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Inverse antagonist

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-14289
    Cimetidine
    5+ Cited Publications

    SKF-92334

    Histamine Receptor Bacterial Cardiovascular Disease Infection Neurological Disease Metabolic Disease Cancer
    Cimetidine (SKF-92334) is an orally active, inverse and BBB-permeable histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine has anti-cancer and anti-inflammatory activity .
    Cimetidine
  • HY-B0349
    Meclizine dihydrochloride
    4 Publications Verification

    Meclozine dihydrochloride

    Histamine Receptor Apoptosis Neurological Disease Endocrinology Cancer
    Meclizine (Meclozine) dihydrochloride, an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine dihydrochloride is a member of the piperazine class of H1 antagonists. Meclizine dihydrochloride is an effective anti-motion sickness agent. Meclizine dihydrochloride crosses the blood-brain barrier. Meclizine dihydrochloride can be used for the research of polyQ toxicity disorders, such as Huntington's disease. Meclizine dihydrochloride is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
    Meclizine dihydrochloride
  • HY-N0049
    Nuciferine
    5+ Cited Publications

    Parasite 5-HT Receptor Dopamine Receptor Neurological Disease
    Nuciferine is an antagonist at 5-HT2A (IC50=478 nM), 5-HT2C (IC50=131 nM), and 5-HT2B (IC50=1 μM), an inverse agonist at 5-HT7 (IC50=150 nM), a partial agonist at D2 (EC50=64 nM), D5 (EC50=2.6 μM) and 5-HT6 (EC50=700 nM), an agonist at 5-HT1A (EC50=3.2 μM) and D4 (EC50=2 μM) receptor.
    Nuciferine
  • HY-32329

    Org-8282

    5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
    Setiptiline
  • HY-101198

    Histamine Receptor Apoptosis Neurological Disease Cancer
    Clobenpropit dihydrobromide is a potent histamine H3R antagonist/inverse agonist with a pEC50 of 8.07 for histamine H3LR . Clobenpropit dihydrobromide acts as partial agonist at histamine H4 receptors (Ki 13 nM). Clobenpropit dihydrobromide also binds to serotonin 5-HT3 receptors (Ki 7.4 nM) and α2A/α2C adrenoceptors (Ki 17.4/7.8 nM) . Clobenpropit dihydrobromide increases apoptosis .
    Clobenpropit dihydrobromide
  • HY-116649

    AM4113

    Cannabinoid Receptor Neurological Disease Metabolic Disease
    CB1 antagonist 2 (AM4113) is an orally active cannabinoid receptor type 1 (CB1R) antagonist. CB1 antagonist 2 suppresses appetite, reduces body weight, and blocks addictive behaviors such as heroin addiction, without causing adverse effects like nausea and depression that are associated with traditional CB1 inverse agonists. CB1 antagonist 2 can be used in studies related to obesity and opioid addiction .
    CB1 antagonist 2
  • HY-112340

    Cannabinoid Receptor Neurological Disease Metabolic Disease
    CB1 antagonist 4 (compound 8) is a selective cannabinoid receptor 1 (CB1) inverse agonist with an IC50 of 8.5 nM for human CB1. CB1 antagonist 4 shows selective for CB1 over CB2 receptors (IC50 of 604.9 nM). CB1 antagonist 4 inhibits GTP binding to CB1-overexpressing cell membranes with an EC50 of 18.5 nM .
    CB1 antagonist 4
  • HY-100775
    Fezagepras sodium
    1 Publications Verification

    Setogepram sodium; PBI-4050 sodium

    Free Fatty Acid Receptor GPR84 Metabolic Disease Inflammation/Immunology
    Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84 . Fezagepras sodium decreases renal, liver and pancreatic fibrosis . Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions .
    Fezagepras sodium
  • HY-100775A
    Fezagepras
    1 Publications Verification

