IL-4 Inhibitor

Epinastine hydrochloride (WAL801 hydrochloride) is a selective and orally active histamine H1 receptor antagonist, CD96/PVR inhibitor and mast cell stabilizer. Epinastine hydrochloride has high affinity for neuronal octopamine receptors in locusts (K_i = 2 nM) and honeybees (K_i = 1.1 nM). Epinastine hydrochloride inhibits TARC, IL-8, and IL-4. Epinastine hydrochloride activates anti-colon cancer immunity and inhibits Substance P (HY-P0201)-induced scratching behavior and increased vascular permeability. Epinastine hydrochloride can be used in the research of allergic diseases.

TSLP-IN-1 is a potent thymic stromal lymphopoietin (TSLP) inhibitor. TSLP-IN-1 disrupts TSLP-TSLPR protein-protein interaction, and downregulates IL-4 and IL-13. TSLP-IN-1 can be used for the research of inflammation diseases, such as skin disease, asthma, and allergies.

Ritlecitinib (PF-06651600) tosylate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib tosylate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib tosylate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).

Naphazoline (Naphthazoline) hydrochloride is a potent α-adrenergic receptor agonist. Naphazoline hydrochloride reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline hydrochloride reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline hydrochloride can be used for non-bacterial conjunctivitis research.

(±)-Praeruptorin A, a coumarin compound, is the main bioactive component in Peucedani Radix. As a calcium channel blocker, (±)-Praeruptorin A exhibits great antihypertensive effects. In addition, (±)-Praeruptorin A also has the effects of relaxing vascular smooth muscle, inhibiting airway inflammation and airway hyperresponsiveness. (±)-Praeruptorin A can be used for the research of allergic asthma, hypertension and other diseases.

Naphazoline (Naphthazoline) nitrate is an α-adrenergic receptor agonist. Naphazoline nitrate reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline nitrate reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline nitrate can be used for non-bacterial conjunctivitis research.

Patiromer is an orally active, selective and non-absorbable intestinal potassium (K⁺) polymer binder that reversibly binds potassium ions in exchange for calcium (Ca²⁺). Patiromer can rapidly and continuously reduce serum potassium levels, maintain a normal blood potassium state, and reduce serum aldosterone levels. Patiromer also increases fecal potassium excretion. Patiromer is mainly used in the study of hyperkalemia associated with diseases such as chronic kidney disease, diabetes, and heart failure, and is particularly suitable for improving renin-angiotensin-aldosterone system inhibitor (RAASi) therapy.

BP79 is a potent TSLP receptor inhibitor. BP79 disrupts TSLP-mediated ternary complex formation, blocks TSLPR-IL7Rα co-localization, binds and stabilizes TSLPR, and inhibits phosphorylated STAT3/6. BP79 suppresses immune cell infiltration, secretion of IL-13, IL-4. BP79 can be used for the research of inflammation diseases, such as atopic dermatitis, allergic asthma, and allergic rhinitis.

JAK1/2-IN-1 is a potent JAK1 and JAK2 inhibitor with IC₅₀ values of 0.4 nM and 8.1 nM, respectively. JAK1/2-IN-1 also inhibits IL-4 and IL-13 with IC₅₀s of 136.5 nM and 19.1 nM, respectively (WO2023244775A1; Example 33a).

Naphazoline (Naphthazoline) is a potent α-adrenergic receptor agonist. Naphazoline reduces vascular hyperpermeability and promotes vasoconstriction. Naphazoline reduces the levels of inflammatory factors (TNF-α, IL-1β and IL-6), cytokines (IFN-γ and IL-4), IgE, GMCSF, and NGF. Naphazoline can be used for non-bacterial conjunctivitis research.

Romilkimab (SAR156597) is a humanized IG antibody that specifically targets IL-4 and IL-13. Romilkimab can be used for the research of diffuse cutaneous systemic sclerosis.

TSLP modulator-1 (Compound 14O) is a potent TSLP signaling modulator. TSLP modulator-1 exhibits potent inhibition of CCL17 and IL-1β mRNA expression. TSLP modulator-1 attenuates the protein levels of IL-6, IL-4 and IL-13. TSLP modulator-1 significantly attenuates calcium influx. TSLP modulator-1 exerts anti-inflammatory effects. TSLP modulator-1 effectively alleviates pruritus and atopic dermatitis-like symptoms.

DPPE-PEG350 (16:0 PEG350 PE) is a CD1d lipid antagonist. DPPE-PEG350 blocks alpha-GalCer-dependent ERK tyrosine kinase phosphorylation in cells. DPPE-PEG350 inhibits cellular IL-4 and IFN-gamma production following alpha-GalCer stimulation. DPPE-PEG350 selectively antagonizes iNKT without affecting MHC class II-dependent OVA-specific Th2 responses. DPPE-PEG350 reduces MCP-1 and VCAM-1 protein expression and necrotic core formation in atherosclerotic lesions. DPPE-PEG350 can be used for research on asthma and atherosclerosis.

APG808 (PR001) is an anti-human IL-4Rα monoclonal antibody. APG808 binds to IL-4Rα, prevents IL-13Rα1/IL-4Rα heterodimer formation, and disrupts IL-13 and IL-4 mediated signaling. APG808 ablates Fc and complement effector functions. APG808 can be used for the research of chronic obstructive pulmonary disease, asthma, atopic dermatitis.

Ompekimig is an immunoglobulin monoclonal antibody that targets IL-4, IL-13, IL-33. Ompekimig shows potential for use in immune-mediated inflammatory diseases such as asthma and atopic dermatitis.

Gimvekibart is a humanized IgG4κ monoclonal antibody inhibitor targeting IL-4Ra/CD124. Gimvekibart can be used for inflammatory diseases like idiopathic pulmonary fibrosis (IPF) research.

NFAT Transcription Factor Regulator-1 is an IL-2 synthesis inhibitor with an IC₅₀ of 182 nM.

Anti-Rat IL-4 Antibody (OX-81) is an antibody inhibitor against rat IL-4. Anti-Rat IL-4 Antibody (OX-81) can specifically block the anti-inflammatory effect of IL-4. Anti-Rat IL-4 Antibody (OX-81) can be used for research on inflammation conditions such as experimental allergic encephalomyelitis (EAE).

PNRI-299 is a selective AP-1 transcription inhibitor with an IC₅₀ of 20 uM. PNRI-299 is a selective APE/Ref-1 inhibitor. PNRI-299 has no effect on NF-κB transcription or thioredoxin (up to 200 uM). PNRI-299 significantly reduces airway eosinophil infiltration, mucus hypersecretion, edema, and IL-4 levels in a mouse asthma model.

Ritlecitinib (PF-06651600) malonate is a highly selective, orally active, irreversible covalent JAK3 inhibitor (IC₅₀=33 nM) without inhibitory activity towards JAK1, JAK2, and TYK2 (IC₅₀ >10 μ M). Ritlecitinib malonate rapidly inactivates the JAK3 kinase, and blocks signaling and downstream STAT phosphorylation mediated by common gamma chain cytokines such as IL-2 and IL-15. Ritlecitinib malonate can inhibit Th1/Th17 cell differentiation and function, and effectively suppress preclinical animal models such as alopecia areata, adjuvant-induced arthritis (AIA), and experimental autoimmune encephalomyelitis (EAE).