CAS NO: | 830354-48-8 |
包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
Cas No. | 830354-48-8 |
别名 | 曲前列尼尔二乙醇胺盐,UT-15C |
Canonical SMILES | O=C([O-])COC1=C(C[C@](C[C@@H](O)[C@@H]2CC[C@@H](O)CCCCC)([H])[C@]2([H])C3)C3=CC=C1.OCC[NH2+]CCO |
分子式 | C23H33O5.C4H12NO2 |
分子量 | 495.7 |
溶解度 | DMF: 20 mg/ml,DMSO: 5 mg/ml,Ethanol: 13 mg/ml,PBS (pH 7.2): 5 mg/ml |
储存条件 | Store at -20°C |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | Treprostinil is a derivative of prostaglandin I2and an agonist of PGI2, PGD2, and PGE2receptors IP2, DP2, and EP2.1,2It binds selectively to IP2, DP2, and EP2over EP1, EP3, and EP4receptors with Kivalues of 32, 4.4, 3.6, 212, 2,505, and 826 nM, respectively, in radioligand binding assays.2Treprostinil inhibits LPS-induced production of TNF-α, IL-1β, IL-6, and granulocyte macrophage colony-stimulating factor (GM-CSF) in isolated human alveolar macrophages when used at a concentration of 200 ng/ml.3It also prevents LPS-induced nuclear translocation and activation of NF-κB in the same cells. Treprostinil relaxes isolated small pulmonary arteries and veins precontracted with the thromboxane A2(TP) receptor antagonist U-46619 , an effect that can be blocked by IP receptor antagonists in the arteries and reduced by IP receptor antagonists in the veins4. It reduces right ventricular systolic pressure, but not right ventricular hypertrophy, compared to hypoxic and sham control animals in a mouse model of chronic hypoxic pulmonary hypertension.5Formulations containing treprostinil have been used in the treatment of primary pulmonary hypertension. 1.Syed, N.I., and Jones, R.L.Assessing the agonist profiles of the prostacyclin analogues treprostinil and naxaprostene, particularly their DP? activityProstaglandins Leukot. Essent. Fatty Acids9519-29(2015) 2.Clapp, L.H., and Gurung, R.The mechanistic basis of prostacyclin and its stable analogues in pulmonary arterial hypertension: Role of membrane versus nuclear receptorsProstaglandins Other Lipid Mediat.12056-71(2015) 3.Raychauduri, B., Malur, A., Bonfield, T.L., et al.The prostacyclin analogue treprostinil blocks NFκB nuclear translocation in human alveolar macrophagesThe Journal of Biological Chemisty277(36)33344-33348(2002) 4.Orie, N.N., Ledwozyw, A., Williams, D.J., 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 veinsProstaglandins Other Lipid Mediat.1061-7(2013) 5.Nikam, V.S., Schermuly, R.T., Dumitrascu, R., et al.Treprostinil inhibits the recruitment of bone marrow-derived circulating fibrocytes in chronic hypoxic pulmonary hypertensionEur. Respir. J.36(6)1302-1314(2010) |