Powder: -20°C for 3 years | In solvent: -80°C for 2 years
Treprostinil 是有效的 DP1、IP 和 EP2 激动剂,EC50分别为0.6、1.9 和 6.2 nM。
产品描述 | Treprostinil is a potent DP1, IP and EP2 agonist (EC50: 0.6/1.9/6.2 nM). |
靶点活性 | EP3:68.9 nM (EC50), EP2:6.2 nM (EC50), DP1:0.6 nM (EC50), IP:1.9 nM (EC50) |
体外活性 | Treprostinil has a high affinity for the IP, EP2 and DP1 receptors (Ki: 32, 3.6 and 4.4 nM, respectively), low affinity for EP1 and EP4 receptors and even lower affinity for EP3, FP, and TP receptors. Activation of IP, DP1 and EP2 receptors can all result in vasodilatation of human pulmonary arteries[1]. Treprostinil inhibits the viability of cultured endothelial colony forming cells. Endothelial colony forming cells proliferation is stimulated by conditioned media from Treprostinil pretreated mesenchymal stem cells [2]. |
体内活性 | Treprostinil is most efficacious in raising intracellular cAMP levels in murine and human hematopoietic stem and progenitor cells [2]. Treprostinil preserves the sinusoidal endothelial cell lining and reduces platelet deposition early post-transplantation compared to placebo. Hepatic tissue blood flow is significantly compromised in the placebo group, whereas treprostinil maintains blood flow similar to normal levels [3]. Treprostinil treatment significantly increases the vessel-forming ability of endothelial colony forming cells combined with mesenchymal stem cells in Matrigel implanted in nude mice. Silencing VEGF-A gene in mesenchymal stem cells also blocks the pro-angiogenic effect of Treprostinil [4]. Treatment with Treprostinil significantly reduces the recruitment of cells compared to normoxic mice. Treprostinil also reduces right ventricular systolic pressure and slightly reduces the vascular remodeling but fails to reverse the right ventricular hypertrophy [5]. |
细胞实验 | Human or murine hematopoietic stem and progenitor cells are incubated in the presence of vehicle or the combination of 10 μM Treprostinil and 30 μM forskolin at 37°C for 1 hour and 24 hours. After washing with phosphate-buffered saline at 4°C, cells are stained for externalized phosphatidylserine with the apoptosis kit [2]. |
动物实验 | Male Lewis rats weighing 200-300 g are used in the study. Donor animals receive treprostinil or placebo 24 h before hepatectomy and the corresponding recipient animal receive a similar treatment until the time of sacrifice. The surgeon is blinded to treatment. Recipients are sacrificed at 1, 3, 6, 24 and 48 h post-transplantation to examine the early events after IRI. Treprostinil (100 ng/kg/min) or placebo is administered subcutaneously via an Alzet implantable osmotic pump. This dose is selected to achieve a steady-state plasma concentration in the range of 5-20 ng/mL [3]. . Bone marrow transplanted (BMT) mice are divided into five different groups with each group consisting of 6 to 10 mice. One group of mice is exposed to hypoxia (10% inspired oxygen fraction) in a normobaric chamber whereas the second group (control BMT) of animals are placed in a normoxic chamber with a normal oxygen environment (21% inspired O2 fraction) for 28 days. Sham group mice receive saline treatment whereas two other groups of mice receive Treprostinil infusions of different dose levels (14 ng/kg and 70 ng/kg per minute) and are exposed to hypoxia for 4 weeks. For comparison, human infusion rates in PAH therapy vary from 10 to 60 ng/kg per min[5]. |
别名 | LRX-15, 曲前列环素, 曲前列尼尔, Orenitram, Remodulin |
分子量 | 390.51 |
分子式 | C23H34O5 |
CAS No. | 81846-19-7 |
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
DMSO: 40 mg/mL
Ethanol: 20 mg/mL
( < 1 mg/mL refers to the product slightly soluble or insoluble )
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
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您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
Treprostinil 81846-19-7 GPCR/G Protein Immunology/Inflammation Prostaglandin Receptor LRX-15 Inhibitor UT-15 曲前列环素 曲前列尼尔 UT15 inhibit Orenitram Remodulin UT 15 inhibitor