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Pack Size | Price | Availability | Quantity |
---|---|---|---|
5 mg | $42 | In Stock | |
10 mg | $58 | In Stock | |
25 mg | $84 | In Stock | |
50 mg | $97 | In Stock | |
1 mL x 10 mM (in DMSO) | $46 | In Stock |
Description | Selexipag (ACT-293987)(NS-304) is prostacyclin receptor agonist that causes vasodilation in pulmonary vasculature and is used in the therapy of pulmonary arterial hypertension (PAH). |
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 177 nM. 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 | Following oral administration, MRE-269 achieves a peak concentration (Cmax) of 1.1 μg/mL in rats and 9.0 μg/mL in dogs. When administered intraduodenally at doses of 1 or 3 mg/kg, NS-304 enhances femoral skeletal blood flow (FSBF) in anesthetized rats for over 4 hours in a dose-dependent manner. Notably, a dose of 3 mg/kg NS-304 significantly elevates FSBF, achieving a peak increase of 93% one hour post-administration[1]. |
Cell Research | 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]. |
Alias | NS-304, ACT-293987, Uptravi |
Molecular Weight | 496.62 |
Formula | C26H32N4O4S |
Cas No. | 475086-01-2 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | |||||||||||||||||||||||||
Solubility Information | DMSO: 15 mg/mL (30.2 mM) ![]() | |||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||
DMSO
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