Description | ASP1126 is a selective and orally active sphingosine-1-phosphate (S1P) agonist (EC50s: 7.12 nM, 517 nM for hS1P1 and hS1P3). |
In vitro | ASP1126 decreases the number of peripheral lymphocytes, naive T cells, central memory T cells, and effector memory T cells in the peripheral blood. |
In vivo | ASP1126 (1 and 5 mg/kg, orally once daily for 14 days) significantly prolongs allograft survival. ASP1126 in combination with 0.02 mg/kg tacrolimus notably improves graft survival time. |
Target activity | S1P1 (human):(EC50)7.12 nM , S1P3 (human): 517 nM |
molecular weight | 581.93 |
Molecular formula | C26H26ClF6NO5 |
CAS | 1228580-11-7 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
References | 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. |