Selexipag

SKU: orb1304415

Description

Selexipag

Research Area

Immunology & Inflammation, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 475086-01-2
• MW: 496.62
• Purity: 99.92%
• Formula: C₂₆H₃₂N₄O₄S
• SMILES: N(CCCCOCC(NS(C)(=O)=O)=O)(C(C)C)C=1N=C(C(=NC1)C2=CC=CC=C2)C3=CC=CC=C3
• Target: Prostaglandin Receptor
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (4.03 mM);DMSO:15 mg/mL (30.2 mM)

Bioactivity

• Target IC50:
  IP (human):260 nM (Ki)
• In Vivo:
  The Cmax of MRE-269 after oral administration of Selexipag is 1.1 μg mL in rats and 9.0 μg mL in dogs. Selexipag 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 at 3 mg/kg causes a sustained increase in FSBF and exhibits a maximal increase of 93% in FSBF 1 h after administratio.
• In Vitro:
  Selexipag is an orally available and long-acting IP receptor agonist prodrug, and its active form, MRE-269, is highly Selective fo the IP receptor. Selexipag inhibit the binding of [3H]Iloprost to the human and rat IP receptors in a concentration dependent manner the Ki is 260 nM fo the human IP receptor and 2100 nM fo the rat IP receptor the intracellular cAMP levels in hIP-CHO cells are increased in a concentration dependent manner by treatment with Selexipag with EC50 of 177 nM. Selexipag 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.
• Cell Research:
  NS-304 is dissolved in DMSO and stored, and then diluted with appropriate medium before us. CHO cells expressin the human IP receptor (hIP-CHO cells) are seeded at × 0^5 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℃, and then incubated for 15 min at 37℃ith 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 terminat the reaction. Intracellular cAMP levels are measured by enzymelinked immunosorbent assa.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

ACT-293987, ACT 293987, ACT293987, Inhibitor, inhibit, NS 304, NS304, NS-304, prostacyclin receptor, Prostaglandin Receptor, ProstaglandinReceptor, Selexipag, Uptravi

Compound Identifiers

PubChem CID

9913767