ASP1126

ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist, with EC50 values of 7.12 nM, 517 nM for hS1P1 and hS1P3, respectively. ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells and effector memory T cells in the peripheral blood. ASP1126 has the potential to be applied in clinical transplantation with improved safety profile[1].

Signaling Pathways >> GPCR/G Protein >> LPL Receptor

Research Areas >> Inflammation/Immunology

EC50: 7.12 nM (hS1P1), 517 nM (hS1P3)[1].

ASP1126 (1 and 5 mg/kg, orally once daily for 14 days) significantly prolongs allograft survival[1]. ASP1126 in combination with 0.02 mg/kg tacrolimus notably improves graft survival time[1]. Animal Model: ACI and Lewis rats aged 6 weeks were used as cardiac donors and recipients, respectively[1]. Dosage: 0.2 mg/kg, 1 mg/kg, 5 mg/kg. Administration: Orally once daily for 14 days. Result: Significantly prolonged allograft survival (median survival time [MST] =9; 8 days at 1 and 5 mg/kg, respectively, compared with 6 days in the vehicle group).

[1]. Okimoto A, et al. ASP1126, a Novel Sphingosine-1-Phosphate-Selective Agonist With a Favorable Safety Profile, Prolongs Allograft Survival in Rats and Nonhuman Primates in Combination With Tacrolimus With a Broad Safety Margin for Bradycardia. Transplant Proc. 2019 Jul - Aug;51(6):2081-2098.