Radioprotectin-1

1622006-09-0

C23H19ClN2O6S

H2O : < 0.1 mg/mL (insoluble); DMSO : 125 mg/mL (256.72 mM; Need ultrasonic)

GPCR/G Protein

Radioprotectin-1 is a potent and specific nonlipid agonist of lysophosphatidic acid receptor 2 (LPA₂), with an EC₅₀ value of 25 nM for murine LPA₂ subtype^[1]. IC50 & Target: EC50: 25 nM (murine LPA₂ subtype)^[1] In Vitro: Radioprotectin-1 is a potent agonist of LPA₂ with an EC₅₀ of 5 pM and functions as a full agonist at the human ortholog of LPA₂^[1].
Radioprotectin-1 (0-3 uM; 15 minutes) effectively reduces apoptosis induced by gamma-irradiation and the radiomimetic drug Adriamycin in cells that expressed LPA₂ either endogenously or after transfection^[1].
In Vivo: Radioprotectin-1 is a high-potency specific agonist of the murine LPA₂ GPCR ^[1].
Radioprotectin-1 (0.1 mg/kg, 0.3 mg/kg; s.c.; every 12 hours; for 3 days) decreases the mortality of C57BL/6 mice in models of the hematopoietic acute radiation syndromes (HE-ARS) and gastrointestinal acute radiation syndromes (GI-ARS) ^[1].
Radioprotectin-1 exerts its radioprotective and radiomitigative action through specific activation of the upregulated LPA₂ GPCR in Lgr5⁺stem cells^[1].