Description
15-deoxy-Δ
12,14-PGD
2 is a metabolite of PGD
2 . It is an agonist of PGD
2 receptor 2 (DP
2) that binds DP
2 (K
i = 50 nM for the mouse receptor expressed in HEK293 cell membranes) and induces activation of eosinophils (EC
50 = 8 nM). It also stimulates the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ) and induces PPARγ-mediated transcription in a reporter assay when used at a concentration of 5 μM. 15-deoxy-Δ
12,14-PGD
2 is cytotoxic to L1210 murine leukemia cells (IC
50 = 0.3 μg/ml). It inhibits ADP-induced platelet aggregation (IC
50 = 320 ng/ml) less potently than PGD
2.
Uses
15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2), a metabolite of PGD2 (HY-101988), is an agonist of prostaglandin receptor 2 (DP2). 15-deoxy-Δ12,14-Prostaglandin D2 binds to DP2 (Ki=50 nM) and induces eosinophil activation (EC50=8 nM). 15-deoxy-Δ12,14-Prostaglandin D2 also stimulates the recruitment of steroid receptor coactivator-1 (SRC-1) to peroxisome proliferator-activated receptor γ (PPARγ), inducing PPARγ-mediated transcription. 15-deoxy-Δ12,14-Prostaglandin D2 (15-Deoxy-Δ12,14-PGD2) is cytotoxic to L1210 murine leukemia cells (IC50=0.3 μg/ml) and inhibits ADP-induced platelet aggregation (IC50=320 ng/mL).
References
[1] Bundy, et al. Synthesis and platelet aggregation inhibiting activity of prostaglandin D analogues. J. Med. Chem. 26(6), 790-799 (1983).
