Selexipag
Based on 3 publication(s) in Google Scholar
Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).
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- Pureté: 99.86%
- CAS No.: 475086-01-2
- Formule: C26H32N4O4S
- Masse moléculaire:496.62
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Activité biologique
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Chemical Information
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Solvant et solubilité
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Publications Citing Use of MedChemExpress (MCE) Selexipag
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IHC
Activité biologique
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hIP 260 nM (Ki) |
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Cell Line
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Type | Value | Description | References |
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| Platelet | IC50 |
6.4 μM
Compound: 14
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Agonist activity at human PGI2 receptor assessed as inhibition of ADP-induced platelet aggregation
Agonist activity at human PGI2 receptor assessed as inhibition of ADP-induced platelet aggregation
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[PMID: 33314936] |
Selexipag (NS-304) is an orally available and long-acting IP receptor agonist prodrug, and its active form, MRE-269, is highly selective for the IP receptor. Selexipag (NS-304) inhibits the binding of [3H]Iloprost to the human and rat IP receptors in a concentration-dependent manner. The Ki is 260 nM for the human IP receptor and 2100 nM for the rat IP receptor. The intracellular cAMP levels in hIP-CHO cells are increased in a concentration-dependent manner by treatment with Selexipag (NS-304) with EC50 of 177nM. Selexipag (NS-304) also inhibits platelet aggregation in humans and monkeys with IC50 values of 5.5 and 3.4 μM, respectively, but it shows no inhibition in dogs (IC50 of >100 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 475086-01-2
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Appearance Solid
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Masse moléculaire 496.62
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Formule C26H32N4O4S
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Color White to yellow
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SMILES
O=C(NS(=O)(C)=O)COCCCCN(C1=NC(C2=CC=CC=C2)=C(C3=CC=CC=C3)N=C1)C(C)C
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Synonyms
NS-304; ACT-293987
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Am J Physiol Lung Cell Mol Physiol
Treatment of rat congenital diaphragmatic hernia with sildenafil and NS-304, selexipag's active compound, at the pseudoglandular stage improves lung vasculature. [Abstract]2018 Aug 1;315(2):L276-L285. PMID: 29745254
Selexipag purchased from MedChemExpress. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2018 Aug 1;315(2):L276-L285. [Abstract]
Western blot analysis shows the level of expression of Ptgir in control and CDH lungs, either untreated (placebo), with mono therapy (Sildenafil, NS-304) or with combination therapy (Sildenafil+NS-304). Total lung extracts of three independent rat pups are used for each group. Cofilin is used as loading control.
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Selexipag purchased from MedChemExpress. Usage Cited in: Erasmus Universiteit Rotterdam. 2017, November 30.
Representative images of immunohistochemistry staining show increased expression of Sma and an increased thickening of the vascular wall of small pulmonary vessels (25-50 µm) in CDH (p<0.001) and control lungs treated with all compounds (all p<0.001).
Solvant et solubilité
DMSO : ≥ 50 mg/mL (100.68 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.03 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocole
CHO cells expressing the human IP receptor (hIP-CHO cells) are seeded at 1×105 cells/well in a 24-well plate and cultured for 48 h. The cells are washed with Dulbecco's phosphate-buffered saline without divalent cations, preincubated in the medium for 1 h at 37°C, and then incubated for 15 min at 37°C with medium containing each drug in the presence of 500 μM 3-isobutyl-1-methylxanthine. The medium is removed, and perchloric acid solution is added to terminate the reaction. Intracellular cAMP levels are measured by enzymelinked immunosorbent assay[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Mice[1]
Male Sprague-Dawley rats, cynomolgus monkeys, and male beagle dogs are used. Selexipag (NS-304) is orally administered to rats at 10 mg/kg and to dogs at 3 mg/kg, and blood samples are collected at various times and centrifuged to obtain plasma. The plasma concentrations of Selexipag (NS-304) and MRE-269 after oral administration of Selexipag (NS-304) to each animal are determined by high performance liquid chromatography coupled to mass spectrometry (LC/MS), and their pharmacokinetic parameters are calculated.Rats are orally administered Selexipag (NS-304) at 3 mg/kg twice daily for 1, 2, 3, or 4 weeks as a pretreatment. On the day after the final administration in the pretreatment, rats are anesthetized with urethane, and the FSBF is measured with a laser Doppler flowmeter after intraduodenal administration of Selexipag (NS-304) at 3 mg/kg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (279 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Kuwano K, et al. 2-[4-[(5,6-diphenylpyrazin-2-yl)(isopropyl)amino]butoxy]-N-(methylsulfonyl)acetamide (NS-304), an orally available and long-acting prostacyclin receptor agonist prodrug. J Pharmacol Exp Ther. 2007 Sep;322(3):1181-8. [Content Brief]
[2]. Mous DS, et al. Treatment of rat congenital diaphragmatic hernia with sildenafil and NS-304, selexipag's active compound, at the pseudoglandular stage improves lung vasculature. Am J Physiol Lung Cell Mol Physiol. 2018 May 10. [Content Brief]
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 |
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| DMSO | 1 mM | 2.0136 mL | 10.0681 mL | 20.1361 mL | 50.3403 mL |
| 5 mM | 0.4027 mL | 2.0136 mL | 4.0272 mL | 10.0681 mL | |
| 10 mM | 0.2014 mL | 1.0068 mL | 2.0136 mL | 5.0340 mL | |
| 15 mM | 0.1342 mL | 0.6712 mL | 1.3424 mL | 3.3560 mL | |
| 20 mM | 0.1007 mL | 0.5034 mL | 1.0068 mL | 2.5170 mL | |
| 25 mM | 0.0805 mL | 0.4027 mL | 0.8054 mL | 2.0136 mL | |
| 30 mM | 0.0671 mL | 0.3356 mL | 0.6712 mL | 1.6780 mL | |
| 40 mM | 0.0503 mL | 0.2517 mL | 0.5034 mL | 1.2585 mL | |
| 50 mM | 0.0403 mL | 0.2014 mL | 0.4027 mL | 1.0068 mL | |
| 60 mM | 0.0336 mL | 0.1678 mL | 0.3356 mL | 0.8390 mL | |
| 80 mM | 0.0252 mL | 0.1259 mL | 0.2517 mL | 0.6293 mL | |
| 100 mM | 0.0201 mL | 0.1007 mL | 0.2014 mL | 0.5034 mL |
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