赛乐西帕 T3216

Product Introduction
Bioactivity


英文名: Selexipag

描述: Selexipag (ACT-293987) 是前列环素受体激动剂，可引起肺血管舒张，用于治疗肺动脉高压。

细胞实验: 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].

体外活性: 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].

体内活性: 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].

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 15 mg/mL (30.2 mM)


关键字: NS 304 | ACT 293987 | Prostaglandin Receptor | Inhibitor | inhibit | NS304 | Selexipag | ACT293987

相关产品: mPGES1-IN-3 | 3-O-Acetyl-16α-hydroxydehydrotrametenolic acid | ONO-AE3-208 | Epibetulinic acid | Timapiprant | Chamigrenal | 6,4'-Dihydroxy-7-methoxyflavanone | Oxysophocarpine | AZD1981 | Latanoprost

相关库: Anti-Aging Compound Library | Drug Repurposing Compound Library | Approved Drug Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Pediatric Drug Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library

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注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途