Treprostinil CAS NO.81846-19-7

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• CAS号:81846-19-7
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• 英文名:REMODULIN
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• 中文名:曲前列尼尔
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• CBNumber:CB7231250
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• 分子式:C23H34O5
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• 分子量:390.51
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• MOL File:81846-19-7.mol

曲前列尼尔化学性质

• 熔点 :121-123°
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• 沸点 :587.1±50.0 °C(Predicted)
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• 密度 :1.158±0.06 g/cm3(Predicted)
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• 储存条件 :Sealed in dry,Store in freezer, under -20°C
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• 溶解度 :Chloroform (Slightly, Heated), Methanol (Slightly, Heated)
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• 形态 :Solid
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• 酸度系数(pKa) :3.19±0.10(Predicted)
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• 颜色 :Off-White to Beige

曲前列尼尔性质、用途与生产工艺

• 理化性质 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。
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• 概述 2002年美国批准曲前列环素皮下注射可用于肺动脉高压的治疗，2006年得到欧盟批准，2004年静脉输注曲前列环素治疗肺动脉高压也在美国得到了批准。
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• 生物活性 Treprostinil (LRX-15) 是高效的DP1和EP2激动剂，其EC50值分别为0.6±0.1和6.2±1.2 nM。
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• 靶点

  DP/DP1 Receptor   0.6 nM (EC 50 )

  IP Receptor   1.9 nM (EC 50 )

  EP 2 Receptor   6.2 nM (EC 50 )

  EP3 Receptor   68.9 nM (EC 50 )

  EP 4 Receptor   181 nM (EC 50 )

  EP 1 Receptor   285 nM (EC 50 )

  TP Receptor   919 nM (EC 50 )

  EP 2 Receptor   3.6 nM (Ki)

  EP 1 Receptor   212 nM (Ki)

  EP 4 Receptor   826 nM (Ki)

  EP3 Receptor   2505 nM (Ki)

  DP/DP1 Receptor   4.4 nM (Ki)

  IP Receptor   32.1 nM (Ki)

  FP Receptor   4680 nM (Ki)

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• 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.

   

   

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• 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.