rheumatic diseases

Azathioprine (BW 57-322) 是一种免疫抑制剂。

Butibufen (FF-106) 是一种具有口服活性的非甾体抗炎化合物，是潜在的环氧合酶抑制剂，具有止痛和解热活性，抑制尿素合成。Butibufen 可用于研究风湿性疾病。

Colchicine (Colcin) 属于天然产物，是一种微管聚合的抑制剂 (IC50=3 nM)，通过与微管蛋白结合来阻断微管的聚合。Colchicine 可以被用于治疗通风和风湿病。

Bullatine A 是一种有效的 P2X7拮抗剂，可抑制 ATP 诱导的细胞凋亡和 P2X 受体介导的炎症反应。它是乌头属的二萜生物碱，能缓解过敏反应，具有抗风湿、抗炎和抗伤害作用，可用于治疗关节炎等神经退行性疾病。

6,7,4'-Trihydroxyflavanone 具有多种药理活性，包括抗风湿、抗缺血、抗炎、抗破骨细胞和对 METH 诱导的 T 细胞失活的保护作用。 6,7,4'-三羟基黄烷酮可用于研究治疗患有神经退行性疾病的 METH 成瘾者。

3-Acetamidocoumarin, a compound significant in biology and medicine, exhibits physiological effects and is utilized in treating various conditions, including burns, brucellosis-rheumatic diseases, and cancer.

Dexamethasone acetate monohydrate is an adrenocortical steroid. It is used in the treatment of many conditions, including rheumatic problems, a number of skin diseases, asthma, severe allergies, chronic obstructive lung disease, brain swelling, croup, and antibiotics

Tiaprofenic acid D3 is a deuterium-labeled Tiaprofenic acid. Tiaprofenic acid is a nonsteroidal anti-inflammatory drug and treatment of rheumatic diseases.

Salazopyridazine 是一种抗菌剂，可以抑制溃疡性结肠炎。Salazopyridazine 能够用于研究风湿病。

Piroxicam cinnamate (Cinnoxicam) 是一种环氧合酶 (COX) 抑制剂，表现出抗炎作用。Piroxicam cinnamate 能够用于研究炎症退行性骨关节疾病，风湿性疾病和精索静脉曲张 (VC) 相关性少弱精子症。

KZR-616, a first-in-class inhibitor of the immunoproteasome, selectively targets the LMP7 (IC50: 39/57 nM=hLMP7/mLMP7) and LMP2 (IC50: 131/179 nM=hLMP7/mLMP7) subunits of the immunoproteasome. KZR-616 has the potential for the research of multiple autoimmune diseases[1][2]. KZR-616 also inhibits MECL-1 subunit (IC50=623 nM) and constitutive proteasome β5 subunit (IC50=688 nM). KZR-616 maintains LMP7 and LMP2 selective inhibition in MOLT-4 cells. KZR-616 (250 nM) shows a comparable cytokine inhibition profile peripheral blood mononuclear cells (PBMC)[1].KZR-616 is an immunoproteasome-selective inhibitor identified based on the optimization of ONX-0914 and PR-924 [3]. KZR-616 (5 mg/kg; i.v.; dosing was repeated on days 6, 8, 11, and 13) shows efficacy in the anticollagen antibody induced arthritis (CAIA) model[1]. [1]. Johnson HWB, et al. Required Immunoproteasome Subunit Inhibition Profile for Anti-Inflammatory Efficacy and Clinical Candidate KZR-616 ((2 S,3 R)- N-(( S)-3-(Cyclopent-1-en-1-yl)-1-(( R)-2-methyloxiran-2-yl)-1-oxopropan-2-yl)-3-hydroxy-3-(4-methoxyphenyl)-2-(( S)-2-(2-morpholinoacetamido)propanamido)propenamide). J Med Chem. 2018 Dec 27;61(24):11127-11143. [2]. Muchamuel T, et al. FRI0296 Kzr-616, a selective inhibitor of the immunoproteasome, blocks the disease progression in multiple models of systemic lupus erythematosus (SLE). Annals of the Rheumatic Diseases 2018;77:685. [3]. Xi J, et al. Immunoproteasome-selective inhibitors: An overview of recent developments as potential drugs for hematologic malignancies and autoimmune diseases. Eur J Med Chem. 2019;182:111646.

Pipebuzone 是一种抗炎、解热、镇痛药，用于治疗各种风湿性疾病。它在临床和病理上都具有良好的耐受性，并具有可靠的抗炎作用。

RO314724 is a HDAC inhibitor. RO314724 is also a a reversible, tightly binding, MMP inhibitor with a Ki of 26 nm. Matrix metalloproteinases (MMPs) belong to the key enzymes of the proteolytic destruction of cartilage matrix during chronic rheumatic diseases. Ro314724 displayed MMP-proteoglycanase inhibitory activity both in vitro and ex vivo and proved to be not harmful to the morphology, viability and proteoglycan biosynthesis of bovine articular cartilage explants.