MRE-269-ACT-333679-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEMRE-269Cat. No.: HY-79593CAS No.: 475085-57-5Synonyms: ACT-333679分式: CHNO分量: 419.52作靶點(diǎn): Prostaglandin Receptor作通路: GPCR/G Protein儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (11

2、9.18 mM)H2O : 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (5.96 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (5.96 mM); Suspended solution; Need ultrasonic and warming3. 請依序添加每種溶劑： 10% DMSO 90% c

3、orn oilSolubility: 2.5 mg/mL (5.96 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 MRE-269是selexipag 的有效代謝物，同時為選擇性的 IP 受體激動劑。IC50 & Target IP Receptor體外研究 MRE-269 induces endothelium-independent vasodilation of rat extralobar pulmonary artery (EPA). MRE-269or other IP receptor agonists including epoproste

4、nol, iloprost, treprostinil and beraprost increase cAMP levelsin hPASMC 1. MRE-269 induces concentration-dependent vasodilation in LPA(+), LPA(-), and SPA(-) 3.體內(nèi)研究 The vasorelaxant effects of MRE-269 on rat small intralobar pulmonary artery (SIPA) and EPA are the same,while the other IP receptor ag

5、onists induce less vasodilation in SIPA than in EPA 1. MRE-269 producessubstantial relaxation of rat small pulmonary artery, although its effects are only significant at highconcentrations of above 10 M (pEC50, 4.980.22). By contrast, in rat small pulmonary veins, MRE-269 onlyproduces minimal relaxa

6、tion over the whole concentration range, with only significant relaxation occurring atthe two highest doses of MRE-269 of 10 and 100 M 2.REFERENCES1. Fuchikami C, et al. A comparison of vasodilation mode among selexipag (NS-304; 2-4-(5,6-diphenylpyrazin-2-yl)(isopropyl)aminobutoxy-N-(methylsulfonyl)

7、acetamide), its active metabolite MRE-269 and various prostacyclin receptor agonists in rat,porcin2. Orie NN, et al. Differential actions of the prostacyclin analogues treprostinil and iloprost and the selexipag metabolite, MRE-269 (ACT-333679) in rat small pulmonary arteries and veins. Prostaglandi

8、ns Other Lipid Mediat. 2013 Oct;106:1-73. Kuwano K, et al. A long-acting and highly selective prostacyclin receptor agonist prodrug, 2-4-(5,6-diphenylpyrazin-2-yl)(isopropyl)aminobutoxy-N-(methylsulfonyl)acetamide (NS-304), ameliorates rat pulmonary hypertension with unique relaxant responsesMcePdfHeightCaution: Product has not been fully validated for medical applications