pruritus

Bepotastine Besilate (TAU 284) is a non-sedating and selective H1 receptor antagonist (pIC50: 5.7).

Bepotastine (Bepotastine free base) free base is a histamine 1 (H1) receptor antagonis.

Hydroxyzine Pamoate (Bobsule) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Diphenhydramine hydrochloride (DPH) is a histamine H1 antagonist used as an antitussive and antiemetic. It is also used for pruritus and dermatoses, for hypersensitivity reactions, as an antiparkinson, a hypnotic, and as an ingredient in common cold preparations.

Hydroxyzine dihydrochloride (Hydroxyzine 2HCl) is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Dexchlorpheniramine Maleate, a histamine receptor antagonist, is used to treat urticaria, allergic rhinitis, allergic conjunctivitis and pruritus.

Delgocitinib (JTE-052) is a JAK inhibitor and a specific JAK1/2/3/Tyk2 inhibitor (IC50=2.6-58 nM) that blocks multiple cytokine signaling pathways and inhibits pruritus, used for research on inflammatory and autoimmune diseases.

S1647 is a dual inhibitor targeting both ASBT and SOAT. It is utilized in research focused on intrahepatic cholestasis, cholestatic pruritus, and constipation.

Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of the MrgX2 receptor, with an IC50 range of 0.042-2.5 nM. It blocks downstream G protein signaling and β-arrestin recruitment, inhibiting Mrgx2 receptor-mediated calcium influx and cell degranulation. Mrgx2 antagonist-3 shows potential for research in inflammation-associated diseases and pruritus, such as chronic urticaria and allergic asthma.

MrgprX2-IN-1 (Compound 2-10) is a selective antagonist of the Mas-related G protein-coupled receptor X2 (MRGPRX2). It functions by inhibiting mast cell degranulation and the release of inflammatory mediators mediated by MRGPRX2, thereby blocking non-IgE-dependent immune responses. MrgprX2-IN-1 holds potential for research into pseudo-allergic reactions, chronic pruritus, and inflammatory diseases.

MrgprX2-IN-2 (Compound example 12) is a selective antagonist of the Mas-related G protein-coupled receptor X2 (MRGPRX2). It works by inhibiting MRGPRX2-mediated mast cell degranulation and the release of inflammatory mediators, thus blocking non-IgE-dependent immune responses. MrgprX2-IN-2 shows potential for research in the areas of pseudo-allergic reactions, chronic pruritus, and inflammatory diseases.

MRGPRX4 modulator-3 (Compound 1C) is an allosteric negative modulator of MAS-related G-protein coupled receptor X4 (MRGPRX4). It significantly inhibits the activation response induced by Nateglinide (an orthosteric agonist), with an IC50 of 337 nM. MRGPRX4 modulator-3 is applicable in studies related to chronic itching, particularly cholestatic pruritus, and pain.

Dimethindene maleate (SU 6518) is a histamine H1 antagonist and can be used in studies about the treatment of hypersensitivity reactions, pruritus and rhinitis.

GRI918013 is a compound that selectively and competitively inhibits the autocrine motility factor (ATX/NPP2), thereby suppressing tumor cell invasion and metastasis. GRI918013 binds competitively to the active site of ATX, preventing the entry of lipid substrates such as lysophosphatidylcholine (LPC). This reduces the ATX-catalyzed hydrolysis of LPC to form lysophosphatidic acid (LPA), thereby inhibiting cell invasion and metastasis associated with the ATX-LPA axis. GRI918013 exhibits an inhibitory effect on the ATX-catalyzed hydrolysis of the LPL substrate FS-3, with an IC50 of 31.42 nM and a Ki of 12.98 nM. GRI918013 can serve as a tool for studying invasion and metastasis in cancers such as melanoma, and is also suitable for research on ATX-LPA axis-related diseases, including fibrotic diseases, neuropathic pain, and cholestatic pruritus.

Ilunocitinib is a non-selective and orally active Janus kinase (JAK) inhibitor for the control of pruritus and atopic dermatitis caused by atopic dermatitis in dogs.

Asimadoline hydrochloride (EMD-61753 hydrochloride) is a κ-opioid receptor agonist potentially for the treatment of pruritus. Asimadoline hydrochloride has also been shown to be used in the treatment of irritable bowel syndrome.

Nav1.8-IN-2 (compound 35A) is a potent Nav1.8 inhibitor (IC50: 0.4 nM) and can be utilized in research on pain disorders, cough, and both acute and chronic pruritus.

Bepotastine tosylate is a selective, orally active second-generation histamine H1 receptor antagonist that exhibits an inhibitory effect on histamine-mediated upregulation of nerve growth factor (NGF) expression. conjunctivitis and urticaria/pruritus.

Halobetasol propionate (BMY-30056) is the propionate salt form of halobetasol, a synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictor activities. Halobetasol, a topical steroid, diffuses across cell membranes to interact with cytoplasmic corticosteroid receptors located in both the dermal and intradermal cells, thereby activating gene expression of anti-inflammatory proteins mediated via corticosteroid receptor response element. Specifically, this agent induces phospholipase A2 inhibitory proteins, which inhibit the release of arachidonic acid, thereby inhibiting the biosynthesis of potent mediators of inflammation, such as prostaglandins and leukotrienes. As a result, halobetasol reduces edema, erythema, and pruritus through its cutaneous effects on vascular dilation and permeability.

GR 89696 free base is a potent and highly selective κ2 opioid receptor agonist, offering potential benefits in pruritus prevention.

Nemolizumab (CIM331) is a humanized monoclonal antibody targeting the human interleukin-31 receptor A, inhibiting IL-31 binding and subsequent signal transduction. It is useful for studying atopic dermatitis with pruritus.

Hydroxyzine-D4 dihydrochloride is a deuterated compound of Hydroxyzine dihydrochloride. Hydroxyzine dihydrochloride (T2200) has a CAS number of 2192-20-3. Hydroxyzine hydrochloride is a histamine H1 receptor antagonist that is effective in the treatment of chronic urticaria, dermatitis, and histamine-mediated pruritus. Unlike its major metabolite CETIRIZINE, it does cause drowsiness. It is also effective as an antiemetic, for relief of anxiety and tension, and as a sedative.

Diphenhydramine Hydrochloride (Standard) is the standard substance of Diphenhydramine Hydrochloride, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Diphenhydramine hydrochloride (DPH) is a histamine H1 antagonist used as an antitussive and antiemetic. It is also used for pruritus and dermatoses, for hypersensitivity reactions, as an antiparkinson, a hypnotic, and as an ingredient in common cold preparations.

Halobetasol propionate (Standard) is the standard substance of Halobetasol propionate, and it is applicable for quantitative analysis, quality control, and related research in biochemical experiments. Halobetasol propionate (BMY-30056) is the propionate salt form of halobetasol, a synthetic corticosteroid with anti-inflammatory, antipruritic, and vasoconstrictor activities. Halobetasol, a topical steroid, diffuses across cell membranes to interact with cytoplasmic corticosteroid receptors located in both the dermal and intradermal cells, thereby activating gene expression of anti-inflammatory proteins mediated via corticosteroid receptor response element. Specifically, this agent induces phospholipase A2 inhibitory proteins, which inhibit the release of arachidonic acid, thereby inhibiting the biosynthesis of potent mediators of inflammation, such as prostaglandins and leukotrienes. As a result, halobetasol reduces edema, erythema, and pruritus through its cutaneous effects on vascular dilation and permeability.