Tolvaptan_product_DataBase

Bioactivity

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[1][2].

Invitro

Tolvaptan (0-100 μM; 24-168 h) decreases the growth of HepG2 cells[2].Tolvaptan (20-100 μM; 24-48 h) induces cell death in HepG2 cells[2].Tolvaptan (0-100 μM; 24-48 h) affects cell cycle of HepG2 cells[2].Tolvaptan (0-100 μM; 24-48 h) causes DNA damage and induces apoptosis of HepG2 cells[2]. Tolvaptan (0-100 μM; 24-48 h) decreases cyclins and CDKs, and increases γ-H2AX, PARP cleavage and LC3B-II in HepG2 cells[2].Tolvaptan (0-100 μM; 4-24 h) induces phosphorylation of JNK, ERK1/2 and p38 in HepG2 cells[2].Tolvaptan (0-100 μM; 24-28 h) induces autophagy of HepG2 cells[2]. Cell Viability Assay[2] Cell Line:

In Vivo

Tolvaptan (10 mg/kg; p.o. once per day for 22 days) improves cyclophosphamide (CP)-induced nephrotoxicity in rats[3]. Animal Model:

Name

Tolvaptan

CAS

150683-30-0

Formula

C26H25ClN2O3

Molar Mass

448.94

Appearance

Solid

Transport

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Reference

[1]. Wu Y, et al. Mechanisms of tolvaptan-induced toxicity in HepG2 cells. Biochem Pharmacol. 2015 Jun 15;95(4):324-36. [2]. El-Shabrawy M, et al. Protective effect of tolvaptan against cyclophosphamide-induced nephrotoxicity in rat models. Pharmacol Res Perspect. 2020 Oct;8(5):e00659.

PeptideDB

Tolvaptan

CAS: 150683-30-0 F: C26H25ClN2O3 W: 448.94