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Cat. No. Product Name CAS No. Information
PC-63295

BMS-986195

1912445-55-6

BMS-986195 (BMS986195) is a novel potent, selective, covalent, irreversible inhibitor of Bruton’s tyrosine kinase (BTK), >5,000-fold selective over all kinases outside of the Tec family, and selectivity ranges 9- to 1010-fold within the Tec family; potently inhibits antigen-dependent interleukin-6 production, CD86 expression and proliferation in B cells (IC50<1 nM); demonstrates robust efficacy in murine models of RA including CIA and CAIA, protecting against clinically evident disease, histologic joint damage and bone mineral density loss.

Rheumatoid Arthritis

Phase 1 Clinical

PC-60536

Poseltinib

1353552-97-2

Poseltinib (HM-71224, LY-3337641) is a potent and selective, covalent inhibitor of Btk with IC50 of 1.95 nM; also inhibits BMX, TEC, TXK, EGFR in biochemical sense (IC50=0.3-2.5 nM); effectively inhibits the phosphorylation of Btk and PLCγ2, and inhibits expression of CD40, CD69, and CD86 by activated primary human B cells with IC50 of 4.2, 4.2, and 7.7 nM, respectively; inhibited the production of TNF-α, IL-6, and IL-1β by human monocytes, and osteoclast formation by human monocytes; ameliorates arthritis in a mouse model.

Rheumatoid Arthritis

Phase 1 Clinical

PC-60504

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.

Rheumatoid Arthritis

Phase 2 Clinical

PC-60422

BMS-986142

1643368-58-4

BMS-986142 is a potent, selective and reversible BTK inhibitor with IC50 of 0.5 nM; displays 20-60-fold selectivity over Tec family kinases, >10,000-fold selectivity over JAK2; potently inhibits signaling and functional end points, including calcium flux (IC50=9 nM), production of cytokines, proliferation, and surface expression of CD86 (IC50=3-4 nM); potently inhibits BCR-stimulated expression of CD69 on B cells in human whole blood with IC50 of 90 nM; exhibits excellent in vivo properties and efficacy, and a very desirable tolerability and safety profile.

Rheumatoid Arthritis

Phase 2 Clinical

PC-60072

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.

Rheumatoid Arthritis

Phase 2 Clinical

PC-60071

AZD-9567

1893415-00-3

AZD-9567 (AZD9567) is a potent, selective, non-steroidal and orally available selective glucocorticoid receptor modulator (SGRM) for treatment of rheumatoid arthritis.

Rheumatoid Arthritis

Phase 2 Clinical

PC-45653

Upadacitinib

1310726-60-3

Upadacitinib (ABT-494) is a potent and selective JAK1 inhibitor with celluar IC50 of 8 nM, biochemical IC50 of 40 nM; displays 74-fold and 50-fold selectivity over JAK2 and JAK3, respectively; a second-generation JAK inhibitor in development for rheumatoid arthritis.

Rheumatoid Arthritis

Phase 3 Clinical

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