CasImg
曲前列尼尔
产品纠错
CAS号:81846-19-7 | 英文名称:REMODULIN
分子式 C23H34O5
分子量 391
EINECS号 808-233-7
MDL MFCD00888847
Smiles
InChIKey
乙二醇化学百科
基本信息
中文名称 曲前列尼尔
英文名称 Treprostinil
CAS号 81846-19-7
分子式 C23H34O5
分子量 390.51
EINECS号 808-233-7
SMILES C(O)(=O)COC1=C2C(=CC=C1)C[C@@]1([H])[C@@]([H])(C2)C[C@@H](O)[C@@H]1CC[C@@H](O)CCCCC
物化性质
熔点 121-123°
沸点 587.1±50.0 °C(Predicted)
密度 1.158±0.06 g/cm3(Predicted)
溶解度 可溶于氯仿(略微加热)、甲醇(略微加热)
形态 固体
酸度系数(pKa) 3.19±0.10(Predicted)
颜色 灰白色至米色
安全信息
生产及用途
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。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。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。

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)

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.

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.

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