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pruritus

" in MedChemExpress (MCE) Product Catalog:

50

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1

Biochemical Assay Reagents

2

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1

Inhibitory Antibodies

1

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6

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-129047
    Trypsin
    Maximum Cited Publications
    20 Publications Verification

    Ser/Thr Protease Protease Activated Receptor (PAR) Infection Inflammation/Immunology
    Trypsin is a serine protease enzyme, and hydrolyzes proteins at the carboxyl side of the Lysine or Arginine. Trypsin activates PAR2 and PAR4. Trypsin induces cell-to-cell membrane fusion in PDCoV infection by the interaction of S glycoprotein of PDCoV and pAPN. Trypsin also promotes cell proliferation and differentiation. Trypsin can be used in the research of wound healing and neurogenic inflammation .
    Trypsin
  • HY-129047A

    Ser/Thr Protease Protease Activated Receptor (PAR) Infection Inflammation/Immunology
    Trypsin MS grade is a serine protease enzyme, and hydrolyzes proteins at the carboxyl side of the Lysine or Arginine. Trypsin MS grade activates PAR2 and PAR4. Trypsin MS grade induces cell-to-cell membrane fusion in PDCoV infection by the interaction of S glycoprotein of PDCoV and pAPN. Trypsin MS grade also promotes cell proliferation and differentiation. Trypsin MS grade can be used in the research of wound healing and neurogenic inflammation .
    Trypsin (MS grade)
  • HY-76711

    Opioid Receptor Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight .
    Naltrexone
  • HY-17609
    Difelikefalin
    1 Publications Verification

    CR-845; FE-202845

    Opioid Receptor Neurological Disease Inflammation/Immunology
    Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
    Difelikefalin
  • HY-145551

    JAK Interleukin Related Inflammation/Immunology
    Atinvicitinib is an orally active and selective JAK1 inhibitor. Atinvicitinib blocks signaling of JAK1-dependent pruritogenic and pro-inflammatory cytokines, including those in the IL-31, IL-4, and IL-13 pathways. Atinvicitinib can be used for the researches of pruritus associated with allergic dermatitis and canine atopic dermatitis .
    Atinvicitinib
  • HY-P99301

    Anti-Canine IL31 Recombinant Antibody; CAN34D3-65; PF-06443537

    Interleukin Related Inflammation/Immunology
    Lokivetmab (Anti-Canine IL31 Recombinant Antibody) is an anti-canine IL-31 monoclonal antibody. Lokivetmab inhibits IL-31-mediated activation of pruritogenic signals in peripheral sensory neurons and reduces TH2-weighted inflammation. Lokivetmab demonstrates long-term efficacy in controlling pruritus and improving skin lesions in dogs with canine atopic dermatitis (CAD). Lokivetmab can be used for the research of atopic dermatitis (AD) in dogs .
    Lokivetmab
  • HY-N15721

    Trp-CA

    Orphan GPCR GLP Receptor Metabolic Disease
    Tryptophan-cholic acid (Trp-CA) is a microbial amino acid-conjugated bile acid that acts as an endogenous ligand and agonist (EC50=9.6 μM) for the orphan G protein-coupled receptor (GPCR) MRGPRE (Mas-related G protein-coupled receptor family member E). Tryptophan-cholic acid is orally effective but has poor oral absorption and does not cross the blood-brain barrier. Tryptophan-cholic acid promotes the secretion of glucagon-like peptide GLP-1, thereby improving glucose tolerance in diabetic mice. Tryptophan-cholic acid improves glucose tolerance, promotes insulin secretion, and alleviates high-fat diet-induced hepatic steatosis without causing pruritus side effects. Tryptophan-cholic acid is primarily used in research on type 2 diabetes (T2D) .
    Tryptophan-cholic acid
  • HY-141582

