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> NTP42 [2055599-51-2]

NTP42 [2055599-51-2]

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Katalog-Nummer HY-129851-5mg

Size : 5mg

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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. NTP42 can be used for the treatment of pulmonary arterial hypertension (PAH).

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NTP42 Chemische Struktur

NTP42 Chemische Struktur

CAS. Nr. : 2055599-51-2

This product is a controlled substance and not for sale in your territory.

Based on 1 publication(s) in Google Scholar

Beschreibung

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].

IC50 & Target[1]

TXA2

 

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 and Selexipag in significantly reducing pulmonary vascular remodelling, inflammatory mast cell infiltration and fibrosis in MCT-treated animals[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Klinische Studie
Molekulargewicht

515.53

Formel

C25H23F2N3O5S
CAS. Nr.

2055599-51-2
Appearance

Solid

Color

White to off-white

SMILES

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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 31.25 mg/mL (60.62 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.9398 mL 9.6988 mL 19.3975 mL
5 mM 0.3880 mL 1.9398 mL 3.8795 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molaritätsrechner

  • Verdünnungsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (4.03 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Reinheit & Dokumentation
Verweise

  • [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.

  • [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.

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.9398 mL 9.6988 mL 19.3975 mL 48.4938 mL
5 mM 0.3880 mL 1.9398 mL 3.8795 mL 9.6988 mL
10 mM 0.1940 mL 0.9699 mL 1.9398 mL 4.8494 mL
15 mM 0.1293 mL 0.6466 mL 1.2932 mL 3.2329 mL
20 mM 0.0970 mL 0.4849 mL 0.9699 mL 2.4247 mL
25 mM 0.0776 mL 0.3880 mL 0.7759 mL 1.9398 mL
30 mM 0.0647 mL 0.3233 mL 0.6466 mL 1.6165 mL
40 mM 0.0485 mL 0.2425 mL 0.4849 mL 1.2123 mL
50 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9699 mL
60 mM 0.0323 mL 0.1616 mL 0.3233 mL 0.8082 mL
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NTP42 Related Classifications

Help & FAQs

Keywords:

NTP422055599-51-2NTP 42NTP-42Prostaglandin ReceptorthromboxaneTXA2pulmonaryarterialhypertensionPAHInhibitorinhibitorinhibit

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