Arthritis is an inflammatory disease of the joints, including the synovium, cartilage, bone, and supporting tissues. It is the leading cause of disability in the US and there are over 100 different types of the disease. The most common types of arthritis are osteoarthritis, rheumatoid arthritis and gout.
Damage to cartilage can lead to the degenerative condition called osteoarthritis. Contributing factors to this may include ageing, obesity, diabetes, injury or inflammatory diseases. The main symptoms of osteoarthritis are pain, stiffness and loss of mobility and function in the joints.
Rheumatoid arthritis is a condition concerning the immune system attacking the body's own tissues. Cytokinespromote the pathogenesis of the condition by maintaining chronic inflammation and driving the degradation of adjacent joint tissue. Macrophages, mast cells, T and B cells accumulate in the synovium which becomes inflamed and infiltrates the surrounding cartilage. This promotes articular destruction, which is mediated by osteoclasts, chondrocytes and synovial fibroblasts. In addition, new blood vessels are created by angiogenesisto supply the hypoxic joint with nutrients.
Arthritis is a debilitating condition which can cause sufferers a great deal of pain. This may be alleviated by certain medications or, in extreme cases, joint replacement surgery.
|Cat. No.||Product Name||CAS No.||Information|
A selective p38 MAPK inhibitor; inhibits IL-1 beta induction of p38 MAPK in primary human chondrocytes with IC50 of 1 uM; inhibits LPS-stimulated serum levels of TNFalpha in normal rats with mean ED50 of 3.99 mg/kg.
An orally bioavailable, selective, non-covalent and reversible BTK inhibitor with IC50 of 2-9 nM; has demonstrated efficacy in pre-clinical autoimmune disease models and is being developed for the treatment of rheumatoid arthritis and lupus, with future development for other autoimmune indications.
A potent, highly selective BTK inhibitor for the treatment of various autoimmune disorders.
AVL-292 besylate (Spebrutinib, CC-292) is a highly selective, covalent Btk inhibitor with IC50 of <1 nM; also less potently inhibits Yes, c-Src, Brk, Lyn, and Fyn with IC50s of 723 nM, 1.729 uM, 2.43 uM, 4.4 uM, and 7.15 uM, rspectively; shows anti-inflammatory activity in the collagen-induced arthritis model of autoimmune disease; also prevents NRG- and EGF-dependent growth factor-driven resistance to lapatinib in HER2(+) breast cancer cells.
Adavivint (SM-04690, SM 04690, SM04690) is a novel small molecule Wnt pathway inhibitor with EC50 of 3 nM in vitro; induces hMSC differentiation into mature, functional chondrocytes and decreases cartilage catabolic marker levels; significantly improves Osteoarthritis Research Society International (OARSI) histology scores and biomarkers in a rodent OA model.
CCX-354 (GSK-2941266, CCX354-C, CCX354) is a potent, selective, orally-available CCR1 antagonist for the treatment of inflammatory diseases such as rheumatoid arthritis (RA).
AK106-001616 (AK 106-001616) is a potent and selective inhibitor of cytosolic phospholipase A2 (cPLA2) with IC50 of 3.8 nM (human cPLA2 enzyme); also inhibited rat cPLA2 with IC50 of 4.3 nM, shows no significant activity against human iPLA2, bovine sPLA2 IB and PAF-AH (>10,000 fold selectivity); suppressed the release of AA from Ca2+ ionophore A23187-stimulated rat RBL-2H3 cells (IC50=5.5 nM), also suppressed the production of PGE2 by LPS-stimulated human PBMCs (IC50=5.1 nM) and the production of LTB4 by Ca2+ ionophore A23187-stimulated RBL-2H3 cells (IC50=2.6 nM); demonstrates in vivo efficacy for inflammation, neuropathic pain, and pulmonary fibrosis.
CR6086 (CR-6086) is a potent, selective prostaglandin E2 receptor 4 (EP4) antagonist with Ki of 16.6 nM (hEP4 receptor), inhibits PGE2-stimulated cAMP production with IC50 of 22 nM; reduces key cytokine players of RA (IL-6 and VEGF expression in macrophages, IL-23 release from dendritic cells, IL-17 release from Th17 cells) in models of human immune cells in culture; significantly improves all features of arthritis: severity, histology, inflammation and pain in CIA models of RA in rats and mice; CR6086 is better than the selective COX-2 inhibitor rofecoxib and at least as effective as the JAK inhibitor tofacitinib.
AZD-9567 is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.
AZD-9567 monohydrate is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.
No.1378 West Wenyi Road, Yuhang District, HangZhou, Zhejiang, China