Radioprotectin-1

Radioprotectin-1 is a potent and specific nonpaid agonist of LPA2, with an EC50 value of 25nM for murine LPA2 subtype[1].

Research Areas >> Others

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

EC50: 25 nM (murine LPA2 subtype)[1]

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 μM; 15 minutes) effectively reduces apoptosis induced by γ-irradiation and the radiomimetic drug Adriamycin in cells that expressed LPA2 either endogenously or after transfection[1]. Cell Viability Assay[1] Cell Line: MEF cells , IEC-6 cells Concentration: 0 μM, 0.1 μM, 0.3 μM, 1.0 μM,3 μM Incubation Time: 15 minutes Result: Protected cells from apoptosis by γ-irradiation- and the radiomimetic chemotherapeuticAdiamycin.

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]. Animal Model: 8-10 weeks old C57BL/6 female mice bearing total body irradiation (TBI) [1] Dosage: 0.1 mg/kg, 0.3 mg/kg Administration: Subcutaneous injection; every 12 hours; for 3 days Result: Decreased mortality of C57BL/6 mice in models of the HE-ARS and the GI-ARS.

[1]. Kuo B, et al. The LPA2 receptor agonist Radioprotectin-1 spares Lgr5-positive intestinal stem cells from radiation injury in murine enteroids. Cell Signal. 2018 Nov;51:23-33.