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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]. | [in vivo]
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). |
| [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 P DOI:10.1016/j.transproceed.2019.05.012 |
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BOC Sciences
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1-631-485-4226; 16314854226 |
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https://www.bocsci.com |
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