan shows marked aquaresis in healthy and diseased animals. Tolvaptan causes a concentration-dependent inhibition of arginine Vasotocin-induced cAMP production with an apparent IC(50) of 0.1 nM in autosomal dominant polycystic kidney disease (ADPKD) cells. Tolvaptan inhibits AVP-induced ERK signaling and cell proliferation. Tolvaptan inhibits AVP-induced Cl(-) secretion and decreases in vitro cyst growth of ADPKD cells cultured within a three-dimensional collagen matrix.

In vivo

Tolvaptan improves hyponatremia, resulting in the prevention of death, and improves organ water retention in rat models with acute and chronic hyponatremia. Tolvaptan reduces cardiac preload without unfavorable effects on renal functions, systemic hemodynamics, or circulating neurohormones in dogs with heart failure (HF). Tolvaptan shows a decrease in kidney weight as well as in cyst and fibrosis volume in animal models of human polycystic kidney disease (PKD). Tolvaptan markedly elevates electrolyte-free water clearance (E-CH(2)O) or aquaresis to a positive value and increases urinary Arginine Vasotocin (AVP) excretion in rats with heart failure.
Cell Data

cell lines：

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Synonyms

OPC-41061 | N-​[4-​[(7-​chloro-​2, ​3, ​4, ​5-​tetrahydro-​5-​hydroxy-​1H-​1-​benzazepin-​1-​yl)​carbonyl]​-​3-​methylphenyl]​-​2-​methyl-benzamide

Specifications & Purity

Moligand™, 10mM in DMSO

Biochemical and Physiological Mechanisms

Tolvaptan (OPC-41061) is an orally effective nonpeptide arginine Vasotocin V2 receptor antagonist with IC50 of 3 nM, used to treat hyponatremia.

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

ANTAGONIST

Mechanism of action

Vasotocin V2 receptor antagonist

Product Properties

• ALogP: 4.8

Names and Identifiers

• Isomeric SMILES: CC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)O)C
• WGK Germany: 3
• PubChem CID: 216237
• Molecular Weight: 448.94

Associated Targets(Human)

AVPR1A Tclin Vasopressin V1a receptor (2 Activities)

Discover Target: AVPR1A

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

AVPR2 Tclin Vasopressin V2 receptor (4 Activities)

Discover Target: AVPR2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 16 mg/mL (46.32 mM); Water: Insoluble; Ethanol: Insoluble
• Melt Point(°C): 225-230°C