Treprostinil (diethanolamine)

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]. 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 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^[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]. 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].