osteoarthritis

oxepinac is an effective and well-tolerated compound for the treatment of painful osteoarthritis. oxepinac has no teratogenic effect on mouse and rabbit fetuses in animal experiments.

Furprofen is a non-steroidal anti-inflammatory agent that inhibits prostate (PGE) synthesis and is used in the study of rheumatoid arthritis and osteoarthritis.

ADL-5747 (ADL-5747 (free base)) (free base) is a delta opioid receptor agonist used in the treatment of neurological disorders, skin and musculoskeletal disorders, and may be used in the study of postherpetic neuralgia, knee osteoarthritis and pain.

Flurbiprofen (dl-Flurbiprofen) is an anti-inflammatory analgesic and antipyretic of the phenylalkynoic acid series. It has been shown to reduce bone resorption in periodontal disease by inhibiting CARBONIC ANHYDRASE.

Valdecoxib (SC 65872) is a prescription drug used in the treatment of osteoarthritis, rheumatoid arthritis, and painful menstruation and menstrual symptoms. It is classified as a nonsteroidal anti-inflammatory drug, or NSAID, and should not be taken by anyone allergic to these types of medications.

Glucosamine hydrochloride (Chitosamine hydrochloride) is commonly used as a treatment for osteoarthritis, although its acceptance as a medical therapy varies.

Fenbufen (Lederfen) is a non-steroidal anti-inflammatory drug used primarily to treat inflammation in osteoarthritis, ankylosing spondylitis, and tendinitis. It can also be used to relieve backaches, sprains, and fractures. Fenbufen is available as a capsule or tablet sold with the brand names Cepal, Cinopal, Cybufen, Lederfen, and Reugast. Fenbufen acts by preventing cyclooxygenase from producing prostaglandins which can cause inflammation.

Parecoxib (SC 69124) is an effective and selective COX-2 inhibitor.

Strontium ranelate (S12911), a strontium (II) salt of the ranelic acid, is a medication for osteoporosis. Studies indicate it can also slow the course of osteoarthritis of the knee. The drug is unusual in that it both increases deposition of new bone by osteoblasts and reduces the resorption of bone by osteoclasts. It is therefore promoted as a dual action bone agent (DABA) indicated for use in the treatment of severe osteoporosis.

Celecoxib (SC 58635) is a Nonsteroidal Anti-inflammatory Drug. The mechanism of action of celecoxib is as a Cyclooxygenase Inhibitor.

Aceclofenac (Preservex) is a non-steroidal anti-inflammatory drug (NSAID) with marked anti-inflammatory and analgesic properties.

Tenoxicam (Tilcotil), an antiinflammatory agent with analgesic and antipyretic properties, is used to treat osteoarthritis and control acute pain.

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

PG-116800 (PG-530742) is a matrix metalloproteinase (MMP) inhibitor. PG-116800 can be used in studies about the treatment of osteoarthritis.

HALOFUGINONE LACTATE is a halogenated derivative of febrifugine, a natural quinazolinone-containing compound found in the Chinese herb D. febrifuga.Halofuginone inhibits prolyl-tRNA synthetase in an ATP-dependent manner with a Ki of 18.3 nM. Halofuginone is a specific inhibitor of type-I collagen synthesis and attenuates osteoarthritis (OA) by inhibition of TGF-β activity

Enpp-1-IN-16 is an inhibitor targeting ENPP1 with potential anti-cancer activity.Enpp-1-IN-16 can be used to study insulin resistance in relation to type II diabetes mellitus and various ENPP1-mediated diseases in the chondrocalcinosis and osteoarthritis classes.

Halofuginone specifically inhibits collagen type I gene expression and matrix metalloproteinase 2 (MMP-2) gene expression, which may result in the suppression of angiogenesis, tumor stromal cell development, and tumor cell growth. Halofuginone Hydrobromide is the hydrobromide salt of halofuginone, a semisynthetic quinazolinone alkaloid anticoccidial derived from the plant Dichroa febrifuga, with antifibrotic and potential antineoplastic activities. These effects appear to be due to halofuginone-mediated inhibition of the collagen type I and MMP-2 promoters. Collagen type I and MMP-2 play important roles in fibroproliferative diseases.

