synovial

Rapanone (2,5-Dihydroxy-3-tridecyl-[1,4]benzoquinone) 是一种具有广泛生物活性的天然苯醌，如抗肿瘤、抗氧化、抗炎、抗菌和抗寄生虫活性。它还是选择性人滑膜 PLA2抑制剂，IC50值为 2.6 μM。

NDMC101 是有效的破骨细胞形成抑制剂，通过下调 NFATc1 调控基因表达抑制破骨细胞分化。它与 DPP4底物相似，通过抑制DPP4抑制早期 T 细胞激活。它能够用于骨疾病的研究，如类风湿关节炎、滑膜炎等。

Hyaluronic acid (hyaluronan) 由玉米发酵得到，是由二糖的重复单元组成的生物聚合物，应用领域广泛。

SXT1596 is a novel SS18-SSX TLE1 interaction inhibitor. SXT1596 reduces cell viability and reactivates EGR1 expression in synovial sarcoma.

SB-505124 hydrochloride (SB505124 hydrochloride) 是一种可口服且具有选择性和高效性的 TGF-βI 型受体(ALK4，ALK5，ALK7) 抑制剂，对 ALK4，ALK5 的IC50值分别为 129 nM 和 47 nM。SB-505124 hydrochloride 抑制滑膜外植体产生 IL-6，通过降低 Il17a 和 Rorc 基因表达以及 IL-17 蛋白的产生减少小鼠 Th17 分化。SB-505124 hydrochloride 可用于研究结直肠癌。

Fce 21258 is used to stimulate the adenylate cyclase of synovial fluid macrophages.

Potent BRD9 degrader. Selectively binds BRD9 and elicits near complete degradation of BRD9 at nanomolar concentrations. Inhibits growth of synovial sarcoma cells in vitro and tumor progression in a synovial sarcoma xenograft mouse model.

Resolvin D5是一种从DHA中提取的氧化脂质介质，具有抗炎作用，在LPS刺激的THP-1细胞中通过ERK-NF-κB信号通路抑制IL-6和CCL5的产生。

Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-1509 (1995).2. Morisseau, C., Newman, J.W., Dowdy, D.L., et al. Inhibition of microsomal epoxide hydrolases by ureas, amides, and amines. Chem. Res. Toxicol. 14(4), 409-415 (2001).3. Jain, M.K., Ghomashchi, F., Yu, B.Z., et al. Fatty acid amides: scooting mode-based discovery of tight-binding competitive inhibitors of secreted phospholipases A2. J. Med. Chem. 35(19), 3584-3586 (1992). Elaidamide is a fatty acid amide that has been found in the cerebrospinal fluid of sleep-deprived cats.1 It inhibits rat microsomal epoxide hydrolase (mEH; Ki = 70 nM).2 Elaidamide also inhibits porcine pancreatic and human synovial phospholipase A2 (PLA2).3 In vivo, elaidamide (10 mg/animal) induces physiological sleep in rats.1 References1. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-1509 (1995).2. Morisseau, C., Newman, J.W., Dowdy, D.L., et al. Inhibition of microsomal epoxide hydrolases by ureas, amides, and amines. Chem. Res. Toxicol. 14(4), 409-415 (2001).3. Jain, M.K., Ghomashchi, F., Yu, B.Z., et al. Fatty acid amides: scooting mode-based discovery of tight-binding competitive inhibitors of secreted phospholipases A2. J. Med. Chem. 35(19), 3584-3586 (1992).

S-methyl-KE-298 是 KE-298 的活性代谢物。KE-298 抑制类风湿关节炎滑膜细胞产生基质金属蛋白酶。

Oxaprozin potassium 是具有口服活性的COX 的抑制剂，其对人血小板COX-1 的IC50值为 2.2 μM，对 IL-1 刺激的人类滑膜细胞COX-2的IC50值为 36 μM。Oxaprozin potassium 诱导细胞凋亡。Oxaprozin potassium 还抑制 NF-κB 活化，Oxaprozin potassium 介导的Akt IKK NF-κB 通路抑制有助于其抗炎特性。

AS1940477 is p38 MAPK inhibitor. AS1940477 inhibited the enzymatic activity of recombinant p38α and β isoforms but showed no effect against other 100 protein kinases including p38γ and δ isoforms. In human peripheral blood mononuclear cells, AS1940477 inhibited lipopolysaccharide (LPS)- or phytohemagglutinin A (PHA)-induced production of proinflammatory cytokines, including TNFα, IL-1β, and IL-6 at low concentrations (LPS TNFα, IC(50)=0.45n M; PHA TNFα, IC(50)=0.40 nM). In addition, equivalent concentrations of AS1940477 that inhibited cytokine production also inhibited TNFα- and IL-1 β-induced production of IL-6, PGE(2), and MMP-3 in human synovial stromal cells. AS1940477 was also found to potently inhibit TNF production in whole blood (IC(50)=12 nM) and effectively inhibited TNFα production induced by systemically administered LPS in rats at less than 0.1mg kg (ED(50)=0.053 mg kg) with an anti-inflammatory effect lasting for 20h after oral administration. Overall, this stu......

