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You are here:Home-Research Areas-Inflammation/Autoimmune Disease-Rheumatoid Arthritis

Request The Product List ofRheumatoid Arthritis Rheumatoid Arthritis

    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.

Illustrations of a healthy joint and joints in the four stages of rheumatoid arthritis. The stages include synovitis, in which the synovial membrane is inflamed and thickened and the bones and cartilage are gradually eroded; pannus, in which there is extensive cartilage loss and exposed and pitted bones; fibrous ankylosis, in which the space between bones in the joint is invaded by fibrous connective tissue; and bony ankylosis, in which the bones are fused.

     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
GY02934

SB-242235

193746-75-7

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.

GY02565

Fenebrutinib

1434048-34-6

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.

GY02520

Evobrutinib

1415823-73-2

A potent, highly selective BTK inhibitor for the treatment of various autoimmune disorders.

GY02431

AVL-292 besylate

1360053-81-1

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.

GY07024

Adavivint

1467093-03-3

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.

GY10248

CCX-354

1010073-75-2

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).

GY10578

AK106-001616

590416-75-4

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.

GY06713

CR6086

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.

GY06567

AZD-9567

1893415-00-3

AZD-9567 is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.

GY06566

AZD-9567 monohydrate

1893415-64-9

AZD-9567 monohydrate is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.

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