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81846-19-7

中文名稱 曲前列尼爾
英文名稱 REMODULIN
CAS 81846-19-7
分子式 C23H34O5
分子量 390.51
MOL 文件 81846-19-7.mol
更新日期 2024/12/20 09:35:51
81846-19-7 結(jié)構(gòu)式 81846-19-7 結(jié)構(gòu)式

基本信息

中文別名
瑞莫杜林
曲羅尼爾
曲前列環(huán)素
曲前列尼爾
曲前列尼爾中間體1
曲前列環(huán)素/曲前列尼爾
曲前列尼爾(瑞莫杜林)
曲前列尼爾(瑞莫杜林) 1G
TREPROSTINIL前列環(huán)素
英文別名
UT-15
LRX 15
BW 15AU
U 62840
15AU-81
Uniprost
Rumodolin
REMODULIN
Orenitram
TREPROSTINIL
所屬類別
原料藥:前列腺素類藥

物理化學性質(zhì)

熔點121-123°
沸點587.1±50.0 °C(Predicted)
密度1.158±0.06 g/cm3(Predicted)
儲存條件Sealed in dry,Store in freezer, under -20°C
溶解度可溶于氯仿(略微加熱)、甲醇(略微加熱)
酸度系數(shù)(pKa)3.19±0.10(Predicted)
形態(tài)固體
顏色灰白色至米色
InChIKeyPAJMKGZZBBTTOY-ZFORQUDYSA-N
SMILESC(O)(=O)COC1=C2C(=CC=C1)C[C@@]1([H])[C@@]([H])(C2)C[C@@H](O)[C@@H]1CC[C@@H](O)CCCCC

安全數(shù)據(jù)

常見問題列表

理化性質(zhì)
曲前列尼爾是是一個化學分子式,同時也是一種藥品。曲前列尼爾主要通過直接舒張肺和全身動脈血管床并抑制血小板聚集發(fā)揮作用。
概述
2002年美國批準曲前列環(huán)素皮下注射可用于肺動脈高壓的治療,2006年得到歐盟批準,2004年靜脈輸注曲前列環(huán)素治療肺動脈高壓也在美國得到了批準。
生物活性
Treprostinil (LRX-15) 是高效的DP1和EP2激動劑,其EC50值分別為0.6±0.1和6.2±1.2 nM。
靶點

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)

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(nèi)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.

曲前列尼爾價格(試劑級)
報價日期產(chǎn)品編號產(chǎn)品名稱CAS號包裝價格
2024/11/08HY-100441曲前列尼爾
Treprostinil
81846-19-72mg880元
2024/11/08HY-100441曲前列尼爾
Treprostinil
81846-19-710mM * 1mLin DMSO1503元
2024/11/08HY-100441曲前列尼爾
Treprostinil
81846-19-75mg1750元
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