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Cat. No. Product Name CAS No. Information
PC-63143

AZD-7594

1196509-60-0

AZD-7594 (AZ-13189620) is a potent, nonsteroidal, selective glucocorticoid receptor modulator (SGRM) with binding IC50 of 0.9 nM, shows no affinity for AR, PR, MR and ERα/β; demonstrates cell potentcy with IC50 of 55 nM (repression of AP-1 dependent transcription), inhibits LPS-stimulated TNF-α production in human PBMC with IC50 0.43 nM; potently inhibits lung edema in a rat model of allergic airway inflammation with inhaled EC50 of 130 uM/Kg.

Asthma

Phase 2 Clinical

PC-61687

AZD 2098

566203-88-1

AZD2098 is a potent, selective, orally bioavailable CCR4 receptor antagonist with pIC50 of 7.8 for hCCR4, pIC50 of 8.0 for rCCR4; shows no significant activity against a panel of chemokine receptors (CXCR1, CXCR2, CCR1, CCR2b, CCR5, CCR7, CCR8; inactive at 10 uM); inhibits Th2 cell CCL22 driven chemotaxis in 0.3% HSA with pIC50 of 6.3; exhibits anti-inflammatory effects in Brown-Norway rats sensitized to ovalbumin.

Asthma

Phase 1 Clinical

PC-61379

Gefapixant

1015787-98-0

Gefapixant (AF-219, MK-7264) is an orally active, small molecule antagonist of P2X3-containing receptor with IC50 of 30 nM (hP2X3 homotrimer) and 100-250 nM (hP2X2/3 heterotrimer); displays no inhibitory impact on any non-P2X3 subunit containing receptors (IC50 >10,000 nM at recombinant homotrimeric hP2X1, hP2X2, hP2X4, rP2X5 and hP2X7 channels); markedly and significantly reduced objective cough frequency in clinical trials.

Asthma

Phase 2 Clinical

PC-60705

MIV-247

1352817-76-5

MIV-247 (MIV247) is a potent, selective, orally active inhibitor of cathepsin S with Ki of 2.1 nM (human cathepsin S); displays high selectivity (>200-fold) overs other related cathepsins, inhibits mouse and cynomolgus monkey cathepsin S with Ki of 4.5 and 7.2 nM, respectively; attenuates mechanical allodynia alone, and also enhances the effect of gabapentin and pregabalin without increasing side effects in mouse model of neuropathic pain.

Asthma

Discontinued

PC-60220

RPL-554

298680-25-8

RPL-554 (LS-193855, RPL554) is a potent, orally available, dual PDE3/PDE4 inhibitor with IC50 of 0.4 nM and 1479 nM, respectively; inhibits LPS-induced TNFα release from human monocytes with IC50 of 0.52 uM, and proliferation of human mononuclear cells to phytohemagglutinin (IC50=0.46 uM); significantly inhibits eosinophil recruitment following antigen challenge in ovalbumin-sensitized guinea pigs (10mg/kg).

Asthma

Phase 2 Clinical

PC-35719

Valategrast hydrochloride

828271-96-1 Valategrast hydrochloride is a potent, α4β1 (VLA-4) and α4β7 dual antagonist.

Asthma

Discontinued

PC-35718

Valategrast

220847-86-9 Valategrast is a potent, α4β1 (VLA-4) and α4β7 dual antagonist.

Asthma

Discontinued

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