    N-Stearoyl phytosphingosine

    JNK NF-κB Interleukin Related TNF Receptor Inflammation/Immunology
    Ceramide 3 (N-Stearoyl phytosphingosine) is an orally active major component of intercellular lipids in the stratum corneum of the skin, and belongs to the ceramide family. Ceramide 3 inhibits c-jun and NF-κB activation induced by Histamine (HY-B1204), and suppresses the expression of IL-4 and TNF-α. Ceramide 3 inhibits scratching behavior and vascular permeability in mice, and exhibits antihistamine effects in guinea pig ileum. Ceramide 3 improves skin barrier function, reduces transepidermal water loss, erythema and the number of circulating epidermal cells, and accelerates barrier repair of irritated or dysfunctional skin .
    Ceramide 3
  • HY-A0015
    Bepotastine besilate
    1 Publications Verification

    Histamine Receptor Inflammation/Immunology Endocrinology
    Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
    Bepotastine besilate
  • HY-B1589A
    Carbinoxamine maleate salt
    1 Publications Verification

    Histamine Receptor Influenza Virus Infection Inflammation/Immunology
    Carbinoxamine maleate salt is a blood-brain barrier-permeable histamine H1 receptor antagonist. Carbinoxamine maleate salt blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. Carbinoxamine maleate salt inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. Carbinoxamine maleate salt can be used in research on allergic rhinitis, influenza, etc.
    Carbinoxamine maleate salt
  • HY-B1177

    Environmental Pollutants TRP Channel Parasite Infection
    Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus .
    Crotamiton
  • HY-132819

    LY-3411067

    JAK Others
    Ilunocitinib (compound 27) is a JAK inhibitor (extracted from patent WO2009114512A1) .
    Ilunocitinib
  • HY-I0021
    Bepotastine
    1 Publications Verification

    Histamine Receptor Inflammation/Immunology Endocrinology
    Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
    Bepotastine
  • HY-P1192

    Neurokinin Receptor Neurological Disease
    GR-73632 is a tachykinin NK1 receptor agonist. GR-73632 activates spinal NK1 receptors to induce scratching, biting and licking behaviors. GR-73632 activates peripheral NK1 receptors to trigger lacrimation in guinea pigs, and activates central NK1 receptors to induce repetitive hind paw tapping behavior in gerbils. GR-73632 is applicable to research related to pruritus .
    GR-73632
  • HY-107747

    Opioid Receptor Inflammation/Immunology
    GR 89696 is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus .
    GR 89696
  • HY-176446

    Mas-related G-protein-coupled Receptor (MRGPR) Inflammation/Immunology
    Mrgx2 antagonist-3 (Compound B-40) is a highly selective antagonist of MrgX2 receptor with an IC50 value of 0.042-2.5 nM. Mrgx2 antagonist-3 blocks downstream G protein signaling and β-Arrestin recruitment, thereby inhibiting MrgX2 receptor-mediated calcium influx and cellular degranulation. Mrgx2 antagonist-3 is promising for research of inflammation-related diseases and pruritus, such as chronic urticaria, allergic asthma .
    Mrgx2 antagonist-3
  • HY-76711S

    Isotope-Labeled Compounds Opioid Receptor Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Naltrexone-d4 is deuterium labeled Naltrexone (HY-76711). Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
    Naltrexone-d4
  • HY-153650

    Natriuretic Peptide Receptor (NPR) Others
    JS11 is an inhibitor for natriuretic polypeptide receptor 1 (Npr1) with an IC50 of 1.9 μM for hNpr1. JS11 ameliorates the pruritus in mouse models .
    JS11
  • HY-116691

    Hydrocortisone 17-propionate 21-acetate

    Glucocorticoid Receptor Neurological Disease Inflammation/Immunology
    Hydrocortisone aceponate (Hydrocortisone 17-propionate 21-acetate) is a diester-based topical glucocorticoid. Hydrocortisone aceponate alleviates symptoms such as erythema, dryness/desquamation, pruritus, epidermal exfoliation, and exudation/crusting. Hydrocortisone aceponate causes extremely few adverse reactions. Hydrocortisone aceponate is applicable to various dermatological disease studies .
    Hydrocortisone aceponate
  • HY-76711R

