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同义名 : | - |
CAS号 : | 2055599-51-2 | |
货号 : | A1207405 | |
分子式 : | C25H23F2N3O5S | |
纯度 : | 99%+ | |
分子量 : | 515.53 | |
MDL号 : | MFCD32669796 | |
存储条件: |
Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月 |
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溶解度 : | - | |
动物实验配方: |
生物活性 | |||
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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]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.94mL 0.39mL 0.19mL |
9.70mL 1.94mL 0.97mL |
19.40mL 3.88mL 1.94mL |
参考文献 |
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