1. GPCR/G Protein
  2. Prostaglandin Receptor

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

Cat. No.: HY-14870 Purity: 99.93%
Handling Instructions

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.

NS-304 Chemical Structure

NS-304 Chemical Structure

CAS No. : 475086-01-2

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 125 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg USD 114 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
10 mg USD 174 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
50 mg USD 576 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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Customer Review

    NS-304 purchased from MCE. Usage Cited in: Am J Physiol Lung Cell Mol Physiol. 2018 May 10.

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    Prostacyclin receptor[1]

    In Vitro

    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. 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 NS-304 with EC50 of 177nM. 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].

    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. 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, 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].

    Clinical Trial
    References
    Preparing Stock Solutions
    Concentration Volume 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.
    Cell Assay
    [1]

    NS-304 is dissolved in DMSO and stored, and then diluted with appropriate medium before use[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]

    NS-304 is prepared in aqueous solution[1].

    Mice[1]
    Male Sprague-Dawley rats, cynomolgus monkeys, and male beagle dogs are used. S-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 NS-304 and MRE-269 after oral administration of 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 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 NS-304 at 3 mg/kg. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    496.62

    Formula

    C₂₆H₃₂N₄O₄S

    CAS No.

    475086-01-2

    SMILES

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

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    NS-304 is dissolved in 0.8% ethanol in water[2].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

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    Inquiry Information

    Product Name:
    NS-304
    Cat. No.:
    HY-14870
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