15-pgdh

SW033291 是有效的15-PGDH 抑制剂，与15-PGDH 亲和力高，Ki 为 0.1 nM。它增加骨髓和其他组织中前列腺素 PGE2 的水平。它还可促进组织再生。

ML-148 是 15-羟基前列腺素脱氢酶 (15-PGDH, IC50 = 56 nM) 的特异性抑制剂。 ML-148 可用于分析一组相关的脱氢酶或还原酶以及有关前列腺素信号通路的研究。

15-PGDH-IN-1 是一种有效的15-PGDH 抑制剂，具有口服活性。15-PGDH-IN-1 对重组人15-PGDH 具有抑制活性，IC50值为 3 nM。15-PGDH-IN-1 可用于组织修复和再生的研究。

15-PGDH-IN-2（Compound 2）是一种具有0.274 nM IC50值的15-PGDH抑制剂，适用于脱发、骨形成、胃溃疡以及皮肤伤口愈合的研究。

CAY10397, a selective inhibitor of 15-hydroxy PGDH, significantly suppresses endogenous 11-oxo-ETE production with a corresponding increase in 11(R)-HETE.

(±)14-HDHA是一种羟基二十二碳六烯酸，是DHA在细胞内通过酶促或非酶促反应生成的氧化代谢物，是15-PGDH的特异性底物之一并且可以被进一步氧化为具有抗炎性的14-oxoDHA，在原代肺泡巨噬细胞中，14-HDoHE 本身也能显著抑制 LPS 诱导的 IL-6 mRNA 表达，可能与哮喘等炎症性疾病有关。

20-hydroxy Prostaglandin F2α (20-hydroxy PGF2α) is the ω-oxidation product of PGF2α. Cultured type II alveolar cells from pregnant rabbits metabolize exogenous PGF2α via microsomal cytochrome P450 ω-oxidation, producing 20-hydroxy PGF2α and its 15-hydroxy PGDH metabolites. Cells from male rabbits exhibit only the 15-hydroxy PGDH pathway.

15-keto PGF1α is the initial metabolite of PGF1α via 15-hydroxy PGDH. In mammals, oxidation of C-15 markedly attenuates receptor binding and activity. In fish, the 15-keto compounds serve as post-ovulatory pheromones and are more active than the parent prostaglandins.

Prostaglandin K2 (PGK2), a 9,11-diketone derivative, results from PGE2 or PGD2 oxidation. Its biological presence remains speculative; however, it demonstrates resistance to in vitro metabolism by 15-hydroxy PGDH.

11β-13,14-Dihydro-15-keto PGF2α, a PGD2 metabolite in the 15-hydroxy PGDH pathway, is formed in human males upon infusion or inhalation of tritiated PGD2, with peak plasma levels of both 11β-PGF2α and 11β-13,14-dihydro-15-keto PGF2α observed within 10 minutes. In human lung homogenates, PGD2 is metabolized firstly to 11β-PGF2α and subsequently to 11β-15-keto-PGF2α in the presence of NAD+, but not to 11β-13,14-dihydro-15-keto PGF2α. Conversely, guinea pig liver and kidney homogenates can metabolize PGD2 to 11β-13,14-dihydro-15-keto PGF2α via 11β-PGF2α, with both NAD+ and NADP+ being requisite for this conversion.

15(R)-HETE, a monohydroxy fatty acid, is synthesized from arachidonic acid via aspirin-acetylated COX-2, leading to the formation of specialized pro-resolving mediators 15(R)-lipoxin A4 and B4 through a transcellular mechanism involving 5-lipoxygenase (5-LO). Additionally, this compound is produced by the cytochrome P450 (CYP) isoform CYP2C9 and can be generated from arachidonic acid by COX-1 in human mast cells, where it accumulates due to its resistance to conversion into 15-KETE by 15-hydroxyprostaglandin dehydrogenase (15-PGDH). As an agonist of PPARβ δ, 15(R)-HETE induces the expression of a target gene in NIH3T3 cells, demonstrating its biological significance.

13,14-Dihydro-15-keto prostaglandin D2 (DK-PGD2), a PGD2 metabolite formed by the 15-hydroxyl PGDH pathway, is a selective agonist for the DP2 receptor and can inhibit ion flux in canine colonic mucosa preparation [1].

15-epi-PGE1 (15R-Prostaglandin E1; 15-Epiprostaglandin E1) 作为PGE1的立体异构体，在生物活性方面显得较为低下。该化合物为人胎盘15-羟基前列腺素脱氢酶 (15-PGDH) 的非竞争性抑制剂，具有170 μM的IC50值。