    Setogepram; PBI-4050

    Free Fatty Acid Receptor GPR84 Metabolic Disease Inflammation/Immunology
    Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84 . Fezagepras decreases renal, liver and pancreatic fibrosis . Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions .
    Fezagepras
  • HY-124717

    Endogenous Metabolite Others
    YC-001 is an inverse agonist and antagonist of rod opsin. YC-001 reversibly binds rod opsin and stabilizes the rod opsin structure. YC-001 protects mice from bright light-induced retinal degeneration. YC-001 has the potential for the research of retinal degeneration .
    YC-001
  • HY-10013A

    MK-0364 racemate

    Cannabinoid Receptor Neurological Disease
    Taranabant racemate (MK-0364 racemate) is an antagonist and/or inverse agonist of the Cannabinoid-1 (CB1) receptor extracted from patent WO 2004048317 A1 .
    Taranabant racemate
  • HY-101630

    EGIS-3886

    5-HT Receptor Neurological Disease
    Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist.
    Deramciclane
  • HY-103476

    GABA Receptor Neurological Disease
    Ro15-4513, imidazobenzodiazepinone derivative, is a partial inverse agonist of benzodiazepine receptor (BZR) . Ro15-4513 is a potent ethanol antagonist . Ro15-4513 has anti-anxiety effect . Ro15-4513 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.
    Ro15-4513
  • HY-14289R

    SKF-92334 (Standard)

    Reference Standards Histamine Receptor Bacterial Endocrinology Cancer
    Cimetidine (Standard) is the analytical standard of Cimetidine. This product is intended for research and analytical applications. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine has anti-cancer and anti-inflammatory activity .
    Cimetidine (Standard)
  • HY-144699

    Estrogen Receptor/ERR Cancer
    ERRα antagonist-2 (Compound 11) is a potential ERRα (estrogen related receptor α) inverse agonist with an IC50 of 0.80 μM. ERRα antagonist-2 suppresses the migration and invasion of the ER-negative MDA-MB-231 cell line. ERRα antagonist-2 inhibits breast cancer growth in vivo .
    ERRα antagonist-2
  • HY-32329A

    MO-8282

    5-HT Receptor Neurological Disease
    Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
    Setiptiline maleate
  • HY-B1109R

    Acecainide (Standard); NAPA (Standard)

    Reference Standards Potassium Channel Drug Metabolite Cardiovascular Disease
    Cimetidine (hydrochloride) (Standard) is the analytical standard of Cimetidine (hydrochloride). This product is intended for research and analytical applications. Cimetidine (SKF-92334) hydrochloride is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity .
    N-Acetylprocainamide (Standard)
  • HY-139748

    Antibiotic Bacterial Infection
    S32212 is a serotonin type 2C receptor inverse agonist and an α2 adrenoceptor antagonist. S32212 exhibits antidepressant activity and can reduce immobility time in forced-swim test in rats .
    ETX0462
  • HY-17610

    TS-091

    Histamine Receptor Neurological Disease
    Enerisant (TS-091) is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
    Enerisant
  • HY-175306

    EBI2/GPR183 Arrestin Inflammation/Immunology Cancer
    GPR183 inverse agonist-1 (Compound 78) is a GPR183 inverse agonist. GPR183 inverse agonist-1 inhibits the GPR183-mediated Gi activation and β-arrestin2 recruitment, and blocks PBMC migration. GPR183 inverse agonist-1 can be used for inflammatory, autoimmune and neoplastic disorders research .
    GPR183 inverse agonist-1
  • HY-B0349A

    Meclozine

    Histamine Receptor Apoptosis Neurological Disease Inflammation/Immunology
    Meclizine (Meclozine), an antihistamine, reversibly inhibits the interaction of histamine at the H1 receptors. Meclizine is a member of the piperazine class of H1 antagonists. Meclizine is an effective anti-motion sickness agent. Meclizine crosses the blood–brain barrier. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR. Meclizine can be used for the research of polyQ toxicity disorders, such as Huntington's disease .
    Meclizine
  • HY-114025