    Reference Standards Opioid Receptor Neurological Disease Metabolic Disease Inflammation/Immunology Cancer
    Naltrexone (Standard) is the analytical standard of Naltrexone (HY-76711). This product is intended for research and analytical applications. Naltrexone is an orally active, long-acting opioid receptor (opioid receptor) antagonist. Naltrexone blocks the euphoric effects of exogenous opioids and reduces alcohol craving by blocking opioid receptors (μ, κ, and δ) as well as opioid growth factor receptors. Low doses of Naltrexone are used to relieve chronic pain, treat inflammatory diseases and inhibit tumor growth, while high doses or continuous administration exert pro-inflammatory or pro-proliferative effects. Naltrexone relieves intractable pruritus caused by psoriasis, atopic dermatitis and other conditions, and its combination with Bupropion (HY-B0403) inhibits food craving, thereby reducing body weight.
    Naltrexone (Standard)
  • HY-17609S1

    CR-845-d5 hydrochloride; FE-202845-d5 hydrochloride

    Isotope-Labeled Compounds Opioid Receptor Neurological Disease Inflammation/Immunology
    Difelikefalin-d5 (CR-845-d5) hydrochloride is the deuterium labeled Difelikefalin (HY-17609). Difelikefalin (CR-845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
    Difelikefalin-d5 hydrochloride
  • HY-19704

    CT327; SNA-120

    Trk Receptor Inflammation/Immunology Cancer
    Pegcantratinib (CT327) is a potent and selective TRKA antagonist with activity against TRKB and TRKC. Pegcantratinib can be used for research of CYLD cutaneous syndrome (CCS) and inflammatory dermatoses, such as psoriasis and concomitant pruritus .
    Pegcantratinib
  • HY-160144S2

    (rac)-BMS-986322

    Drug Isomer Others
    (rac)-Lomedeucitinib ((rac)-BMS-986322) is the racemate of Lomedeucitinib. Lomedeucitinib (BMS-986322) is a tyrosine protein kinase (TYK2) inhibitor. Lomedeucitinib has anti-inflammatory activity and significant inhibitory effect on IFNα (IC50=0.047 μM) production downstream of IL-12/TYK2. Lomedeucitinib is indicated for the study of plaque psoriasis and pruritus .
    (rac)-Lomedeucitinib
  • HY-A0015A

    Histamine Receptor Inflammation/Immunology Endocrinology
    (Rac)-Bepotastine (besilate) is the isomer of Bepotastine (besilate) (HY-A0015), and can be used as an experimental control. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
    (Rac)-Bepotastine besilate
  • HY-176767

    Mas-related G-protein-coupled Receptor (MRGPR) Inflammation/Immunology
    MrgprX2-IN-1 (Compound 2-10) is a selective Mas-related G-protein coupled receptor X2 (MRGPRX2) antagonist. MrgprX2-IN-1 blocks IgE-independent immune responses by inhibiting MRGPRX2-mediated mast cell degranulation and release of inflammatory mediators. MrgprX2-IN-1 is promising for research of pseudo-allergic reactions, chronic pruritus, and inflammatory diseases .
    MrgprX2-IN-1
  • HY-176768

    Mas-related G-protein-coupled Receptor (MRGPR) Inflammation/Immunology
    MrgprX2-IN-2 (Compound example 12) is a selective Mas-related G-protein coupled receptor X2 (MRGPRX2) antagonist. MrgprX2-IN-2 blocks IgE-independent immune responses by inhibiting MRGPRX2-mediated mast cell degranulation and release of inflammatory mediators. MrgprX2-IN-2 is promising for research of pseudo-allergic reactions, chronic pruritus, and inflammatory diseases .
    MrgprX2-IN-2
  • HY-164298

    Mas-related G-protein-coupled Receptor (MRGPR) Neurological Disease Inflammation/Immunology
    MRGPRX2 modulator-3 (Compound 4-400) is a quinoline derivative and a MRGPRX2 modulator. MRGPRX2 modulator-3 can be used in the research of MRGPRX2-related diseases, such as allergies, pruritus, pain, inflammation and autoimmune diseases, etc .
    MRGPRX2 modulator-3
  • HY-17609S

