Tolvaptan,150683-30-0

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YZ剂描述：

产品名称：Tolvaptan

产品别名：托伐普坦

英文别名：OPC-41061

靶点：Vasopressin Receptor

CAS：150683-30-0

纯度：>98%

外观：白色至类白色结晶性粉末

保存方法：store at -20℃ for one year（Powder）； in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months.

描述：

Tolvaptan (OPC-41061)?is a selective, competitive arginine vasopressin receptor 2 antagonist with an IC50 of 1.28uM for the inhibition of AVP-induced platelet aggregation. Tolvaptan (OPC-41061) is used to treat hyponatremia (low blood sodium levels) associated with congestive heart failure, cirrhosis, and the syndrome of inappropriate antidiuretic hormone (SIADH). Tolvaptan (OPC-41061) is also in fast-track clinical trials for polycystic kidney disease. Treatment with t tolvaptan (OPC-41061) causes rapid and sustained body weight reductions concurrent with increases in urine output, improves and/or normalizes serum sodium in hyponatremic patients, reduces signs and symptoms of congestion and increases thirst. However, tolvaptan (OPC-41061) has not been shown to decrease heart failure re-hospitalization or mortality. As an adjunct to standard therapy, tolvaptan (OPC-41061) is unique in that it is virtually the only novel agent tested in patients hospitalized for acute heart failure syndrome (AHFS) to reach its primary end point for short-term efficacy without causing deleterious side effects.

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

体外研究：

TolvaptanYZ[(3)H] AVP结合人类V(2)受体比 V(1a)高29倍，并没有表现出对V（1B）受体的YZ。Tolvaptan不仅YZ[(3)H〕AVP的结合也YZAVP诱导的HeLa细胞中环AMP的表达。Tolvaptan在健康和患病的动物中表现显著的夜尿症。 在常染色体显性多囊肾病（ADPKD）细胞中，Tolvaptan浓度依赖性YZ精氨酸加压素诱导的cAMP产生，IC50为0.1 nM。TolvaptanYZAVP诱导的ERK信号传导和细胞增殖。TolvaptanYZAVP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。

体内研究：在大鼠模型-急性和慢性低钠血症中，Tolvaptan改善低钠血症，导致预防死亡，并可以提高器官水份保留。Tolvaptan降低心脏前负荷，不会对肾功能，全身血流动力学，或在心脏衰竭（HF）狗中循环神经激素产生不利影响。在人类多囊肾病（PKD）动物模型中，Tolvaptan导致肾脏重量减轻以及囊肿纤维化和体积的减小。 在大鼠模型-急性和慢性低钠血症中，Tolvaptan明显升高无电解质水的间隙（E-CH(2)O）或aquaresis为正值，并增加尿精氨酸加压素（AVP）在心脏衰竭大鼠中的排泄。>

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