    Histamine Receptor Neurological Disease Endocrinology
    H4 Receptor antagonist 1 is a potent and selective histamine H4 receptor inverse agonist, with an IC50 of 19 nM.
    H4 Receptor antagonist 1
  • HY-175784

    Cannabinoid Receptor Neurological Disease
    CB2R antagonist 4 is a selective CB2R antagonist/inverse agonist with a pKi of 6.54. CB2R antagonist 4 shows a ≥11-fold selectivity towards CB2R over CB1R and can be utilized in neurological research .
    CB2R antagonist 4
  • HY-13974

    Adrenergic Receptor Neurological Disease
    S32212 is a serotonin type 2C receptor inverse agonist and an 2 adrenoceptor antagonist. S32212 exhibits antidepressant activity and can reduce immobility time in forced-swim test in rats .
    S32212
  • HY-12192

    Histamine Receptor Metabolic Disease
    A-423579 is an orally active non-imidazole histamine H3 receptor antagonist. A-423579 exhibits high affinity and good selectivity for human and rat H3 receptors, and possesses both antagonistic and inverse agonistic activities. A-423579 can effectively reduce body weight in obese rodents, with concomitant decreases in fat content, plasma leptin levels, and triglycerides. A-423579 possesses anti-obesity activity and can be used in the research of obesity and related metabolic disorders .
    A-423579
  • HY-175264

    Pregnane X Receptor (PXR) Cytochrome P450 Metabolic Disease
    MI891 is a highly selective PXR antagonist (IC50 = 3.76 μM, Kd = 1.7 μM) and inverse agonist (IC50 = 6.1 μM). MI891 selectively disrupts the interaction between PXR and its coactivator SRC1. MI891 effectively inhibits Rifampicin (HY-B0272)-induced PXR activation. MI891 is useful for the study of metabolic diseases and other diseases .
    MI891
  • HY-171235

    5-HT Receptor Neurological Disease
    5-HT2A antagonist 3 (Formula (III)) is a 5-HT2A receptor antagonist and inverse agonist with a pIC50 of 8.7 and a pKi of 9. 5-HT2A antagonist 3 can be utilized in neurological reesearch .
    5-HT2A antagonist 3
  • HY-119010

    Melatonin Receptor Neurological Disease
    UCM 549 is a melatonin MT2 receptor inverse agonist and a MT1 receptor antagonist .
    UCM 549
  • HY-113730

    CXCR Others
    VUF5834 is a non-peptide chemokine receptor CXCR3 antagonist with non-competitive antagonistic and inverse agonistic activities. VUF5834 blocks the effects of CXCL10 and CXCL11 on human CXCR3, exhibits non-competitive antagonistic and inverse agonistic properties to CXCR3, and, except for TAK-779, has a slightly lower affinity for rodent CXCR3 than for primate CXCR3.
    VUF5834
  • HY-14289S

    SKF-92334-d3

    Histamine Receptor Endocrinology Cancer
    Cimetidine-d3 is the deuterium labeled Cimetidine. Cimetidine (SKF-92334) is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine is an inverse agonist. Cimetidine has anti-cancer and anti-inflammatory activity .
    Cimetidine-d3
  • HY-155481A

    Cannabinoid Receptor Others
    CB2 receptor antagonist 4 (compound (R)-1) is a CB2R-selective inverse agonist with a Kd value of 39 nM .
    CB2 receptor antagonist 4
  • HY-168333

    5-HT Receptor mTOR CDK Neurological Disease
    5-HT6 inverse agonist 1 (Compound 33) is an antagonist for 5-HT6 receptor with a Ki of 23 nM and a Kb of 6.62 nM. 5-HT6 inverse agonist 1 inhibits the 5-HT6R mediated Cdk5 and mTOR signaling pathway. 5-HT6 inverse agonist 1 reduces tactile hypersensitivity in spinal nerve ligation (SNL)-induced rat model .
    5-HT6 inverse agonist 1
  • HY-178319

