rheumatic diseases

Butibufen (FF-106) is an orally active non-steroidal anti-inflammatory compound, a potential cyclooxygenase inhibitor with analgesic and antipyretic activity, and inhibits urea synthesis.Butibufen has been used in the study of rheumatic diseases.

Colchicine (Colcin) is a natural product that is an inhibitor of microtubule polymerization (IC50=3 nM) and blocks microtubule polymerization by binding to microtubule proteins. Colchicine can be used in the treatment of ventilation and rheumatic diseases.

Azathioprine (BW 57-322), an immunosuppressive agent, inhibits purine synthesis and GTP-binding protein Rac1 activation.

1. Bullatine A, a diterpenoid alkaloid of the genus Aconitum, possesses anti-rheumatic, anti-inflammatory and anti-nociceptive effects, may be used for the treatment of neurodegenerative diseases such as arthritis.

6,7,4'-Trihydroxyflavanone possesses various pharmacological activities, including anti-rheumatic, anti-ischemic, anti-inflammatory, anti-osteoclastogenic, and protective effects against METH-induced deactivation of T cells. 6,7,4'-Trihydroxyflavanone can be used for studies about the treatment of METH-addicts suffering from neurodegenerative diseases.

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.

Salazopyridazine is an antibacterial agent that inhibits ulcerative colitis. salazopyridazine can be used in the study of rheumatic diseases.

Piroxicam cinnamate (Cinnoxicam), a cyclooxygenase (COX) inhibitor with anti-inflammatory properties, is used to study inflammatory degenerative bone and joint diseases, rheumatic diseases, and varicocele-related oligospermia.

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

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

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 is an anti-inflammatory, antipyretic and analgesic drug used in the treatment of various rheumatic diseases. It is well tolerated clinically and pathologically and has a reliable anti-inflammatory effect.

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.

Tiaprofenic acid (Acido tiaprofenico) is a non-steroidal anti-inflammatory drug used to treat pain, especially arthritic pain.