    CR-845-d5; FE-202845-d5

    Isotope-Labeled Compounds Opioid Receptor Neurological Disease
    Difelikefalin-d5 (CR-845-d5) is deuterium labeled Difelikefalin. Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
    Difelikefalin-d5
  • HY-116691R

    Hydrocortisone 17-propionate 21-acetate (Standard)

    Reference Standards Glucocorticoid Receptor Neurological Disease Inflammation/Immunology
    Hydrocortisone aceponate (Hydrocortisone 17-propionate 21-acetate) Standard is the analytical standard of Hydrocortisone aceponate (HY-116691). This product is intended for research and analytical applications. Hydrocortisone aceponate (Hydrocortisone 17-propionate 21-acetate) is a diester-based topical glucocorticoid. Hydrocortisone aceponate alleviates symptoms such as erythema, dryness/desquamation, pruritus, epidermal exfoliation, and exudation/crusting. Hydrocortisone aceponate causes extremely few adverse reactions. Hydrocortisone aceponate is applicable to various dermatological disease studies .
    Hydrocortisone aceponate (Standard)
  • HY-173003

    Mas-related G-protein-coupled Receptor (MRGPR) Inflammation/Immunology
    EP-3945 is a potent agonist of Mas-related G protein-coupled receptor (MRGPR), more effective than the MRGPRD small molecule agonist β-Alanine (HY-N0230). MRGPR plays a crucial role in inflammatory pruritus and pain sensation. Additionally, MRGPR binds to Gq (MRGPRX2, MRGPRX4, MRGPRX1 couple with Gq; MRGPRX2, MRGPRD couple with Gi), with EP-3945 measured EC50 for Gq being 211.6 nM .
    EP-3945
  • HY-107747A

    Opioid Receptor Inflammation/Immunology
    GR 89696 free base is a highly selective κ2 opioid receptor agonist with potential to prevent pruritus .
    GR 89696 free base
  • HY-17609C

    CR-845 acetate; FE-202845 acetate

    Opioid Receptor Neurological Disease
    Difelikefalin (CR-845; FE-202845) acetate is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin acetate produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .
    Difelikefalin acetate
  • HY-I0021A

    Histamine Receptor Inflammation/Immunology Endocrinology
    Bepotastine tosylate is a selective and orally active second-generation histamine H1 receptor antagonist. Bepotastine tosylate can suppress the expression of nerve growth factor (NGF). Bepotastine tosylate can be used in studies of allergic rhinitis, allergic conjunctivitis and urticaria/pruritus .
    Bepotastine tosylate
  • HY-A0015R

    Reference Standards Histamine Receptor Inflammation/Immunology Endocrinology
    Bepotastine (besilate) (Standard) is the analytical standard of Bepotastine (besilate). This product is intended for research and analytical applications. Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
    Bepotastine besilate (Standard)
  • HY-B1177R

    Reference Standards Parasite TRP Channel Infection
    Crotamiton (Standard) is the analytical standard of Crotamiton. This product is intended for research and analytical applications. Crotamiton is a TRPV4 inhibitor. Crotamiton inhibits TRPV4 currents. Crotamiton inhibits TRPV4 selective agonist-induced pruritus-related behaviors in mice. Crotamiton inhibits Histamine- and Chloroquine-induced calcium influx via the H1R/TRPV1, MRGPRA3/TRPA1 pathways, and also suppresses calcium influx in primary mouse dorsal root ganglion neurons. Crotamiton is applicable to research related to pruritus, scabies, and non-scabietic pruritus .
    Crotamiton (Standard)
  • HY-168523

    Apical Sodium-Dependent Bile Acid Transporter Metabolic Disease
    S1647 is a ASBT and SOAT dual inhibitor. S1647 can be used in the study of intrahepatic cholestasis, cholestatic pruritus, and obstipation .
    S1647
  • HY-118557A

