NTP42 是一种血栓素 (TXA2) 受体拮抗剂，拮抗用前列腺素受体 (TP) 激动剂 U46609 刺激细胞后 TP 介导的 [Ca2+] 流通，IC50 为 3.278 nM。NTP42 可用于治疗肺动脉高压 (PAH)。
货号:ajcx15438
CAS:2055599-51-2
分子式:C25H23F2N3O5S
分子量：515.53
溶解度:DMSO: 31.25 mg/mL (60.62 mM)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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 U46609[1]. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH)[2].

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[2]. Animal Model: Male Wistar-Kyoto rats[2]

[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.