Asthma

β2AR agonist 7 is a MABA with both muscarinic acetylcholine M3 receptor antagonistic activity and β2-adrenergic receptor agonistic activity, with a K_i of 1.75 nM for hM₃ and an EC₅₀ of 0.054 nM for hβ₂. β2AR agonist 7 binds to the M3 muscarinic receptor with high affinity and long-acting kinetic characteristics. β2AR agonist 7 induces smooth muscle relaxation and acts as a bronchoprotective agent against acute bronchoconstriction. β2AR agonist 7 can be used in the research of asthma and chronic obstructive pulmonary disease.

MY-1250 is a histamine release inhibitor. MY-1250 is the major active metabolite of Repirinast (HY-109544). MY-1250 stimulates adenylate cyclase to increase intracellular cyclic adenosine monophosphate levels, reduce intracellular ATP levels, inhibit antigen-induced intracellular calcium store mobilization, and induce phosphorylation of the 78 kDa protein. MY-1250 inhibits antigen- and phospholipase A₂-induced release of histamine and slow-reacting substance of anaphylaxis from mast cells, lung tissue fragments and basophils. MY-1250 can be used in research related to allergic diseases and bronchial asthma.

QX008N is a humanized IgG1 monoclonal antibody and also a TSLP inhibitor with a K_D value of 0.0175 nM. QX008N blocks TSLP-induced signaling pathways by inhibiting the interaction of TSLP-TSLPR-IL-7Rα. QX008N reduces eosinophil and IgE levels, improves pulmonary function, blocks TSLP-induced inflammation, and enhances the inhibitory effect on inflammatory mediators when administered in combination with anti-IL-4R antibodies. QX008N is applicable to relevant research on asthma.

GS-1160-180 is a PAF receptor antagonist. GS-1160-180 competes with PAF for receptor binding, with no activity against collagen or adenosine diphosphate-induced platelet aggregation. GS-1160-180 can be used for research on asthma, anaphylactic shock, gastric ulceration, and transplant rejection.

Altrakincept is a recombinant hIL-4 receptor and IL-4 neutralizer. Altrakincept neutralizes endogenous IL-4, and prevents the decline of pulmonary function and acute asthma exacerbations after abrupt withdrawal of inhaled glucocorticoids.

BI 894416 is a spleen tyrosine kinase (SYK) inhibitor. BI 894416 has a deuterium-labeled derivative that can be used as an internal standard for bioanalytical studies. BI 894416 is applicable to the research of severe asthma.

AZ-11665362 is a CRTh2 (DP2) receptor antagonist with an IC₅₀ of 2.6 nM. AZ-11665362 shows weak activity against aldose reductase, serotonin transporter, CYP 2C19, and CYP 2C9. AZ-11665362 lacks measurable inhibitory activity against COX-1 and COX-2. AZ-11665362 can be used for the research of asthma, and other inflammatory diseases.

KDM4C-IN-2 is a histone lysine demethylase KDM4C (JMJD2C) inhibitor with an IC₅₀ of 147 μM and a K_i of 51 μM. KDM4C-IN-2 can be used for the research of cancer, such as prostate and breast cancer.

PDE4B-IN-7 is a PDE-4B inhibitor with an IC₅₀ of 160 nM. PDE4B-IN-7 can form a firm and stable binding with the active site of PDE-4B. PDE4B-IN-7 inhibits acetylcholine-induced bronchospasm in guinea pigs. PDE4B-IN-7 exerts activity against susceptible Gram-positive and Gram-negative bacterial strains. PDE4B-IN-7 can be used for the researches of asthma and bacterial agent.

S-Petasin is a phosphodiesterase (PDE) inhibitor with IC₅₀ values of 25.5 μM and 17.5 μM for PDE3 and PDE4, respectively. S-Petasin inhibits cholesterol side-chain cleavage enzyme, 11β-hydroxylase, PPAR-γ, and iNOS induction at RNA and protein levels. S-Petasin induces apoptosis, activates caspases, cleaves PARP, modulates mitochondrial membrane permeability, and regulates BCL2/BAX, p53, Bcl-XL, MMP-2, MMP-9, p21, CDK4, and cyclin D1 expression. S-Petasin reduces inflammatory cell accumulation, cytokine and IgE levels, and enhances serum IgG2a levels. S-Petasin relaxes isolated sensitized guinea pig trachealis and exhibits gastrointestinal anti-spasmodic activity. S-Petasin reduces tonsillitis severity and asthmatic attack frequency. S-Petasin can be used for the research of prostate cancer, obesity, melanoma, allergic asthma, asthma, and peritonitis.

