产品
编 号：F177245
分子式：C26H25ClN2O3
分子量：448.94
分子式：C26H25ClN2O3
分子量：448.94
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
询价
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10mg
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50mg
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结构图
CAS No: 150683-30-0
产品详情
生物活性：
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.
体内研究：
Tolvaptan (10 mg/kg; p.o. once per day for 22 days) improves cyclophosphamide (CP)-induced nephrotoxicity in rats.Animal Model:Male albino rats with cyclophosphamide intraperitoneal injection
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg once per day; for 22 days
Result:Improved the level of urine volume, serum Na+, serum osmolarity, urinary creatinine, free water clearance, serum creatinine, urea, serum K+, blood pressure, urine osmolarity, fractional excretion of sodium and signs of nephrotoxicity in mice. Decreased caspase-3, Bax and pro-inflammatory cytokines, and increased antiapoptotic Bcl-2 in renal tissue of mice.
体外研究：
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.
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.
体内研究：
Tolvaptan (10 mg/kg; p.o. once per day for 22 days) improves cyclophosphamide (CP)-induced nephrotoxicity in rats.Animal Model:Male albino rats with cyclophosphamide intraperitoneal injection
Dosage:10 mg/kg
Administration:Oral gavage; 10 mg/kg once per day; for 22 days
Result:Improved the level of urine volume, serum Na+, serum osmolarity, urinary creatinine, free water clearance, serum creatinine, urea, serum K+, blood pressure, urine osmolarity, fractional excretion of sodium and signs of nephrotoxicity in mice. Decreased caspase-3, Bax and pro-inflammatory cytokines, and increased antiapoptotic Bcl-2 in renal tissue of mice.
体外研究：
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.
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