托伐普坦 T2326

Product Introduction
Bioactivity


英文名: Tolvaptan

描述: Tolvaptan (OPC-41061) 是一种可口服的选择性精氨酸加压素受体 2 拮抗剂，可用于治疗低钠血症。

激酶实验: Cell-free autophosphorylation assay using time-resolved fluorometry: Neratinib is prepared as 10 mg/mL stocks in DMSO and diluted in 25 mM HEPES (pH 7.5; 0.002 ng/mL-20 μg/mL). Purified recombinant COOH-terminal fragments of HER2 (amino acids 676-1255) or epidermal growth factor receptor (EGFR) (amino acids 645-1186) [diluted in 100 mM HEPES (pH 7.5) and 50% glycerol] is incubated with increasing concentrations of Neratinib in 4 mM HEPES (pH 7.5), 0.4 mM MnCl2, 20 μM sodium vanadate, and 0.2 mM DTT for 15 minutes at room temperature in 96-well ELISA plates. The kinase reaction is initiated by the addition of 40 μM ATP and 20 mM MgCl2 and allowed to proceed for 1 hour at room temperature. Plates are washed, and phosphorylation is detected using Europium-labeled anti-phospho-tyrosine antibodies (15 ng/well). After washing and enhancement steps, signal is detected using a Victor2 fluorescence reader (excitation wavelength 340 nm, emission wavelength 615 nm). The concentration of Neratinib that inhibits receptor phosphorylation by 50% (IC50) is calculated from inhibition curves.

体外活性: Tolvaptan降低心脏衰竭犬体内心脏前负荷,而对肾功能,全身血流动力学或循环神经激素没有不利影响.Tolvaptan在人类多囊肾病动物模型中,导致肾脏重量减轻以及囊肿纤维化和体积的减小.Tolvaptan在大鼠模型-急性和慢性低钠血症中,改善低钠血症,起到预防死亡作用.在心力衰竭大鼠中,Tolvaptan明显升高无电解质水清除（E-CH(2)O）,并增加尿精氨酸加压素的排泄.

体内活性: Tolvaptan在常染色体显性多囊肾病的细胞中,浓度依赖性抑制精氨酸加压素诱导的cAMP产生,IC50为0.1 nM。Tolvaptan抑制AVP诱导的ERK信号传导和细胞增殖。Tolvaptan抑制AVP引起的氯（-）的分泌,并降低在三维胶原基质内培养ADPKD细胞体外生长囊肿。Tolvaptan抑制[（3）H] AVP与人类V（2）受体的结合,其选择性比V（1a）受体高29倍,并且对V（1b）受体没有抑制作用。AVP诱导的HeLa细胞中,Tolvaptan不仅抑制[(3)H〕AVP的结合也抑制环AMP的表达。

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: Ethanol : 4.5 mg/mL (10 mM)
DMSO : 44.9 mg/mL (100 mM)


关键字: antidiuretic hormone | Inhibitor | cell cycle | OPC 41061 | inhibit | hyponatremia | Vasopressin Receptor | Tolvaptan | SIADH | OPC41061 | apoposis | Autophagy

相关产品: (D-Arg8)-Inotocin | Fuscoside | OPC-51803 | RG7713 | Vasopressin Dimer (parallel) (TFA) | Atosiban | Desmopressin | L-371,257 | (d(CH2)51,Tyr(Me)2,Dab5,Arg8)-Vasopressin | Fedovapagon

相关库: Approved Drug Library | ReFRAME Related Library | Anti-Cancer Drug Library | Inhibitor Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Anti-Obesity Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | NO PAINS Compound Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途