    PZL-1

    Drug Derivative Adrenergic Receptor Cardiovascular Disease
    Photoazolol-1 is a β-adrenergic receptor (βAR)-blocker derivative. Photoazolol-1 can transfer from an inverse agonist to a neutral antagonist upon photoactivation .
    Photoazolol-1
  • HY-155481

    Cannabinoid Receptor Neurological Disease
    CB2 receptor antagonist 3 (compound (S)-1) is an inverse agonist of the cannabinoid receptor CB2R with Kd=39 nM. CB2 receptor antagonist 3 can be used as a tool to synthesize a variety of CB2R probes .
    CB2 receptor antagonist 3
  • HY-112219

    Histamine Receptor Inflammation/Immunology Endocrinology
    H3R antagonist 1 is a histamine receptor 3 (H3R) inverse agonist. H3R antagonist 1 increases the expression levels of myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes. H3R antagonist 1 can be used for the study of multiple sclerosis .
    H3R antagonist 1
  • HY-112219A

    Histamine Receptor Inflammation/Immunology Endocrinology
    H3R antagonist 1 hydrochloride is a histamine receptor 3 (H3R) inverse agonist. H3R antagonist 1 hydrochloride increases the expression levels of myelin-associated glycoprotein (MAG) and myeline basic protein (MBP) in differentiating oligodendrocytes. H3R antagonist 1 hydrochloride can be used for the study of multiple sclerosis .
    H3R antagonist 1 hydrochloride
  • HY-14517

    Histamine Receptor Neurological Disease
    H3R antagonist 5 (Compound 1b) is a selective histamine H3 receptor inverse agonist with a IC50 of 0.54 nM and the ability to cross the blood-brain barrier. H3R antagonist 5 can be used in central nervous system-related research .
    H3R antagonist 5
  • HY-117118A

    5-HT Receptor Neurological Disease
    AC-90179 is a selective 5-HT2A receptor inverse agonist (Ki = 2.1 nM) and 5-HT2C antagonist, a potential antipsychotic compound .
    AC-90179
  • HY-101630A

    EGIS-3886 fumarate

    5-HT Receptor Others
    Deramciclane fumarate is an antagonist of 5-HT Receptor. Deramciclane fumarate is an inverse agonist of 5-HT2C Receptor with an IC50 of 168 nM. Deramciclane fumarate also decreases basal phosphoinositide hydrolysis .
    Deramciclane fumarate
  • HY-17610A

    TS-091 hydrochloride

    Histamine Receptor Neurological Disease
    Enerisant (TS-091) hydrochloride is a potent, highly selective, competitive and orally active histamine H3 receptor antagonist/inverse agonist with IC50s of 2.89 nM and 14.5 nM against human and rat histamine H3 receptors, respectively .
    Enerisant hydrochloride
  • HY-B0349S

    Meclozine-d8

    Isotope-Labeled Compounds Histamine Receptor Apoptosis Inflammation/Immunology
    Meclizine-d8 is a deuterium labeled Meclizine. Meclizine is a histamine H1 receptor antagonist and has the potential to treat nausea and motion sickness. Meclizine is an agonist ligand for mouse constitutive androstane receptor (CAR) and an inverse agonist for Human CAR .
    Meclizine-d8
  • HY-14289A

    SKF-92334 hydrochloride

    Histamine Receptor Bacterial Metabolic Disease Cancer
    Cimetidine (SKF-92334) hydrochloride is an orally active, inverse and BBB-permeable histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity .
    Cimetidine hydrochloride
  • HY-100449A

    Prostaglandin Receptor Endocrinology
    (S)-AL 8810 is an 11β-fluoro analog of PGF2α that acts as a potent and selective antagonist at the FP receptor. (S)-AL 8810 is the C-15 epimer of AL 8810, having the inverse, (S), or "natural" configuration at C-15 relative to AL 8810, which is 15-(R) .
    (S)-AL-8810
  • HY-100775R

