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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-70272

Zaprinast

37762-06-4

Zaprinast (M&B 22948) is a potent, cGMP-specific phosphodiesterase inhibitor with IC50 of 0.5-0.76 and 0.15 uM for PDE5 and PDE6 respectively, also is an agonist for GPR35 (EC50=16/840 nM for rat/human GPR35); weakly inhibits PDE9, PDE10, and PDE11 with IC50 of 10-30 uM; enhances the vasodilatory effects of nitric oxide in a range of vascular tissues by prolonging the cGMP-mediated activation of cGMP-dependent protein kinase; also reduces cellular 2HG levels by inhibiting the upstream enzyme glutaminase (GLS), reverses histone hypermethylation and soft-agar growth of IDH1-mutant cells.

Asthma

Discontinued

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-35978

Gemilukast

1232861-58-3 Gemilukast (ONO-6950, ONO6950) is a potent, orally active, dual CysLT1 and CysLT2 antagonist with IC50 of 1.7 and 25 nM against human CysLT1 and human CysLT2, respectively; antagonized intracellular calcium signaling via human and guinea pig CysLT1 and CysLT2 receptors with IC50 values of 1.7 and 25 nM, respectively (human receptors) and 6.3 and 8.2 nM, respectively (guinea pig receptors); attenuated CysLT1-mediated bronchoconstriction and airway vascular hyperpermeability induced by LTD4 in normal guinea pigs (1 or 0.3 mg/kg, p.o.), strongly inhibited this asthmatic response to the level attained by combination therapy with montelukast and BayCysLT2RA.

Asthma

Phase 2 Discontinued

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