Treprostinil (UT-15C) diethanolamine 是一种有效的EP2、DP1和IP激动剂,EP2、DP1、IP、EP1、EP4、EP3 和 FPKi的值分别为 3.6、4.4、32.1、212、826、2505 和 4680 nM。Treprostinil (UT-15C) diethanolamine 增加 cAMP 的上调,从而维持血管系统内的动态平衡。Treprostinil (UT-15C) diethanolamine 可导致人肺动脉的血管扩张。
产品描述
Treprostinil (UT-15C) diethanolamine is a potent EP2, DP1 and IP agonist with K i values of 3.6, 4.4, 32.1, 212, 826, 2505 and 4680 nM for EP2, DP1, IP, EP1, EP4, EP3 and FP, 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].
体外活性
Treprostinil (UT-15C) diethanolamine (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 EC 50 values 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 (UT-15C) diethanolamine (10 μM) increases cAMP accumulation in murine and human hematopoietic stem and progenitor cells (HSPCs) [2]. Treprostinil (UT-15C) diethanolamine (10 μM; 2-6 h; PC3 cells) enhances the action of SDF-1 via CXCR4 [2].
体内活性
Treprostinil (UT-15C) diethanolamine (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 (UT-15C) 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 (UT-15C) 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.
Cas No.
830354-48-8
分子式
C27H45NO7
分子量
495.65
储存和溶解度
(< 1 mg/ml refers to the product slightly soluble or insoluble )
Powder: -20°C for 3 years
In solvent: -80°C for 2 years