| Identification | Back Directory | [Name]
NTP-42 | [CAS]
2055599-51-2 | [Synonyms]
NTP-42
Benzenesulfonamide, 5-cyano-2-[[4'-(difluoromethoxy)[1,1'-biphenyl]-3-yl]oxy]-N-[[(1,1-dimethylethyl)amino]carbonyl]- | [Molecular Formula]
C25H23F2N3O5S | [MDL Number]
MFCD32669796 | [MOL File]
2055599-51-2.mol | [Molecular Weight]
515.53 |
| Chemical Properties | Back Directory | [density ]
1.39±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO: 31.25 mg/mL (60.62 mM) | [form ]
Solid | [pka]
4.56±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
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[1]. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH)[2]. | [in vivo]
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 (HY-15025) and Selexipag (HY-14870) 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. |
| [IC 50]
TXA2 | [References]
[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. |
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