    S-MPEC hydrochloride

    5-HT Receptor Others
    Iferanserin hydrochloride (S-MPEC hydrochloride) is a selective serotonin receptor antagonist with the potential to inhibit internal hemorrhoids. Iferanserin hydrochloride demonstrated efficacy and tolerability in ongoing Phase IIb clinical trials, with the ability to significantly reduce patient-reported symptoms of bleeding and pruritus .
    Iferanserin hydrochloride
  • HY-A0015S

    Isotope-Labeled Compounds Histamine Receptor Inflammation/Immunology Endocrinology
    Bepotastine-d6(besylate) is deuterium labeled Bepotastine (besilate). Bepotastine besilate is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine besilate has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
    Bepotastine-d6 besylate
  • HY-B1589

    Histamine Receptor Infection Inflammation/Immunology
    (±)-Carbinoxamine is a blood-brain barrier-permeable histamine H1 receptor antagonist. (±)-Carbinoxamine blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. (±)-Carbinoxamine inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. (±)-Carbinoxamine can be used in research on allergic rhinitis, influenza, etc.
    (±)-Carbinoxamine
  • HY-B1589AR

    Reference Standards Histamine Receptor Influenza Virus Infection Inflammation/Immunology
    Carbinoxamine maleate salt (Standard) is the analytical standard of Carbinoxamine maleate salt (HY-B1589A). This product is intended for research and analytical applications. Carbinoxamine maleate salt is a blood-brain barrier-permeable histamine H1 receptor antagonist. Carbinoxamine maleate salt blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. Carbinoxamine maleate salt inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. Carbinoxamine maleate salt can be used in research on allergic rhinitis, influenza, etc.
    Carbinoxamine maleate salt (Standard)
  • HY-181006

    Interleukin Related Calcium Channel CCR Inflammation/Immunology
    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 .
    TSLP modulator-1
  • HY-I0021R

    Histamine Receptor Reference Standards Inflammation/Immunology Endocrinology
    Bepotastine (Standard) is the analytical standard of Bepotastine. This product is intended for research and analytical applications. Bepotastine is a selective and orally active second-generation histamine H1 receptor antagonist, can suppress the expression of nerve growth factor (NGF). Bepotastine has the potential for allergic rhinitis, allergic conjunctivitis and urticaria/pruritus research .
    Bepotastine (Standard)
  • HY-183050

    Mas-related G-protein-coupled Receptor (MRGPR) Others
    HEP-50768 is an orally active and selective MRGPRX4 (hX4) antagonist. HEP-50768 suppresses basal and bile-acid-stimulated hX4 activity. HEP-50768 binds the receptor’s transmembrane pocket and induces extracellular loop rearrangements. HEP-50768 modulates GPCR microswitch motifs and reduces bile-acid-induced pruritic scratching behaviors. HEP-50768 can be used for the research of cholestatic pruritus .
    HEP-50768
  • HY-182710

    Sodium Channel Neurological Disease
    DA-0218 is a Nav1.7 inhibitor. DA-0218 exerts state-dependent inhibitory effects. DA-0218 alleviates formalin-induced inflammatory pain behavior and Paclitaxel-induced mechanical hyperalgesia in mice. DA-0218 inhibits Histamine-induced acute pruritus and lymphoma-induced chronic pruritus in mice. DA-0218 can be used in research related to inflammatory pain, neuropathic pain, acute pruritus and chronic pruritus .
    DA-0218
  • HY-180847

    Sodium Channel Neurological Disease
    Quinisocaine is a topical anesthetic used for the study of pain and pruritus .
    Quinisocaine
  • HY-183773

    Opioid Receptor Neurological Disease
    KOR agonist-9 is a selective kappa opioid receptor (KOR) agonist with an EC50 of 1.41 nM. KOR agonist-9 exhibits >125-fold selectivity over μ/δ-opioid receptors. KOR agonist-9 antinociceptive and antipruritic effects in mice. KOR agonist-9 can be used for the research of pain, pruritus .
    KOR agonist-9
  • HY-182517

