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289480-64-4

中文名稱 曲前列尼爾鈉
英文名稱 REMODULIN
CAS 289480-64-4
分子式 C23H34O5
分子量 390.517
MOL 文件 289480-64-4.mol
更新日期 2024/11/06 21:56:18
289480-64-4 結構式 289480-64-4 結構式

基本信息

中文別名
曲列前素
曲前列素
曲前列尼爾鈉
曲前列尼爾酸
曲前列環(huán)素鈉鹽
曲前列尼爾鈉9(瑞莫杜林)
曲前列尼爾鈉9(瑞莫杜林) 1G
曲前列尼爾鈉289480-64-4,工廠零售289480-64-4
英文別名
UT 15 (pharMaceutical)
Treprostinil Sodium API
Treprostinil sodium salt
Treprostinil Sodium (UT-15)
289480-64-4 Treprostinil Sodium

物理化學性質

儲存條件Inert atmosphere,Store in freezer, under -20°C
溶解度DMSO : ≥ 26 mg/mL (63.03 mM)
形態(tài)固體
顏色白色

安全數據

危險性符號(GHS)GHS hazard pictograms
GHS07
警示詞警告
危險性描述H302-H315-H319-H335
海關編碼2918999090

常見問題列表

應用

吸入曲前列素鈉(一種前列環(huán)素類似物)是最近獲得FDA批準用于治療致命性孤兒疾病的藥物:肺動脈高壓(PAH)。與安慰劑相比,曲前列環(huán)素可保留竇狀內皮細胞襯里并減少移植后早期的血小板沉積。安慰劑組的肝組織血流明顯受損,而曲前列環(huán)素維持血流量與正常水平相似。前列腺素治療顯著增加內皮細胞集落形成細胞與間充質干細胞在裸鼠移植的基質膠中的血管形成能力。在間充質干細胞中沉默VEGF-A基因也會阻斷曲前列環(huán)素的促血管生成作用。曲前列環(huán)素在提高小鼠和人類造血干細胞和祖細胞中的細胞內cAMP水平方面最有效。與常氧小鼠相比,用曲前列環(huán)素治療顯著減少細胞募集。曲前列環(huán)素還可降低右心室收縮壓并略微減少血管重塑,但無法逆轉右心室肥厚。

作用機制
曲前列環(huán)素對DP1,EP2和IP受體具有高親和力(分別為Ki = 4.4,3.6和32nM),對EP1和EP4受體的親和力低,對EP3,FP和TP受體的親和力甚至更低。與曲前列環(huán)素一樣,IP,DP1和EP2受體的激活均可導致人肺動脈的血管舒張。前列環(huán)素抑制培養(yǎng)的內皮細胞集落形成細胞的活力。來自曲前列素預處理的間充質干細胞的條件培養(yǎng)基刺激內皮細胞集落形成細胞增殖。
生物活性
Treprostinil sodium (UT-15, Remodulin, Orenitram, Tyvaso, Trevyent) 是一種有效的 DP1、EP2 和 IP 受體的激動劑,對應的Ki值分別為4.4 nM、3.6 nM和32 nM。
靶點
TargetValue
EP2
(Cell-free assay)
3.6 nM(Ki)
DP1
(Cell-free assay)
4.4 nM(Ki)
IP
(Cell-free assay)
32 nM(Ki)
體外研究

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.

體內研究

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.

曲前列尼爾鈉價格(試劑級)
報價日期產品編號產品名稱CAS號包裝價格
2024/08/19S0325曲前列尼爾鈉
Treprostinil sodium
289480-64-45mg2456.96元
2024/08/19S0325曲前列尼爾鈉
Treprostinil sodium
289480-64-425mg8187.17元
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