Treprostinil (diethanolamine salt)
(Synonyms: 曲前列尼尔二乙醇胺盐,UT-15C) 目录号 : GC48202
An agonist of IP2, DP2, and EP2 receptors
Cas No.:830354-48-8
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Treprostinil is a derivative of prostaglandin I2 and an agonist of PGI2, PGD2, and PGE2 receptors IP2, DP2, and EP2.1,2 It binds selectively to IP2, DP2, and EP2 over EP1, EP3, and EP4 receptors with Ki values of 32, 4.4, 3.6, 212, 2,505, and 826 nM, respectively, in radioligand binding assays.2 Treprostinil 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.3 It 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.5 Formulations 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)
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.0173 mL | 10.0867 mL | 20.1735 mL |
| 5 mM | 0.4035 mL | 2.0173 mL | 4.0347 mL |
| 10 mM | 0.2017 mL | 1.0087 mL | 2.0173 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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