Asthma|Inhibitors Agonists Modulators Antagonists|HmoBio.com

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Asthma is a common chronic inflammatory disease of the respiratory system that affects approximately 22 million people in US. It has been classified as a complex genetic condition that is determined by the interaction of numerous genes along with environmental factors.

Asthma can be characterized by hyper-reactivity of the airways and the propensity of airways to constrict in response to various stimuli. This leads to symptoms such as shortness of breath, chest tightening, coughing and wheezing. Triggers of asthma 'attacks' include common colds, exercise, allergens (irritants such as smoke, fumes and dust, along with pollutants).

Normal versus asthmatic bronchiole

Cytokine signaling contributes greatly to asthma and the associated airway obstruction. Cytokines such as IL-4 cause the secretion of mucus and the onset of allergic inflammatory responses including the development of T helper cells. There are also numerous structural changes that occur in asthmatic airways and collectively lead to 'remodeling'. These include deposition of matrix proteoglycan and collagen in the submucosa, epithelial mucus metaplasia and a proliferation of microvessels and nerves.

Treatment for asthma includes bronchodilator therapy or anti-inflammatory drugs, particularly corticosteroid inhalation. Corticosteroids act by blocking the immune reaction to an allergen, decreasing inflammation by inhibiting cells such as mast cells, eosinophils and basophils.

Cat. No.	Product Name	CAS No.	Information
H8763	Remibrutinib	1787294-07-8	Remibrutinib is a potent and orally active bruton tyrosine kinase (BTK) inhibitor with an IC50 value of 1 nM. Remibrutinib inhibits BTK activity with an IC50 value of 0.023 μM in blood. Remibrutinib has the potential for Chronic urticaria (CU) treatment.
H7076	RV-1729	1293915-42-0	RV-1729 is a potent, selective PI3Kδ inhibitor with IC50 of 12 nM, 2-fold selectivity for PI3Kδ relative to PI3Kγ and 16-fold over PI3Kα; inhibits PMA-induced peroxide production in U937 cells and phosphorylation of Akt in MCP1-stimulated THP1 cells with IC50 of 1.1 and 46 nM; significantly inhibits allergen-induced responses in murine models of asthma and COPD.
H6432	IPL-576092	202415-99-4	A novel orally active, anti-inflammatory compound that inhibits leukocyte infiltration and changes in lung function in response to allergen challenge; significantly attenuates characteristics of asthmatic response.
H5859	GW3965 hydrochloride	405911-17-3	A potent, selective, orally active LXR agonist that recruits the steroid receptor coactivator 1 to human LXRα in a cell-free ligand-sensing assay with an EC50 of 125 nM; acts as a full agonist on hLXRα and hLXRβ in cell-based reporter gene assays with EC50 of 190 and 30 nM, respectively; increases expression of ABCA1 in the small intestine and peripheral macrophages in C57BL/6 mice at 10 mg/kg.
H5858	GW3965	405911-09-3	A potent, selective, orally active LXR agonist that recruits the steroid receptor coactivator 1 to human LXRα in a cell-free ligand-sensing assay with an EC50 of 125 nM; acts as a full agonist on hLXRα and hLXRβ in cell-based reporter gene assays with EC50 of 190 and 30 nM, respectively; increases expression of ABCA1 in the small intestine and peripheral macrophages in C57BL/6 mice at 10 mg/kg.
H5765	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.
H5418	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.
H5410	Tofimilast	185954-27-2	Tofimilast (CP-325366) is a potent, selective PDE4 inhibitor with IC50 of 23, 13 and 13 nM for PDE4A, PDE4B, and PDE4D, respectively; shows weakly or no inhibition for PDE4C, and no activity for PDE1, PDE2, PDE3, PDE5, PDE6, and PDE7; increases cAMP levels in PGE1-stimulated U937 cells with an EC50 of 230 nM, inhibits human monocyte PDE mediated cAMP catabolism with an IC50 of 67 nM and LPS stimulated human monocyte TNFα release with an IC50 of 59 nM; shows low oral bioavailability and no emesis-associated behaviors in the ferret emesis model.
H5403	RPL-554	298680-25-8	RPL-554 (Ensifentrine,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).
H5402	Rolipram	61413-54-5	A potent, selective inhibitor of phosphodiesterases PDE4 with IC50 of 3 nM, 130 nM and 240 nM for PDE4A, PDE4B, and PDE4D, respectively; increases phosphorylation of CREB in U937 cells in a dose-dependent fashion, dose-dependently inhibits the IFN-gamma-stimulated phosphorylation of p38 MAPK with IC50 of 290 nM; inhibits TNF production, attenuates carrageenan-induced paw inflammation in mice.

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