oa 3

Kartogenin (KGN) sodium 是一种软骨样组织形成的诱导剂 (EC50: 100 nM)。Kartogenin sodium 通过结合纤维蛋白 A，阻断其与转录因子核心结合因子 β 亚基 (CBFβ) 的作用，并调节 CBFβ-RUNX1 转录程序来诱导软骨形成。此外，Kartogenin sodium 能促进肌腱-骨连接处 (TBJ) 的伤口愈合，因其能刺激胶原蛋白合成。广泛应用于再生医学中的无细胞疗法，Kartogenin sodium 用于软骨再生及保护、腱骨愈合、伤口愈合与肢体发育等方面，同时对骨关节炎 (OA) 的研究也颇具价值。

Nitrated unsaturated fatty acids, such as 10- and 12-nitrolinoleate , cholesteryl nitrolinoleate, and nitrohydroxylinoleate, represent a new class of endogenous lipid-derived signalling molecules. LNO2 isomers serve as potent endogenous ligands for PPARγ and can also decompose or be metabolized to release nitric oxide. 9-Nitrooleate is one of two regioisomers of nitrooleate, the other being 10-nitrooleate (OA-NO2; used for the mixture of isomers), which are formed by nitration of oleic acid in approximately equal proportions in vivo. Peroxynitrite, acidified nitrite, and myeloperoxidase in the presence of H2O2 and nitrite, all mediate the nitration of oleic acid. OA-NO2 is found in human plasma as the free acid and esterified in phospholipids at concentrations of 619 ± 52 nM and 302 ± 369 nM, respectively. OA-NO2 activates PPARγ approximately 7-fold at a concentration of 1 μM and effectively promotes differentiation 3T3-L1 preadipocytes to adipocytes at 3 μM.

Dihydroprehelminthosporol is a strongly phytotoxic metabolite, it exhibits cytotoxicity towards two human cancer cell lines, A549 and SK-OA-3.

PF-4693627 is an effective and selective microsomal prostaglandin E synthase-1 inhibitor (IC50=3 nM). It is used for the treatment of inflammation caused by osteoarthritis (OA) and rheumatoid arthritis (RA).

α-Glucosidase-IN-3是一种针对α-葡萄糖苷酶(IC50=1.28 µM)和α-淀粉酶(IC50=3.8 µM)的齐墩果酸肟酯衍生物。

NF157 significantly decreases the expression of metalloproteinase (MMP)-3, MMP-13, which can be used in the treatment of osteoarthritis (OA). NF157 is a highly selective nanomolar P2Y11 antagonist (pKi: 7.35). The IC50s are 463 nM, 1811 µM, 170 µM for P2Y

Cathepsin K inhibitor3 是一种高选择性的cathepsin K 抑制剂，其IC50值为 0.5 nM。Cathepsin K inhibitor3 具有良好的药代动力学特征，可用于骨关节炎 (OA) 疾病的研究。

OA-Br-1 是口服活性的PTP1B选择性抑制剂，IC50值为7.08 μM。它能够诱导细胞凋亡 (apoptosis) 并且具有广谱的抗癌细胞增殖活性。OA-Br-1 通过PTP1B PI3K AKT 信号通路在体内外对抗乳腺癌。

Yohimbic acid hydrate，一种Yohimbine的两性脱甲基衍生物，具有血管舒张效果，且在骨关节炎（OA）研究中展现出潜在应用价值。