产品描述: NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM for antagonizing T prostanoid receptor (TP)- mediated [Ca2+] mobilization following stimulation of cells with the alternative TP agonist U46619. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH) |
靶点:
TXA2;ProstaglandinReceptor;PPAR |
体内研究:
NTP42 (0.25 mg/kg BID) is potent in a monocrotaline (MCT)-induced PAH rat model (28-day drug treatment is initiated within 24 h post-MCT) in haemodynamic assessments. NTP42 reduces the MCT-induced PAH, including mean pulmonary arterial pressure (mPAP) and right systolic ventricular pressure (RSVP). Moreover, NTP42 is superior to Sildenafil and Selexipag in significantly reducing pulmonary vascular remodelling, inflammatory mast cell infiltration and fibrosis in MCT-treated animals |
参考文献:
1. B. Therese KINSELLA, et al. Thromboxane receptor antagonists. WO2016203314A1. 2. Eamon Mulvaney, et al. NTP42, a novel antagonist of the thromboxane receptor, attenuates experimentally induced pulmonary arterial hypertension. |
溶解性:
Soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
1.94 ml |
9.699 ml |
19.398 ml |
5 mM |
0.388 ml |
1.94 ml |
3.88 ml |
10 mM |
0.194 ml |
0.97 ml |
1.94 ml |
50 mM |
0.039 ml |
0.194 ml |
0.388 ml |
|
注意: |
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