AGG-523 is an aggrecanase specific inhibitor that has been shown to attenuate increases in synovial fluid ARG-aggrecan levels following surgically-induced joint instability in the rat MT model. Pharmacologic inhibition of aggrecanase activity in humans using AGG-523 may be an effective treatment for slowing cartilage degradation following joint injury.

FPTI is an inhibitor against SYT-SSX1 fusion protein in synovial sarcoma which down-regulates SYT-SSX1 and modulates its downstream target genes.

BE-16627B is a novel metalloproteinase (MP) inhibitor isolated from Streptomyces sp. BE16627B selectively inhibited MPs such as human stromelysin and 92 kD gelatinase. After the cells were cultured with BE16627B for 5 days, BE16627B inhibited MP activity in the primary culture supernatants from synovial cells in a dose-dependent fashion without showing apparent cytotoxicity or affecting the production and secretion of MPs. Its IC50 for active collagenolysis before activation by trypsin was 25 microM.

AB05831, also known as 2-Acetamido-1,2-dideoxynojirimycin, is a highly potent and specific inhibitor of beta-hexosaminidase. N-Acetyl-3-hexosaminidase (HEX) is a member of lysosomal hydrolases, which catalyzes hydrolysis of terminal, non-reducing N-acetyl-|3-D-glucosamine (GlcNAc) andN-acetyl-(3-D-galactosamine (GalNAc) residues in glycoproteins, gan-gliosides, and glycosaminoglycans (GAGs). HEX, released by chondrocytes into the extracellular compartment, promotes cartilage matrix degradation. Osteoarthritis patients have increased HEX activity in synovial fluid.

Tabituximab barzuxetan (OTSA101-DTPA-90Y) 是一种放射免疫偶联物，由靶向FZD-10 (OTSA-101)的人源化单克隆抗体组成，并用钇 90 标记。Tabituximab barzuxetan 具有抗肿瘤活性。Tabituximab barzuxetan 可用于滑膜肉瘤的研究。

TNO211为具备生物活性的肽，主要研究对象是基质金属蛋白酶（MMP），一类能够降解多种细胞外基质蛋白并调控诸多生物活性分子的肽链内切酶家族。MMP在细胞表面受体裂解、凋亡配体释放及趋化因子 细胞因子失活等过程中起作用，同时与细胞增殖、迁移（粘附 分散）、分化、血管生成、细胞凋亡及宿主防御等生物行为密切相关。TNO211可靶向MMP-2、8、12、13和14，包含MMP特定可裂解的Gly-Leu键，并具有EDANS DABCYL荧光标记，其荧光检测在监测内皮细胞培养基和患者滑液中的MMP活性方面表现出高灵敏度。吸光度 电磁场测量参数为340 490 nm。

HAP-1为针对滑膜细胞的转导肽，可促进蛋白质复合物在人类及兔子滑膜细胞中的特异性内吞作用。当HAP-1与抗菌肽(KLAK)2融合时，形成促进细胞凋亡的肽DP2。

1,2-Dinonadecanoyl-sn-glycero-3-PC (DNPC), a saturated phospholipid, serves as a standard in quantifying phosphatidylcholines in human synovial fluid and has been utilized in researching lipid bilayer phase transition dynamics.

PDE4-IN-18 (compound 1l) 作为PDE4抑制剂 (IC50=1.55 μM),展现了显著的抗炎效果.该化合物通过减少免疫细胞的过度浸润和肠膜形成,以及显著降低滑膜组织内如TNF-α和IL-6等促炎细胞因子的mRNA水平,有效抑制炎症.PDE4-IN-18 主要用于类风湿性关节炎和银屑病的相关研究.

Masticadienolic acid is a specific competitive inhibitor of secreted phospholipase A2, it not only protects the active site histidine from alkylation but also inhibits the action of secreted from pancreas, synovial fluid, and bee venom. Masticadienolic ac

(2R,3R)-2,3,4-Trihydroxybutanoic acid，亦名赤藓酸，为一种广泛分布于人体多种生物体液中的天然有机酸，包括眼房水、尿液、血浆、脑脊液及滑液。该化合物在健康的成人与儿童体内均能检出，其生成过程涉及 GlcNAc 的氧化反应。