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15-keto Prostaglandin E2-d9 (15-keto PGE2-d9) is intended for use as an internal standard for the quantification of 15-keto PGE2 (Item No. 14720) by GC- or LC-MS. 15-keto PGE2 is a metabolite of PGE2 (Item No. 14010) formed by 15-hydroxy prostaglandin dehydrogenase (15-PGDH).1 Unlike PGE2, 15-keto PGE2 does not bind effectively to the PGE2 receptors EP2 and EP4 expressed in CHO cells (Kis = 2.6 and 15 μM, respectively) or induce adenylate cyclase activity in the same cells (EC50s = 1.8 and >33 μM, respectively). However, it does bind to EP2 and EP4 in HEK cells expressing these receptors (IC50s = 0.117 and 2.82 μM, respectively), as well as induces cAMP formation (EC50s = 0.137 and 0.426 μM, respectively) and the transcriptional activity of β-catenin/TCF in the same cells.2 15-keto PGE2 inhibits CD3-CD28-MHC-I-induced proliferation of isolated human CD4+ T cells in a concentration-dependent manner.3 It also reduces mortality in a mouse model of LPS-induced sepsis when administered at a dose of 15 mg/kg.4 a Kd = 1 nM for PGE2).1WARNING This product is not for human or veterinary use. | [References]
[1] N. NISHIGAKI A I M Negishi. Two Gs-coupled prostaglandin E receptor subtypes, EP2 and EP4, differ in desensitization and sensitivity to the metabolic inactivation of the agonist.[J]. Molecular Pharmacology, 1996, 146 1: 1031-1037. DOI: 10.1254/fpj.108.supplement_65
[2] SUZU ENDO. 15-Keto-PGE2 acts as a biased/partial agonist to terminate PGE2-evoked signaling.[J]. The Journal of Biological Chemistry, 2020: 13338-13352. DOI: 10.1074/jbc.ra120.013988
[3] LISA SCHMIDLEITHNER. Enzymatic Activity of HPGD in Treg Cells Suppresses Tconv Cells to Maintain Adipose Tissue Homeostasis and Prevent Metabolic Dysfunction.[J]. Immunity, 2019: 1232-1248.e14. DOI: 10.1016/j.immuni.2019.03.014
[4] ING-JUNG CHEN . Targeting the 15-keto-PGE2-PTGR2 axis modulates systemic inflammation and survival in experimental sepsis[J]. Free Radical Biology and Medicine, 2018, 115: Pages 113-126. DOI: 10.1016/j.freeradbiomed.2017.11.016 |
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