NTP42

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].

Research Areas >> Cardiovascular Disease

Signaling Pathways >> GPCR/G Protein >> Prostaglandin Receptor

TXA2

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] Dosage: 0.25 mg/kg BID Administration: 28-day drug treatment was initiated within 24 h post-MCT (60 mg/kg) Result: Reduced the MCT-induced PAH, including mPAP and RSVP.

[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.