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Treprostinil

产品编号 T5150 CAS 81846-19-7

别名: LRX-15, 曲前列环素, 曲前列尼尔, Orenitram, Remodulin

Treprostinil 是有效的 DP1、IP 和 EP2 激动剂，EC50分别为0.6、1.9 和 6.2 nM。

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Treprostinil, CAS 81846-19-7

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其他形式的 Treprostinil:

Treprostinil diethanolamine
现货
Treprostinil Sodium
询价

选择批次

纯度: 99.71%

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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

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

存储

Powder: -20°C for 3 years | In solvent: -80°C for 2 years

溶解度

DMSO: 40 mg/mL

Ethanol: 20 mg/mL

( < 1 mg/mL refers to the product slightly soluble or insoluble )

参考文献

1. Whittle BJ, et al. Binding and activity of the prostacyclin receptor (IP) agonists, treprostinil and iloprost, at human prostanoid receptors: treprostinil is a potent DP1 and EP2 agonist. Biochem Pharmacol. 2012 Jul 1;84(1):68-75. 2. Kazemi Z, et al. Repurposing Treprostinil for Enhancing Hematopoietic Progenitor Cell Transplantation. Mol Pharmacol. 2016 Jun;89(6):630-44. 3. Ghonem N, et al. Treprostinil, a prostacyclin analog, ameliorates ischemia-reperfusion injury in rat orthotopic liver transplantation. 4. Smadja DM, et al. Treprostinil indirectly regulates endothelial colony forming cell angiogenic properties by increasing VEGF-A produced by mesenchymal stem cells. Thromb Haemost. 2015 Oct;114(4):735-47. 5. Nikam VS, et al. Treprostinil inhibits the recruitment of bone marrow-derived circulating fibrocytes in chronic hypoxic pulmonary hypertension. Eur Respir J. 2010 Dec;36(6):1302-14.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

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。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 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 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

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技术支持

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。

Keywords

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

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Treprostinil

存储

溶解度

参考文献

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剂量换算

体内实验配液计算器

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输入分子式，点击计算，可计算出产品的分子量。

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