中文名 | Treprostinil |
英文名 | Treprostinil |
别名 | 瑞莫杜林 曲罗尼尔 曲前列环素 曲前列尼尔 曲前列尼尔中间体1 曲前列尼尔(瑞莫杜林) |
英文别名 | UT-15 LRX 15 U-62840 BW 15AU UNIPROST RUMODOLIN Treprostinil Treprostinil-13C2-d1 Treprostinil free acid [[(1R,2R,3aS,9aS)-2,3,3a,4,9,9a-Hexahydro-2-hydroxy-1-[(3S)-3-hydroxyoctyl]-1H-benz[f]inden-5-yl]oxy]acetic acid 2-[[[(1R,2R,3aS,9aS)-2α-Hydroxy-1β-[(S)-3-hydroxyoctyl]-2,3,3a,4,9,9a-hexahydro-1H-benzo[f]indene]-5-yl]oxy]acetic acid |
CAS | 81846-19-7 |
EINECS | 808-233-7 |
化学式 | C23H34O5 |
分子量 | 390.51 |
密度 | 1.158±0.06 g/cm3(Predicted) |
熔点 | 121-123° |
沸点 | 587.1±50.0 °C(Predicted) |
溶解度 | 氯仿 (微溶,加热),甲醇 (微溶,加热) |
酸度系数 | 3.19±0.10(Predicted) |
存储条件 | Sealed in dry,Store in freezer, under -20°C |
外观 | 固体 |
颜色 | Off-White to Beige |
物化性质 | 曲前列尼尔是是一个化学分子式,同时也是一种药品。曲前列尼尔主要通过直接舒张肺和全身动脉血管床并抑制血小板聚集发挥作用。 |
体外研究 | Treprostinil has high affinity for the DP1, EP2 and IP receptors (K i =4.4, 3.6 and 32 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, as with treprostinil, can all result in vasodilatation of human pulmonary arteries.Treprostinil inhibits viability of cultured endothelial colony forming cells. Endothelial colony forming cells proliferation is stimulated by conditioned media from Treprostinil pretreated mesenchymal stem cells. |
体内研究 | Inhaled treprostinil sodium, a prostacyclin analog, is the most recent agent to receive FDA approval for the treatment of a fatal orphan disease: pulmonary arterial hypertension (PAH). 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.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. Treprostinil is most efficacious in raising intracellular cAMP levels in murine and human hematopoietic stem and progenitor cells. 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 remodelling but fails to reverse the right ventricular hypertrophy. |
上游原料 | 曲前列尼尔二乙醇胺盐 101692-03-9 Treprostinil Methyl Ester |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.561 ml | 12.804 ml | 25.608 ml |
5 mM | 0.512 ml | 2.561 ml | 5.122 ml |
10 mM | 0.256 ml | 1.28 ml | 2.561 ml |
5 mM | 0.051 ml | 0.256 ml | 0.512 ml |