Selexipag NEW
| Price | $42 | $58 | $84 |
| Package | 5mg | 10mg | 25mg |
| Min. Order: | |
| Supply Ability: | 10g |
| Update Time: | 2024-11-17 |
Product Details
| Product Name: Selexipag | CAS No.: 475086-01-2 |
| Purity: 99.92% | Supply Ability: 10g |
| Release date: 2024/11/17 |
Product Introduction
Bioactivity
| 名稱 | Selexipag |
| 描述 | 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). |
| 細(xì)胞實(shí)驗(yàn) | 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]. |
| 體外活性 | Selexipag is an orally available and long-acting IP receptor agonist prodrug, and its active form, MRE-269, is highly selective for the IP receptor. Selexipag 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 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)[1]. |
| 體內(nèi)活性 | 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 administration[1]. |
| 存儲(chǔ)條件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 15 mg/mL (30.2 mM) |
| 關(guān)鍵字 | NS 304 | ACT 293987 | Prostaglandin Receptor | Inhibitor | inhibit | NS304 | Selexipag | ACT293987 |
| 相關(guān)產(chǎn)品 | Tranilast | Rutin | Rebamipide |
| 相關(guān)庫(kù) | 疼痛相關(guān)化合物庫(kù) | 經(jīng)典已知活性庫(kù) | EMA 上市藥物庫(kù) | 抗癌臨床化合物庫(kù) | 藥物功能重定位化合物庫(kù) | 抗癌上市藥物庫(kù) | FDA 上市藥物庫(kù) | 已知活性化合物庫(kù) |
Company Profile Introduction
Target Molecule Corp. (TargetMol) is a global high-tech enterprise, headquartered in Boston, MA, specializing in chemical and biological research product and service to meet the research needs of global customers.
TargetMol has evolved into one of the biggest global compound library and small molecule suppliers and a customer based on 40+ countries. TargetMol offers over 80 types of compound libraries and a wide range of high-quality research chemicals including inhibitors, activator, natural compounds, peptides, inhibitory antibodies, and novel life-science kits, for laboratory and scientific use. Besides, virtual screening service is also available for customers who would like to conduct the computer-aided drug discovery.
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