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Synonyms | NS-304, ACT-293987 | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C26H32N4O4S |
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分子量 | 496.62 | CAS No. | 475086-01-2 | |
Solubility (25°C)* | 体外 | DMSO | 99 mg/mL (199.34 mM) | |
Ethanol | 49 mg/mL (98.66 mM) | |||
Water | Insoluble | |||
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
製品説明 | Selexipag (NS-304, ACT-293987) is an orally active, first-in-class, selective prostacyclin IP receptor agonist with Ki value of 260 nM for human IP, whereas Ki values > 10,000 nM are measured at the other human G-protein-coupled prostanoid receptors (EP1-4, DP, FP and TP). |
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in vitro | Selexipag is an orally available, selective IP receptor agonist. It is rapidly hydrolysed in the hepatic microsomes to an active metabolite. Selexipag and its active metabolite have a higher binding affinity for the human IP receptor than for any other prostanoid receptor[1]. |
in vivo | As selexipag is rapidly hydrolysed in the liver to the active metabolite, peak-trough fluctuations in serum levels of active compound may be reduced, thereby reducing the likelihood of adverse events. Thus, Selexipag is well tolerated, with a safety profile in line with that of the expected pharmacological effect[1]. Selexipag has a half-life of 0.8-2.5 hours[2]. |
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Selexipag improves Lipopolysaccharide-induced ARDS on C57BL/6 mice by modulating the cAMP/PKA and cAMP/Epac1 signaling pathways [ Biol Pharm Bull, 2022, 10.1248/bpb.b21-01057] | PubMed: 35598975 |
Novel Targets in a High-Altitude Pulmonary Hypertension Rat Model Based on RNA-seq and Proteomics [ Front Med (Lausanne), 2021, 8:742436] | PubMed: 34805208 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。