NTP42
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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.

Chemical Structure

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NTP42
CAS# 2055599-51-2
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 555765
Name: NTP42
CAS#: 2055599-51-2
Chemical Formula: C25H23F2N3O5S
Exact Mass: 515.13
Molecular Weight: 515.532
Elemental Analysis: C, 58.25; H, 4.50; F, 7.37; N, 8.15; O, 15.52; S, 6.22

Price and Availability

Size Price Availability Quantity
50mg USD 750 2 Weeks
100mg USD 1250 2 Weeks
200mg USD 1950 2 Weeks
500mg USD 2950 2 Weeks
1g USD 4250 2 Weeks
2g USD 6450 2 Weeks
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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

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.9001

More Info: 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

Product Data:
Product Data
Instruction:
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Biological target: NTP42 is a thromboxane A2 (TXA2) receptor antagonist with an IC50 of 3.278 nM.
In vitro activity: TBD
In vivo activity: In vivo activity In the MCT-PAH rat model, NTP42:KVA4 alleviated disease-induced changes in cardiopulmonary hemodynamics, pulmonary vascular remodeling, inflammation, and fibrosis, to a similar or greater extent than the PAH SOCs tested. In the PAB model, NTP42:KVA4 improved RV geometries and contractility, normalized RV stiffness, and significantly increased RV ejection fraction. In both models, NTP42:KVA4 promoted beneficial RV adaptation, decreasing cellular hypertrophy, and increasing vascularization. Notably, elevated expression of the TP target was observed both in RV tissue from these and related disease models, and in clinical RV specimens of PAH and DCM. Reference: Front Cardiovasc Med. 2022 Dec 14;9:1063967. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC9794752/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 31.3 60.62

Preparing Stock Solutions

The following data is based on the product molecular weight 515.53 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol: 1. Mulvaney EP, Renzo F, Adão R, Dupre E, Bialesova L, Salvatore V, Reid HM, Conceição G, Grynblat J, Llucià-Valldeperas A, Michel JB, Brás-Silva C, Laurent CE, Howard LS, Montani D, Humbert M, Vonk Noordegraaf A, Perros F, Mendes-Ferreira P, Kinsella BT. The thromboxane receptor antagonist NTP42 promotes beneficial adaptation and preserves cardiac function in experimental models of right heart overload. Front Cardiovasc Med. 2022 Dec 14;9:1063967. doi: 10.3389/fcvm.2022.1063967. PMID: 36588576; PMCID: PMC9794752. 2. Mulvaney EP, Reid HM, Bialesova L, Mendes-Ferreira P, Adão R, Brás-Silva C, Kinsella BT. Efficacy of the thromboxane receptor antagonist NTP42 alone, or in combination with sildenafil, in the sugen/hypoxia-induced model of pulmonary arterial hypertension. Eur J Pharmacol. 2020 Dec 15;889:173658. doi: 10.1016/j.ejphar.2020.173658. Epub 2020 Oct 27. PMID: 33121950.
In vitro protocol: TBD
In vivo protocol: 1. Mulvaney EP, Renzo F, Adão R, Dupre E, Bialesova L, Salvatore V, Reid HM, Conceição G, Grynblat J, Llucià-Valldeperas A, Michel JB, Brás-Silva C, Laurent CE, Howard LS, Montani D, Humbert M, Vonk Noordegraaf A, Perros F, Mendes-Ferreira P, Kinsella BT. The thromboxane receptor antagonist NTP42 promotes beneficial adaptation and preserves cardiac function in experimental models of right heart overload. Front Cardiovasc Med. 2022 Dec 14;9:1063967. doi: 10.3389/fcvm.2022.1063967. PMID: 36588576; PMCID: PMC9794752. 2. Mulvaney EP, Reid HM, Bialesova L, Mendes-Ferreira P, Adão R, Brás-Silva C, Kinsella BT. Efficacy of the thromboxane receptor antagonist NTP42 alone, or in combination with sildenafil, in the sugen/hypoxia-induced model of pulmonary arterial hypertension. Eur J Pharmacol. 2020 Dec 15;889:173658. doi: 10.1016/j.ejphar.2020.173658. Epub 2020 Oct 27. PMID: 33121950.

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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