曲前列尼尔二乙醇胺盐  98%

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产品简介:一种有效的 EP2、DP1 和 IP 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。
靶点:DP1:4.4 nM (Ki) EP1: 212 nM (Ki) EP4:826 nM (Ki) EP3:2505 nM (Ki) IP:32.1 nM (Ki) FP:4680 nM (Ki) EP2:3.6 nM (Ki)
体外研究: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 EC50 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. Treprostinil diethanolamine (10 μM) increases cAMP accumulation in murine and human hematopoietic stem and progenitor cells (HSPCs) . Treprostinil diethanolamine (10 μM; 2-6 h; PC3 cells) enhances the action of SDF-1 via CXCR4.
体内研究: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. Treprostinil diethanolamine (0.15 mg/kg; i.h.; every 8 h; for 10 d; BALB/c mice) increases survival of lethally irradiated recipient mice. 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.
保存条件:-20°C
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