S-Adenosyl-L-methionine (Ademetionine) is an intermediate metabolite of methionine,for treatment of primary biliary cirrhosis and major depressive disorder.

Etofenamate is a non-steroidal anti-inflammatory drug (NSAID) used for the treatment of joint and muscular pain.

Campesterol ((24R)-5-Ergosten-3β-ol) is a plant sterol with cholesterol lowering and anticarcinogenic effects, it and other plant sterols often decrease LDL cholesterol levels overall. Campesterol has anti-inflammatory effect, it inhibits several pro-inflammatory and matrix degradation mediators typically involved in osteoarthritis- induced cartilage degradation, also sometimes used to treat some specific prostate conditions.

S-(5'-Adenosyl)-L-methionine tosylate (SAMe) is a ubiquitous methyl donor involved in a wide variety of biological reactions, including those mediated by DNA and protein methyltransferases [1]. S-(5'-Adenosyl)-L-methionine tosylate (SAMe) is a stable salt of SAM that is included in nutritional supplements for oral use [2]. S-(5'-Adenosyl)-L-methionine tosylate (SAMe) reportedly ameliorates depression, pain associated with osteoarthritis and fibromyalgia, and liver toxicity [3].

Lumiracoxib (Prexige) is a novel, selective COX-2 inhibitor with IC50 and Ki of 0.14 μM and 0.06 μM, exhibits 515-fold selectivity over COX-1. Phase 4.

Oxaceprol (N-Acetyl-L-hydroxyproline) is an established therapeutic agent for osteoarthritis.

Gefapixant (AF219) is a P2X3 receptor (P2X3R) antagonist with IC50 of ~30 nM at recombinant hP2X3 homotrimers and 100-250 nM at hP2X2 3 heterotrimeric receptors.

MMP13-IN-3 is >1000 selective over other MMPs. MMP13-IN-3 is an effective, selective, and orally active MMP-13 inhibitor (IC50=1 nM) for the potential treatment of osteoarthritis.

SGK1-IN-4 is a selective inhibitor of SGK1 and can be used in studies about osteoarthritis.

Licofelone (ML-3000) is a dual COX LOX inhibitor potentially for treating osteoarthritis, acting as both an analgesic and anti-inflammatory. By inhibiting 5-LOX, it may reduce the gastrointestinal toxicity associated with other non-steroidal anti-inflammatory drugs, which only inhibit COX (cyclooxygenase).

amyloid P-IN-1 can be used in studies about diseases with depletion of serum amyloid P components such as Alzheimer's disease, amyloidosis, osteoarthritis, and type 2 diabetes mellitus.

Zaloglanstat (ISC-27864) is a potent inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1). It is utilized in the research of various conditions, including asthma, osteoarthritis, rheumatoid arthritis, acute or chronic pain, and neurodegenerative diseases.

Anemonin is a furanone dimer found in the Buttercup (Ranunculaceae) family. Anemonin has been shown to regulate tyrosinase-related proteins and mRNA in human melanocytes and may be useful in attenuting osteoarthritis progression.

S-Adenosyl-DL-Methionine (Ademetionine) is a ubiquitous methyl donor involved in a wide variety of biological reactions, including those mediated by DNA and protein methyltransferases. SAM reportedly ameliorates depression, pain associated with osteoarthritis and fibromyalgia, and liver toxicity.

CL-82198, a selective MMP-13 inhibitor, serves as a pharmacological intervention to halt the progression of osteoarthritis (OA). Its mechanism of action involves binding to the S1’ pocket of MMP-13, ensuring its selectivity and preventing inhibition of other MMPs.

Cindunistat( PHA-728669F, PF-00572986, PHA-84250, SD-6010, and SC-084250) is a potent and oral selective iNOS inhibitor which is expected to be used in patients with symptomatic osteoarthritis of the knee.

Gefapixant citrate is an orally active P2X3 receptor (P2X3R) antagonist that acts on human homologous recombinant hP2X3 (IC50: ~30 nM) and hP2X2 3 (IC50: 100-200 nM). Gefapixant citrate can be used to study chronic cough and knee osteoarthritis.

ADAMTS-5-IN-2 is a potent inhibitor of ADAMTS-5, exhibiting an IC50 of 0.71 µM, and holds potential for osteoarthritis research.

