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Selexipag

Catalog No. T3216 CAS 475086-01-2

Synonyms: NS-304, ACT-293987, Uptravi

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).

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Selexipag, CAS 475086-01-2

Pack Size	Availability	Price/USD
5 mg	In stock	$ 42.00
10 mg	In stock	$ 58.00
25 mg	In stock	$ 84.00
50 mg	In stock	$ 97.00
1 mL * 10 mM (in DMSO)	In stock	$ 46.00

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Purity: 99.92%

Purity: 99.69%

Biological Description

Chemical Properties

Storage & Solubility Information

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].

Synonyms	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: 49.7 mg/mL(100 mM)

References and Literature

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.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library GPCR Compound Library EMA Approved Drug Library Anti-Cancer Clinical Compound Library Anti-Cancer Approved Drug Library Drug Repurposing Compound Library Immunology/Inflammation Compound Library Pediatric Drug Library Human Metabolite Library FDA-Approved & Pharmacopeia Drug Library

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Keywords

Selexipag 475086-01-2 GPCR/G Protein Immunology/Inflammation Others Prostaglandin Receptor NS 304 NS-304 ACT 293987 ACT-293987 Uptravi Inhibitor inhibit NS304 ACT293987 inhibitor

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