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MedKoo Cat#: 555765 | Name: NTP42
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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

NTP42
NTP42
CAS#2055599-51-2

Theoretical Analysis

MedKoo Cat#: 555765

Name: NTP42

CAS#: 2055599-51-2

Chemical Formula: C25H23F2N3O5S

Exact Mass: 515.1326

Molecular Weight: 515.53

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 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
200mg USD 1,950.00 2 Weeks
500mg USD 2,950.00 2 Weeks
1g USD 4,250.00 2 Weeks
2g USD 6,450.00 2 Weeks
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Related CAS #
No Data
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
View handling instruction
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/
Solvent mg/mL mM
Solubility
DMSO 31.3 60.62
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

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.
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

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