mast cell

Ketotifen fumarate (HC 20511 fumarate) is a cycloheptathiophene blocker of histamine H1 receptors and release of inflammatory mediators.

Peptide from giant hornet Vespa orientalis that has biological effects similar to mast cell degranulating peptide from bee venom.

Mast Cell Degranulating Peptide HR-2 acetate from giant hornet Vespa orientalis that has biological effects similar to mast cell degranulating peptide from bee venom.

Mast cell degranulating peptide (28-49) is a bee venom depolarizer that enhances cGMP levels in cerebellum tablets of mice.

Chymase-IN-1 is a selective, orally active inhibitor of human mast cell chymase (IC50: 29 nM).

Eclazolast (RHC 2871) is a lipophilic anti-allergic compound that inhibits mediator release in a mast cell model.Eclazolast inhibits extracellular secretion by affecting only the direct processes associated with Fc(epsilon)RI in the cell.The effect of Eclazolast is highly dependent on the concentration of antigen that triggers the cell.

JNJ-10311795 (RWJ-355871) is a potent dual inhibitor of neutrophil elastase (Ki = 38 nM) and mast cell chymase (Ki = 2.3 nM) with significant anti-inflammatory activity, useful for studying pneumonia.

Salbutamol (Albuterol) stimulates beta2-adrenergic receptors in the lungs, thereby activating the enzyme adenylate cyclase that catalyzes the conversion of ATP to cyclic-3', 5'-adenosine monophosphate (cAMP). Salbutamol Sulfate is the sulfate salt of the short-acting sympathomimetic agent albuterol, a 1:1 racemic mixture of (R)-albuterol and (S)-albuterol with bronchodilator activity. Increased cAMP concentrations relax the bronchial smooth muscle, relieve bronchospasms, and reduce inflammatory cell mediator release, especially from mast cells. To a lesser extent, Salbutamol stimulates beta1-adrenergic receptors, thereby increasing the force and rate of myocardial contraction.

Olopatadine hydrochloride (ALO4943A) is an antihistamine with mast-cell stabilizing properties used as eye drops in the treatment of ALLERGIC CONJUNCTIVITIS.

Epinastine hydrochloride (WAL-801CL HCl) is an antihistamine and mast cell stabilizer that is used in eye drops to treat allergic conjunctivitis.

1-Heptanol (Heptan-1-ol) is a RIFM spice that is a cell membrane fluidizer and induces signaling to mast cells.1-Heptanol shows antiarrhythmic effects in atrial species of Langendorff perfused mouse hearts.1-Heptanol is a RIFM spice that is a cell membrane fluidizer and induces signaling to mast cells.1-Heptanol is a RIFM spice that is a RIFM spice and induces signaling to mast cells.

Rupatadine (UR-12592, rupatadine) is a potent and orally available dual antagonist of PAF and histamine H1 receptors with Ki values of 0.55 μM and 0.1 μM, respectively, which provides relief of allergic symptoms and anti-inflammatory properties, and is used in allergic rhinitis and chronic urticaria.

PKC ζ pseudosubstrate acetate is an inhibitor of protein kinase C (PKC) ζ; attached to cell permeabilisation Antennapedia domain vector peptide. Consists of amino acids 113 - 129 of PKC ζ pseudosubstrate domain linked by a disulphide bridge to the Antenna

Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.

Compound 48/80 trihydrochloride (C48/80 trihydrochloride) is a mixture of N-methyl-p-methoxyphenethylamine and formaldehyde produced via a condensation reaction. It acts as a mast cell degranulator and histamine releaser and inhibits phosphatidylinositol-specific phospholipase C activity in human platelets.

Evatanepag (CP-533536 free acid) is an EP2 receptor selective prostaglandin E2 (PGE2) agonist that induces local bone formation with EC50 of 0.3 nM.CP-533536 demonstrated the ability to heal fractures when administered locally as a single dose in rat models of fracture healing.

Lodoxamide tromethamine is a mast cell stabilizer with anti-allergic properties and can be used in studies about the treatment of asthma and allergic conjunctivitis.

Tazanolast, a selective mast-cell-stabilizing drug, inhibits the release of chemical mediators (histamine and leukotrienes) from mast cells, reduces inflammation, and is used in the treatment of allergic disorders, such as asthma and allergic rhinitis.

Timapiprant sodium inhibits mast cell activation of Th2 lymphocytes and eosinophils. Timapiprant sodium is a potent and selective D prostanoid receptor 2 antagonist. Timapiprant sodium potently displaces [3H] PGD2 from human recombinant DP2 (Ki=13 nM), ra

Quinotolast (FK021) is an orally active mast cell stabilizer with cytoprotective properties on the gastric mucosa. It exhibits both antiallergic and antiulcer functions.

Histamine glutarimide is a novel small molecule agent functioning as an inhibitor of glutaminyl-peptide cyclotransferase (QPCT), which targets key inflammatory processes including eosinophilic migration and mast cell degranulation, Histamine glutarimide has demonstrated significant anti-asthmatic effects in various preclinical animal models of allergic asthma.

GE1111 is an antagonist of the mas-related G protein-coupled receptor X2 (MRGPRX2), exhibiting an IC50 of 9.42 μM. It inhibits mast cell degranulation with an IC50 of 4.7 μM. In the C48 80-induced systemic allergic reaction model, GE1111 demonstrates both antiallergic and anti-inflammatory properties.

Z-3578 is a small molecule antagonist targeting the MrgX2 (Mas-related G protein-coupled receptor X2) with notable anti-pseudoallergic properties, exhibiting a KD value of 729 nM. It effectively inhibits mast cell degranulation induced by substance P (SP) and C48/80, with IC50 values of 4.90 µM and 6.18 µM, respectively, suppresses the release of β-hexosaminidase, and significantly reduces the release of histamine and TNF-α, as well as intracellular calcium flux. Additionally, in a mouse pseudoallergy model, Z-3578 significantly alleviates foot swelling, dye leakage, and reduces serum histamine levels, indicating a strong in vivo anti-allergic effect. Z-3578 presents as a promising lead compound in the field of anti-allergic treatments, particularly for pseudoallergic reactions.

Olopatadine, an antihistamine, as well as anticholinergic and mast cell stabilizer, is used for the treatment of itching associated with allergic conjunctivitis (eye allergies). There is also a potential for Olopatadine to treat steroid rebound (red skin