您好,欢迎来到化工原料网! [登录] [免费注册]
化工原料网
位置:首页 > 产品库 > Treprostinil(diethanolamine salt)
立即咨询
咨询类型:
     
*姓名:
*电话:
*单位:
Email:
*留言内容:
请详细说明您的需求。
*验证码:
 
Treprostinil(diethanolamine salt)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Treprostinil(diethanolamine salt)图片
CAS NO:830354-48-8
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
Treprostinil (UT-15C) diethanolamine 是一种有效的 EP2、DP1 和 IP 激动剂,对 EP2、DP1、IP、EP1、EP4、EP3 和 FP 的 Ki 值分别为 3.6、4.4、32.1、212、826、2505 和 4680 nM .
Cas No.830354-48-8
别名曲前列尼尔二乙醇胺盐,UT-15C
Canonical SMILESO=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 tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation 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)