Scrophenoside A (compound 1) is a phenyl glycoside found in the stems of Picrorhiza scrophulariiflora.Scrophenoside A exhibits anti-asthma activity.Scrophenoside A can be used for the research of asthma.

Frititorine A is a steroidal alkaloid that exists in the bulbs of Fritillaria tortifolia. Frititorine A exerts a relaxing effect on acetylcholine-induced tracheal contraction. Frititorine A can be used in asthma-related research.

SF-3-030 is a potent, selective and non-ATP competitive ERK1/2 inhibitor. SF-3-030 selectively induces apoptosis in melanoma cells containing mutated BRaf and constitutively active ERK1/2 signalling. SF-3-030 mitigates multiple features of asthma in a murine model of asthma. SF-3-030 can be used for the research of asthma and melanomasup.

SM-15178 is a potent, orally active and selective leukotriene B₄ (LTB₄) receptor antagonist with an IC₅₀ of 0.30 μM. SM-15178 attenuates LTB₄ (HY-107608)-induced neutrophil accumulation in mouse skin and bronchoconstriction in guinea pigs. SM-15178 emonstrates significant anti-inflammatory efficacy across multiple animal models of inflammation. SM-15178 can be used for the research of chronic inflammatory diseases such as inflammatory bowel disease, psoriasis, and asthma.

CK-571 is a potent and selective inhibitor of smooth muscle myosin-2 (SMM), with an IC₅₀ value of 86 nM. CK-571 exhibits IC₅₀ values for cardiac muscle myosin (CMM), skeletal muscle myosin (SKM), and non-muscle myosin-2A (NMM-2A) of 2.3, 42, and 0.58 μM, respectively. CK-571 can be used for research on asthma, chronic obstructive pulmonary disease, and other smooth muscle-related diseases.

α5β1 integrin-IN-1 is a potent and selective α5β1 integrin inhibitor with an IC₅₀ value of approximately 0.4 nM (pIC₅₀ = 9.4 M). α5β1 integrin-IN-1 disrupts the interaction between α5β1 integrin and fibronectin, thereby blocking smooth muscle tension transmission and α5β1 integrin-mediated cell adhesion. α5β1 integrin-IN-1 can be used in the research of asthma and allergic asthma.

E 6080 is an orally active and selective 5-lipoxygenase (5-LOX) inhibitor with an IC₅₀ of 0.2 μM in rat basophilic leukemia cell. E 6080 shows potent inhibitory effects on the release of leukotrienes. E 6080 inhibits the bronchospasm induced by antigen (ovalbumin) inhalation in sensitized conscious guinea pigs. E 6080 can be used for the study of asthma.

TAC 363 is a selective tachykinin NK-2 receptor antagonist. TAC 363 shows a rightward shift in the contractile response curve induced by Neurokinin A (HY-P0197) with a pA₂ of 9.82. TAC 363 has a weak antagonistic effect on NK-1 receptors. TAC 363 can inhibit Neurokinin A-induced bronchoconstriction in guinea pigs with an ED₅₀ of 0.3 mg/kg. TAC 363 can be used for the research of bronchial asthma.

ONO 2050297 (Compound 19) is a selective Cysteinyl leukotriene (CysLT) antagonist with IC₅₀s of 17  and 0.87 nM for CysLT1 and CysLT2, respectively. ONO 2050297 can be used for bronchial asthma research.

Butixocort propionate (JO 1222), a corticosteroid, is a potent Glucocorticoid Receptor agonist. Butixocort propionate exhibits anti-inflammatory activity. Butixocort propionate can be used for the researches of inflammation, immunology and metabolic disease, such as asthma and arthritis.