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 분자식: C₂₆H₂₅ClN₂O₃ 분자량: 448.94 EC 번호: 691-537-5 PubChem CID: 216237

등급 & 순도 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

개요

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%

사양

동의어

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

사양 및 순도

Moligand™, 10mM in DMSO

생화학 및 생리적 메커니즘

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

보관 조건

Store at -80°C

배송

Dry ice packs + Cold packs

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등급

Moligand™

작업 유형

ANTAGONIST

작동 메커니즘

Vasotocin V2 receptor antagonist

제품 특성

ALogP

4.8

이름과 식별자

이성체 SMILES

CC1=CC=CC=C1C(=O)NC2=CC(=C(C=C2)C(=O)N3CCCC(C4=C3C=CC(=C4)Cl)O)C

WGK 독일

3

PubChem CID

216237

분자량

448.94

관련 대상(인간)

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)

화학 및 물리적 특성

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

자주 묻는 질문

What is Moligand??

Moligand? is one of Aladdin Scientific's premium product lines, formulated for high-purity applications across multiple workflows. Compared to standard grades in the same workflow, Moligand? products typically offer tighter specifications, more rigorous QC, and stronger lot-to-lot consistency.

How should this product be stored?

Store at ?80 °C. Ultra-low temperature storage is required to maintain the specified shelf life.

How is this product shipped?

This product ships frozen with dry ice and cold packs. Unpack on arrival and transfer it to the storage condition stated above; handle dry ice with insulated gloves in a ventilated area.

What are the CAS number, molecular formula and molecular weight?

The CAS Number is 150683-30-0, the molecular formula is C26H25ClN2O3, and the molecular weight is 448.94 g/mol.

What documentation is provided?

Available product documentation, including Certificates of Analysis (COA), Safety Data Sheets (SDS), and specification sheets, is shown in the product document area. Document availability and access follow the current site policy.