    TRP Channel Inflammation/Immunology
    AG1529 is a TRPV1 inhibitor and capsaicinoid-based soft agent with a human TRPV1 IC50 of 0.9-0.93 μM. AG1529 reversibly blocks capsaicin-evoked TRPV1 activation, binds to the TRPV1 capsaicin binding site, moderately affects pH-induced TRPV1 gating, and does not alter voltage- or heat-mediated TRPV1 responses. AG1529 suppresses TRPV1-mediated neuronal excitability, reduces capsaicin- and pH-evoked neuronal firing, abolishes histaminergic and inflammation-mediated TRPV1 sensitization. AG1529 exhibits anti-nociceptive and antipruritic effects, attenuates in vivo hyperalgesia and pruritus, dose-dependently reduces acute histaminergic itch in rodents, and mildly blocks hTRPA1 and hTRPM8 channel activity. AG1529 undergoes hydrolysis and dermal deactivation, minimizes TRPV1-associated side reactions, does not evoke capsaicin-like burning sensation, and does not disrupt physiological thermal regulation. AG1529 can be used for the research of inflammatory cutaneous nociception and acute histaminergic pruritus .
    AG1529
  • HY-B1589S

    Isotope-Labeled Compounds Histamine Receptor Influenza Virus Infection Inflammation/Immunology
    (±)-Carbinoxamine-d6 is the deuterium labeled (±)-Carbinoxamine (HY-B1589) . (±)-Carbinoxamine is a blood-brain barrier-permeable histamine H1 receptor antagonist. (±)-Carbinoxamine blocks the action of histamine on H1 receptors, reducing symptoms such as sneezing, rhinitis, rhinorrhea, erythema, pruritus and urticaria. (±)-Carbinoxamine inhibits influenza virus entry into cells via endocytosis, targets the early stage of the viral life cycle, and simultaneously reduces viral replication levels in the lungs, alleviating pathological damage and inflammatory responses in lung tissues. (±)-Carbinoxamine can be used in research on allergic rhinitis, influenza, etc.
    (±)-Carbinoxamine-d6
  • HY-165459

    MK-056

    TRP Channel Infection Inflammation/Immunology
    KJM429 (MK-056) is a high-affinity ligand for the rat vanilloid receptor rTRPV1 (Ki=30-63 nM) with a unique dual regulatory function. KJM429 acts as a competitive antagonist to inhibit TRPV1 receptor activation induced by Capsaicin (HY-10448), resiniferatoxin, thermal stimulation and weak acid (pH 6.0), and switches to a TRPV1 agonist under strong acid conditions (pH<5.5). KJM429 effectively blocks calcium influx induced by Capsaicin and partial thermal stimulation, and triggers calcium uptake under low pH conditions, with minimal effects on non-TRPV1-mediated calcium signaling. KJM429 can be used for research on the mechanisms of pain-related diseases such as postherpetic neuralgia, diabetic neuropathy, cluster headache, osteoarthritis and pruritus .
    KJM429
  • HY-119601

    Phosphodiesterase (PDE) Cancer
    GRI918013 (compound 1) is a selective and competitive autotaxin (ATX/NPP2) inhibitor with anti-invasive and anti-metastatic activity. GRI918013 competitively binds to ATX, blocking lipid substrates such as lysophosphatidylcholine (LPC) from entering the ATX active site, thereby inhibiting ATX-mediated hydrolysis of LPC to lysophosphatidic acid (LPA), and consequently inhibiting ATX-LPA axis-related tumor cell invasion and metastasis. GRI918013 inhibits ATX-mediated hydrolysis of the LPL substrate FS-3 (IC50=31.42 nM, Ki=12.98 nM). GRI918013 can be used in research on cancer invasion and metastasis, such as melanoma, and can also serve as a tool compound for ATX-LPA axis-related diseases such as fibrotic diseases, neuropathic pain, and cholestatic pruritus .
    GRI918013

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