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Treprostinil diethanolamine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Treprostinil diethanolamine图片
CAS NO:830354-48-8

UT-15C
Treprostinil diethanolamine (UT-15C) 是一种有效的EP2DP1IP激动剂,对 EP2、DP1、IP、EP1、EP4、EP3 和 FP 的Ki值分别为 3.6、4.4、32.1、212、826、2505 和 4680 nM。Treprostinil diethanolamine 增加 cAMP 的上调,从而维持血管系统内的动态平衡。Treprostinil diethanolamine 可导致人肺动脉的血管扩张。
生物活性

Treprostinil (UT-15C) diethanolamine is a potentEP2,DP1andIPagonist withKivalues of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1,IP, EP1, EP4, EP3 andFP, respectively. Treprostinil (UT-15C) diethanolamine increases upregulation of cAMP toward maintaining homeostasis within the vasculature. Treprostinil (UT-15C) diethanolamine can result in vasodilatation of human pulmonary arteries[1][2][3].

IC50& Target[1]

IP

32.1 nM (Ki)

FP

4680 nM (Ki)

体外研究
(In Vitro)

Treprostinil diethanolamine (UT-15C; 0.001-10,000 nM; 60 min; HEK293 cells) has high potency in activating DP1 and EP2 receptors as well as the IP receptor with EC50values of 0.6 nM, 6.2 nM and 1.9 nM, respectively, 36-fold less active at the EP3 receptor, 95-fold less active at the EP4 and 150-fold less active at the EP1 site than at the IP receptor[1].
Treprostinil diethanolamine (10 μM) increases cAMP accumulation in murine and human hematopoietic stem and progenitor cells (HSPCs)[2].
Treprostinil diethanolamine (10 μM; 2-6 h; PC3 cells) enhances the action of SDF-1 via CXCR4[2].

体内研究
(In Vivo)

Treprostinil diethanolamine (UT-15C; 0.15 mg/kg; i.h.; every 8 h; for 10 d; BALB/c mice) enhances the ability of HSPCs to repopulate the bone marrow and increases bone marrow reconstitution[2].
Treprostinil diethanolamine (0.15 mg/kg; i.h.; every 8 h; for 10 d; BALB/c mice) increases survival of lethally irradiated recipient mice[2].
Treprostinil diethanolamine (0.1 mg/kg; i.h.; for 24h; male lewis rats) inhibits the mRNA expression of TNF-α and IFN-γ and increases in IL-10 expression[3].

Animal Model:BALB/c mice[2]
Dosage:0.15 mg/kg
Administration:Subcutaneous injection; every 8 hours; for 10 days
Result:Increased survival of lethally irradiated recipient mice.
Animal Model:Male lewis rats[3]
Dosage:0.1 mg/kg
Administration:Subcutaneous injection; for 24 hours
Result:Decreased the mRNA expression of TNF-α and IFN-γ and increased the expression of IL-10.
Clinical Trial
分子量

495.65

Formula

C27H45NO7

CAS 号

830354-48-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

 
 
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