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Tolvaptan

(Synonyms: 托伐普坦; OPC-41061)

目录号: PL04689 纯度: ≥99%

Tolvaptan 是一种选择性，竞争性并且具有口服活性的 vasopressin receptor 2 (V2R) 拮抗剂，抑制 AVP 诱导的血小板聚集，其 IC50 值为 1.28 μM。Tolvaptan 可诱导细胞凋亡，影响细胞周期。Tolvaptan 可用于低钠血症的研究。

CAS No. :150683-30-0

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PL04689-1 mL x 10 mM (in DMSO)		¥647.00	请登录

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中文名称	Tolvaptan
中文别名	托伐普坦;N-[4-[(5R)-7-氯-5-羟基-2,3,4,5-四氢-1-苯并氮杂卓-1-甲酰基]-3-甲基苯基]-2-甲基苯甲酰胺;托伐普坦-D7;托伐普坦标准品;托伐普坦杂质;盐酸帕唑替尼;托伐普坦(标准品)
英文名称	Tolvaptan
英文别名	N-(4-(7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide;Tolvaptan;N-[4-[(5R)-7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl]-3-methylphenyl]-2-methylbenzamide;N-(4-(7-Chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-benzo[b]-azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide;N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-methylphenyl]-2-methylbenzamide;N-[4-(9-chloro-6-hydroxy-2-azabicyclo[5.4.0]undeca-8,10,12-triene-2-carbonyl)-3-methyl-phenyl]-2-methyl-benzamide;N-[4-[(7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl]-3-methylphenyl]-2-methylBenzamide;benzazepine derivative,32;OPC 41061;OPC-41061;Samsca;UNII-21G72T1950;Tolvptan;TOIVAPTAN;Tolvaptan-d7;Tolvaptan Tablets;pazopanib hydrochloeide;Best Price Tolvaptan from China CAS NO.150683-30-0;C26H25ClN2O3;Benzamide, N-(4-((7-chloro-2,3,4,5-tetrahydro-5-hydroxy-1H-1-benzazepin-1-yl)carbonyl)-3-methylphenyl)-2-methyl-;benzazepine derivative, 32;Tolvaptan [USAN:INN:BAN]
Cas No.	150683-30-0
分子式	C₂₆H₂₅ClN₂O₃
分子量	448.94
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Tolvaptan 是一种选择性，竞争性并且具有口服活性的 vasopressin receptor 2 (V2R) 拮抗剂，抑制 AVP 诱导的血小板聚集，其 IC50 值为 1.28 μM。Tolvaptan 可诱导细胞凋亡，影响细胞周期。Tolvaptan 可用于低钠血症的研究。

产品详情

Tolvaptan 是一种选择性，竞争性并且具有口服活性的 vasopressin receptor 2 (V₂R) 拮抗剂，抑制 AVP 诱导的血小板聚集，其 IC₅₀ 值为 1.28 μM。Tolvaptan 可诱导细胞凋亡，影响细胞周期。Tolvaptan 可用于低钠血症的研究。

生物活性

Tolvaptan is a selective, competitive and orally active vasopressin receptor 2 (V 2 R) antagonist with an IC 50 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.

性状

Solid

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Tolvaptan (10 mg/kg; p.o. once per day for 22 days) improves cyclophosphamide (CP)-induced nephrotoxicity in rats. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male albino rats wit

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (222.75 mM)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Tolvaptan

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