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15-deoxy-Δ12,14-Prostaglandin D2-d4 (15-deoxy-Δ12,14-PGD2-d4) is an internal standard for the quantification of 15-deoxy-Δ12,14-PGD2 (Item No. 12700) by GC- or LC-MS. 15-deoxy-Δ12,14-PGD2 is a metabolite of PGD2 (Item No. 12010).1 It is an agonist of PGD2 receptor 2 (DP2) that binds DP2 (Ki = 50 nM for the mouse receptor expressed in HEK293 cell membranes) and induces activation of eosinophils (EC50 = 8 nM).2,3 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.1 15-deoxy-Δ12,14-PGD2 is cytotoxic to L1210 murine leukemia cells (IC50 = 0.3 µg/ml).4 It inhibits ADP-induced platelet aggregation (IC50 = 320 ng/ml) less potently than PGD2.5WARNING This product is not for human or veterinary use. | [References]
[1] MATS SÖDERSTRÖM . Novel prostaglandin D2-derived activators of peroxisome proliferator-activated receptor-γ are formed in macrophage cell cultures[J]. Biochimica et biophysica acta. Molecular and cell biology of lipids, 2003, 1631 1: Pages 35-41. DOI: 10.1016/s1388-1981(02)00322-0 [2] AARON N HATA. Expression and molecular pharmacology of the mouse CRTH2 receptor.[J]. Journal of Pharmacology and Experimental Therapeutics, 2003, 306 2: 463-470. DOI: 10.1124/jpet.103.050955 [3] G. MONNERET. 15-Deoxy-Δ12,1412,14-prostaglandins D2 and J2 Are Potent Activators of Human Eosinophils1[J]. The Journal of Immunology, 2002, 28 1: 3563-3569. DOI: 10.4049/jimmunol.168.7.3563 [4] B M FORMAN. 15-Deoxy-delta 12, 14-prostaglandin J2 is a ligand for the adipocyte determination factor PPAR gamma.[J]. Cell, 1995, 83 5: 803-812. DOI: 10.1016/0092-8674(95)90193-0 [5] G. L. BUNDY. ChemInform Abstract: Synthesis and Platelet Aggregation Inhibiting Activity of Prostaglandin D Analogues.[J]. ChemInform, 1984, 15 8. DOI: 10.1002/chin.198408306 |
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