Tolvaptan
Tolvaptan (OPC-41061) is a highly potent selective, competitive vasopressin V2-receptor antagonist with Ki of 0.43 nM, >200-fold more selective than for V1A-receptors; inhibits cAMP production induced by AVP with no intrinsic agonist activity; clearly produces dose-dependent aquaresis in rats; orally active. (In Vitro) :Tolvaptan (0-100 μM; 24-168 h) decreases the growth of HepG2 cells.Tolvaptan (20-100 μM; 24-48 h) induces cell death in HepG2 cells.Tolvaptan (0-100 μM; 24-48 h) affects cell cycle of HepG2 cells.Tolvaptan (0-100 μM; 24-48 h) causes DNA damage and induces apoptosis of HepG2 cells.Tolvaptan (0-100 μM; 24-48 h) decreases cyclins and CDKs, and increases γ-H2AX, PARP cleavage and LC3B-II in HepG2 cells.Tolvaptan (0-100 μM; 4-24 h) induces phosphorylation of JNK, ERK1/2 and p38 in HepG2 cells.Tolvaptan (0-100 μM; 24-28 h) induces autophagy of HepG2 cells. (In Vivo) :Tolvaptan (10 mg/kg; p.o. once per day for 22 days) improves cyclophosphamide (CP) -induced nephrotoxicity in rats.
Product Specifications
CAS Number
150683-30-0
Product Name Alternative
OPC 41061 | OPC-41061
Field of Research
Pharmacology & Drug Discovery
Purity
>98% (HPLC)
Solubility
10 mM in DMSO
Smiles
O=C (NC1=CC=C (C (N2CCC[C@@H] (O) C3=CC (Cl) =CC=C32) =O) C (C) =C1) C4=CC=CC=C4C
Molecular Formula
C26H25ClN2O3
Molecular Weight
448.9413
Storage Conditions
Storage temperature: -20°C. Stability: ≥ 2 years
Notes
For research use only.
Other Product Names
Benzamide, N-[4-[ (7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl) carbonyl]-3-methylphenyl]-2-methyl-
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