Kartogenin (KGN) sodium acts as an inducer of chondrogenic tissue formation (EC 50: 100 nM). It promotes chondrogenesis by binding to fibrin A, disrupting its interaction with the transcription factor core binding factor beta subunit (CBFβ), and modulating the CBFβ-RUNX1 transcriptional program. Additionally, Kartogenin sodium aids tendon-bone junction (TBJ) wound healing by stimulating collagen synthesis. It is extensively utilized in cell-free therapies for cartilage regeneration and protection, tendon-bone healing, wound healing, and limb development. The compound is also vital for cartilage repair, coordinating limb development, and osteoarthritis (OA) research [1] [2] [3] [4].

S-Allylmercaptocysteine HCl is an organosulfur compound isolated from aged garlic with anti-inflammatory, antioxidant, anticancer, and antitumor activities.S-Allylmercaptocysteine HCl inhibits inflammation in COPD and targets Nrf2 in osteoarthritis therapy through the NOX4 NF-kappaB pathway. Targeting Nrf2.

Diacerein (Fisiodar) is a prodrug which is metabolized to rhein. It is currently approved in France for the treatment of osteoarthritis although the use of diacerein is restricted due to the side effects including sevre diarrhea [L780]. Diacerein is under investigation for the treatment of Insulin Resistance, Diabetes Mellitus (Type 2), and Diabetes-Related Complications.

Anemarsaponin E1, isolated from the Guizhi-Shaoyao-Zhimu decoction (GSZD), is used in research for rheumatoid arthritis (RA), gout, osteoarthritis, and related conditions [1].

Chondroitin sulfate sodium, a class of glycosaminoglyphans, is extensively utilized in managing osteoarthritis. It mitigates mediators of inflammation and apoptosis while diminishing the production of inflammatory cytokines, iNOS, and MMPs [1] [2] [3] [4].

EP4 receptor antagonist 3 is a highly potent and specific inhibitor of the EP4 receptor, intended for research purposes in studying EP4 receptor-mediated diseases, including acute and chronic pain, osteoarthritis, rheumatoid arthritis, and cancer.

MMP13-IN-5 (compound 13m) is a potent and selective inhibitor of MMP-2 and MMP-13, with IC50 values of 3.6 μM for MMP-2 and 14.6 μM for MMP-13, implicated in osteoarthritis (OA) pathology [1].

OGT-IN-2 is a potent O-GlcNAc transferase (OGT) inhibitor. OGT-IN-2 inhibits sOGT and ncOGT with IC50 values of 30 μM and 53 μM, respectively[1]. OGT-IN-2 can be used for the research of articular diseases[1].

Tedalinab is an effective and selective cannabinoid receptor 2 agonist. Tedalinab has the potential for neuropathic pain and osteoarthritis treatment. Tedalinab has >4700-fold functional selectivity for CB2 over CB1.

Cathepsin K inhibitor 2 is a potent inhibitor of cathepsin K, a cysteine protease expressed under the control of the CTSK gene, which is closely related to osteoporosis and hydrolyses collagen. Cathepsin K inhibitor 2 has shown potential in osteoarthritis.

CMC2.24 (TRB-N0224) is an orally active tricarbonylmethane agent that demonstrates effectiveness in inhibiting Ras activation and the downstream effector ERK1 2 pathway, thus effectively combating pancreatic tumor formation in mice. Additionally, CMC2.24 exerts potent inhibitory effects on zinc-dependent MMPs, with IC50s ranging from 2.0-69 μM. Furthermore, CMC2.24 aids in alleviating the progression of osteoarthritis by restoring cartilage homeostasis and inhibiting chondrocyte apoptosis through the NF-κB HIF-2α axis[1][2][3].

Specnuezhenide (Nuezhenide) is isolated from the fruit of Ligustrum lucidum. It inhibits NF-κB and wnt β-catenin signaling, thereby suppressing IL-1β-induced chondrocyte inflammation. It exerts anti-inflammatory effects in a rat model of osteoarthritis (OA).

Fursultiamine (Alinamin F) is a disulfide derivative of thiamine, or an allithiamine. It has potential uses in the treatment of vitamin B1 deficiency.