    Setogepram sodium (Standard); PBI-4050 sodium (Standard)

    Reference Standards Free Fatty Acid Receptor GPR84 Metabolic Disease Inflammation/Immunology
    Fezagepras (sodium) (Standard) is the analytical standard of Fezagepras (sodium). This product is intended for research and analytical applications. Fezagepras (Setogepram) sodium acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84 . Fezagepras sodium decreases renal, liver and pancreatic fibrosis . Fezagepras sodium exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions .
    Fezagepras sodium (Standard)
  • HY-100775AR

    Setogepram (Standard); PBI-4050 (Standard)

    Reference Standards Free Fatty Acid Receptor GPR84 Metabolic Disease Inflammation/Immunology
    Fezagepras (Standard) is the analytical standard of Fezagepras. This product is intended for research and analytical applications. Fezagepras (Setogepram) acts as an orally active agonist for GPR40 and as an antagonist or inverse agonist for GPR84 . Fezagepras decreases renal, liver and pancreatic fibrosis . Fezagepras exerts anti-fibrotic, anti-inflammatory and anti-proliferative actions .
    Fezagepras (Standard)
  • HY-118037

    CXCR Inflammation/Immunology
    VUF10132 is a non-peptide CXCR3 receptor antagonist with anti-inflammatory activity, inhibiting diseases such as rheumatoid arthritis, multiple sclerosis, and psoriasis. VUF10132 has high affinity for the human CXCR3 receptor but slightly lower affinity for the murine CXCR3 receptor. Additionally, VUF10132 exhibits inverse agonist properties at the CXCR3 receptor .
    VUF10132
  • HY-14289AR

    SKF-92334 hydrochloride (Standard)

    Reference Standards Histamine Receptor Bacterial Endocrinology Cancer
    Cimetidine (hydrochloride) (Standard) is the analytical standard of Cimetidine (hydrochloride). This product is intended for research and analytical applications. Cimetidine (SKF-92334) hydrochloride is an orally active and inverse histamine H2 receptor antagonist with a Ki of 0.6 μM. Cimetidine hydrochloride is a gastric acid reducer, and can be used for duodenal and gastric ulcers research. Cimetidine hydrochloride has anti-cancer and anti-inflammatory activity .
    Cimetidine hydrochloride (Standard)
  • HY-32329S

    Isotope-Labeled Compounds 5-HT Receptor Adrenergic Receptor Neurological Disease
    Setiptiline-d3 is the deuterium labeled Setiptiline. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
    Setiptiline-d3
  • HY-32329R

    Org-8282 (Standard)

    5-HT Receptor Adrenergic Receptor Reference Standards Neurological Disease
    Setiptiline (Standard) is the analytical standard of Setiptiline. This product is intended for research and analytical applications. Setiptiline (Org-8282) is a serotonin receptor antagonist. Setiptiline is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine.
    Setiptiline (Standard)
  • HY-32329AR

    MO-8282 (Standard)

    5-HT Receptor Reference Standards Neurological Disease
    Setiptiline (maleate) (Standard) is the analytical standard of Setiptiline (maleate). This product is intended for research and analytical applications. Setiptiline maleate (MO-8282 maleate) is a serotonin receptor antagonist. Setiptiline maleate is a tetracyclic antidepressant (TeCA) which acts as a noradrenergic and specific serotonergic antidepressant (NaSSA). Setiptiline maleate acts as a norepinephrine reuptake inhibitor, α2-adrenergic receptor antagonist, and serotonin receptor antagonist, likely at the 5-HT2A, 5-HT2C, and/or 5-HT3 subtypes, as well as an H1 receptor inverse agonist/antihistamine .
    Setiptiline maleate (Standard)

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