2. GPCR/G Protein
  3. Prostaglandin Receptor
  4. Selexipag

Selexipag  (Synonyms: NS-304; ACT-293987)

Cat. No.: HY-14870 Purity: 99.92%
COA Handling Instructions

Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).

For research use only. We do not sell to patients.

Selexipag Chemical Structure

Selexipag Chemical Structure

CAS No. : 475086-01-2

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10 mM * 1 mL in DMSO USD 55 In-stock
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Customer Review

Based on 4 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Selexipag purchased from MCE. 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.

    Selexipag purchased from MCE. 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).

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Selexipag (NS-304) is an orally available and potent agonist for the Prostacyclin (PGI2) receptor (IP receptor).

    IC50 & Target[1]

    hIP

    260 nM (Ki)

    In Vitro

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    In Vivo

    The Cmax of MRE-269 after oral administration of NS-304 is 1.1 μg/mL in rats and 9.0 μg/mL in dogs. Selexipag (NS-304) at 1 or 3 mg/kg increases FSBF in anesthetized rats for more than 4 h after intraduodenal administration in a dose-dependent manner. In particular, Selexipag (NS-304) at 3 mg/kg causes a sustained increase in FSBF and exhibits a maximal increase of 93% in FSBF 1 h after administration[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    496.62

    Appearance

    Solid

    Formula

    C26H32N4O4S
    CAS No.
    SMILES

    O=C(NS(=O)(C)=O)COCCCCN(C1=NC(C2=CC=CC=C2)=C(C3=CC=CC=C3)N=C1)C(C)C
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (100.68 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.0136 mL 10.0681 mL 20.1361 mL
    5 mM 0.4027 mL 2.0136 mL 4.0272 mL
    10 mM 0.2014 mL 1.0068 mL 2.0136 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      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

    • 2.

      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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.03 mM); Clear solution

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.92%

    COA (249 KB) LCMS (265 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
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    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Selexipag475086-01-2NS-304 ACT-293987NS304NS 304ACT293987ACT 293987ACT-293987Prostaglandin ReceptorInhibitorinhibitorinhibit

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