|N-(叔丁基氨基甲酰基)-5-氰基-2-((4'-(二氟甲氧基)-[1,1'-联苯]-3-基)氧基)苯磺酰胺|CsnPharm

CAS No.: 2055599-51-2

NTP42 is a TxA2 Synthetase antagonist with IC50 value of 3.278nM.

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400-920-2911

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生物活性

描述Thromboxane A₂ (TXA₂), a potent mediator of platelet aggregation and inducing constriction of various types of smooth muscle (SM) including vascular, renal and pulmonary SM, mediates its actions in humans by binding to the TPα and TPβ isoforms of the thromboxane prostanoid receptor (TP). NTP42 is a novel antagonist of the TP, currently in development for the treatment of pulmonary arterial hypertension (PAH) by antagonizing the action of TXA₂. In an MCT-induced PAH rat model, NTP42 (0.25 mg/kg BID, p.o.) reduced the MCT-induced PAH, including mean pulmonary arterial pressure (mPAP) and right systolic ventricular pressure (RSVP), being at least comparable to the standard-of-care drugs Sildenafil (50 mg/kg BID, p.o.) or Selexipag (1 mg/kg BID, p.o.) in bringing about these effects. Moreover, NTP42 was superior to Sildenafil and Selexipag in significantly reducing pulmonary vascular remodelling, inflammatory mast cell infiltration and fibrosis in MCT-treated animals^[1].
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实验方案

技术信息

CAS号

2055599-51-2

储存条件

分子式

C25H23F2N3O5S

运输

蓝冰

分子量

515.53

别名

溶解度

DMSO	30.0 mg/mL (58.2 mM) warming

动物实验配方

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