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Cat. No. Product Name CAS No. Information
PC-50005

AQX 1125 acetate

782487-29-0

A sepecific, orally bioavailable SHIP1 activator with no effect on functional androgen, oestrogen, oestrogen-related receptor α, glucocorticoid, mineralocorticoid and progesterone receptor at 30 uM; inhibits the pAkt (S473) in MOLT-4 cells, and inhibits cytokine release in mixed splenocytes; significantly decreases β-hexosaminidase release in mouse BMMCs; inhibits chemotaxis in human mononuclear cells (EC50=0.26 uM); suppresses leukocyte accumulation and inflammatory mediator release in rodent models of pulmonary inflammation and allergy.

COPD

Phase 2 Clinical

PC-50004

AQX 1125

782487-28-9

AQX 1125 (Rosiptor) is a specific, orally bioavailable SHIP1 activator with no effect on functional androgen, oestrogen, oestrogen-related receptor α, glucocorticoid, mineralocorticoid and progesterone receptor at 30 uM; inhibits the pAkt (S473) in MOLT-4 cells, and inhibits cytokine release in mixed splenocytes; significantly decreases β-hexosaminidase release in mouse BMMCs; inhibits chemotaxis in human mononuclear cells (EC50=0.26 uM); suppresses leukocyte accumulation and inflammatory mediator release in rodent models of pulmonary inflammation and allergy.

COPD

Phase 2 Clinical

PC-60474

BAY85-8501

1161921-82-9

BAY 85-8501 (BAY85-8501) is a potent, selective human neutrophil elastase (HNE) inhibitor with IC50 of 65 pM; displays no significant inhibition toward 21 related serine proteases (>30 uM); demonstrates completely prevented the development of lung injury and subsequent inflammation in vivo.

COPD

Phase 2 Clinical

PC-60297

AZD-7986

1802148-05-5

AZD-7986(INS-1007, AZD7986) is a highly potent, reversible, and selective DPP1 inhibitor with enzyme and cell pIC50 of 8.4; shows excellent selectivity over other cathepsins, including cathepsins S, L, B, K, D, E, Z, H, and G; inhibits activation of all three NSPs (NE, Pr3, and CatG) with pIC50 of 7 in human primary bone marrow-derived CD34+ neutrophil progenitor cells; exhibits suitable human PK properties and is a clinical candidate for COPD.

COPD

Phase 1 Clinical

PC-45643

GSK-2269557

1254036-71-9

GSK-2269557 is a highly potent and selective inhibitor of PI3Kδ (pKi=9.9); displays >1000 fold selectivity versus other PI3K isoforms; inhibits both IFNγ and IL-2 production in a concentration-dependent manner, with pIC50 values of 8.2 and 8.1, respectively, in a human lung parenchyma assay; shows activity in rat acute OVA model of Th2-driven lung inflammation (ED50=67ug/kg).

COPD

Phase 2 Clinical

PC-63395

JNJ-49095397

1220626-82-3 JNJ-49095397 (RV-568) is a specific narrow-spectrum kinase inhibitor that inhibits a selected set of kinases involved in COPD inflammation with IC50 of 5, 40 and 52 nM for p38α, p38γ and HCK, respectively; shows potent anti-inflammatory effects in monocytes and macrophages, demonstrates synergistic interaction in poly I:C-stimulated BEAS-2B cells and in the cigarette smoke model combined with corticosteroid.

COPD

Phase 2 Clinical

PC-63284

AZD-7624

1095004-78-6 AZD-7624 is a potent, selective, inhaled p38α MAPK inhibitor with pIC50 of 10.0, displays 15-fold selectivity for p38α over p38β MAPK and >10,000-fold selectivity over p38γ and p38δ MAPK; inhibits LPS-induced TNF-α and IL-6 release in human alveolar macrophages pIC50 of 9.2 and 8.8, respectively; shows potential for prevention of exacerbations in COPD.

COPD

Phase 2 Discontinued

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