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MedKoo CAT#: 555765
CAS#: 2055599-51-2
Description: NTP42 is a novel antagonist of the thromboxane prostanoid receptor (TP), currently in development for the treatment of pulmonary arterial hypertension (PAH). PAH is a devastating disease with multiple pathophysiological hallmarks including excessive pulmonary vasoconstriction, vascular remodelling, inflammation, fibrosis, in situ thrombosis and right ventricular hypertrophy.
MedKoo Cat#: 555765
Name: NTP42
CAS#: 2055599-51-2
Chemical Formula: C25H23F2N3O5S
Exact Mass: 515.1326
Molecular Weight: 515.5318
Elemental Analysis: C, 58.25; H, 4.50; F, 7.37; N, 8.15; O, 15.52; S, 6.22
Synonym: NTP-42; NTP 42; NTP42;
IUPAC/Chemical Name: N-(tert-Butylcarbamoyl)-5-cyano-2-((4'-(difluoromethoxy)-(1,1'-biphenyl)-3-yl)oxy)benzenesulfonamide
InChi Key: RIIKDGPBTPECSW-UHFFFAOYSA-N
InChi Code: InChI=1S/C25H23F2N3O5S/c1-25(2,3)29-24(31)30-36(32,33)22-13-16(15-28)7-12-21(22)34-20-6-4-5-18(14-20)17-8-10-19(11-9-17)35-23(26)27/h4-14,23H,1-3H3,(H2,29,30,31)
SMILES Code: O=S(C1=CC(C#N)=CC=C1OC2=CC(C3=CC=C(OC(F)F)C=C3)=CC=C2)(NC(NC(C)(C)C)=O)=O
Signalling through the TP, thromboxane (TX) A2 is a potent vasoconstrictor and mediator of platelet aggregation. It is also a pro-mitogenic, pro-inflammatory and pro-fibrotic agent. Moreover, the TP also mediates the adverse actions of the isoprostane 8-iso-prostaglandin F2α, a free-radical-derived product of arachidonic acid produced in abundance during oxidative injury. Mechanistically, TP antagonists should treat most of the hallmarks of PAH, including inhibiting the excessive vasoconstriction and pulmonary artery remodelling, in situ thrombosis, inflammation and fibrosis.
From haemodynamic assessments, NTP42 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 or Selexipag 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
Mulvaney EP, Reid HM, Bialesova L, Bouchard A, Salvail D, Kinsella BT. NTP42, a novel antagonist of the thromboxane receptor, attenuates experimentally induced pulmonary arterial hypertension. BMC Pulm Med. 2020;20(1):85. Published 2020 Apr 6. doi:10.1186/s12890-020-1113-2
