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Inverse

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332

Inhibitors & Agonists

29

Fluorescent Dye

10

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6

Natural
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9

Isotope-Labeled Compounds

146

Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-132909

    Nuclear Hormone Receptor 4A/NR4A Inflammation/Immunology Cancer
    Nurr1 inverse agonist-1 is an inverse agonist tool for the neuroprotective transcription factor Nurr1.
    Nurr1 inverse agonist-1
  • HY-49076

    ROR Cancer
    RORγ inverse agonist 1 is the inverse agonist of RORγ .
    RORγ inverse agonist 1
  • HY-139847

    ROR Inflammation/Immunology
    RORγt inverse agonist 23 is a potent, selective, and orally available novel retinoic acid receptor-related orphan receptor γt inverse agonist.
    RORγt inverse agonist 23
  • HY-122737

    ROR Inflammation/Immunology
    RORγt Inverse agonist 8 is a potent, selective, orally bioavailable RORγt inverse agonist, with an IC50 of 19 nM for human RORγt-LBD .
    RORγt Inverse agonist 8
  • HY-143271

    ROR Inflammation/Immunology
    RORγt inverse agonist 29 is a potent, orally active and selective RORγt inverse agonist (IC50: 21 nM). RORγt inverse agonist 29 can be used in the research of skin inflammation and autoimmune diseases like psoriasis .
    RORγt inverse agonist 29
  • HY-135280

    CB1 Inverse agonist 1

    Cannabinoid Receptor Metabolic Disease
    MRL-650 (CB1 inverse agonist 1) is a highly potent, orally active, and specific inverse agonist of CB1 receptor with IC50s of 7.5 nM and 4100 nM for CB1 and CB2 receptors, respectively. Anorexigenic effects .
    MRL-650
  • HY-147533

    ROR Inflammation/Immunology
    RORγt inverse agonist 30 (Compound 1) is a potent RORγt inverse agonist with the IC50 of 46 nM. Targeting the nuclear receptor RORγt is effective in autoimmune disorders .
    RORγt inverse agonist 30
  • HY-149833

    Estrogen Receptor/ERR Infection Metabolic Disease
    ERRγ inverse agonist 2 (compound 19) is a potent and selective ERRγ inverse agonist with a Kd value of 6.5 μM. ERRγ inverse agonist 2 inhibits the expression of hepcidin, fibrinogen and gluconeogenic genes. ERRγ inverse agonist 2 has antimicrobial, anti-coagulant and antidiabetic activities .
    ERRγ inverse agonist 2
  • HY-111748

    ROR Inflammation/Immunology
    RORγt Inverse agonist 2 is a selective, orally active RORγt inverse agonist with an EC50 of 119 nM .
    RORγt Inverse agonist 2
  • HY-132195

    ROR Inflammation/Immunology
    RORγt inverse agonist 14 (8e) is a potent, orally active and selective RORγt inverse agonist (EC50 of 2.5 nM) with anti-inflammatory activity. RORγt inverse agonist 14 is used in the study for rheumatoid arthritis and psoriasis .
    RORγt inverse agonist 14
  • HY-156354

    Others Metabolic Disease
    GPR61 Inverse agonist 1 (Compound 1) is a GPR61 inverse agonist (IC50: 11 nM). GPR61 Inverse agonist 1 can be used for research of disorders of metabolism and body weight, such as obesity and cachexia .
    GPR61 Inverse agonist 1
  • HY-12095

    Cannabinoid Receptor Neurological Disease
    CB1 inverse agonist 2 is an orally active inverse agonist of Cannabinoid Receptor CB1. CB1 inverse agonist 2 effectively inhibits CP55940-induced hypothermia and anorexia in mice model .
    CB1 inverse agonist 2
  • HY-130243

    ROR Inflammation/Immunology
    RORγt Inverse agonist 6 (compound 43) is a RORγt inverse agonist for the study of Th17-driven autoimmune diseases. RORγt Inverse agonist 6 (compound 43) suppresses IL-17A gene expression by IL-23 stimulation in vivo .
    RORγt Inverse agonist 6
  • HY-114411

    Estrogen Receptor/ERR Cancer
    ERRγ Inverse Agonist 1 (Compound 12) is a potent, selective and orally bioavailable Estrogen-related Receptor grammar (ERRγ) inverse agonist, with an IC50 of 40 nM .
    ERRγ inverse agonist 1
  • HY-155548

    ROR Inflammation/Immunology
    RORγt inverse agonist 31 (14g) is a potent retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonist, with an IC50 of 0.428 μM. RORγt inverse agonist 31 can alleviate the severity of Imiquimod (HY-B0180)-induced psoriasis in mice .
    RORγt inverse agonist 31
  • HY-131338

    ROR Inflammation/Immunology
    RORγt inverse agonist 13 (Compound 3i) is a potent, orally active and selective RORγt inverse agonist, with improved agent-like properties, with an IC50 of 63.8 nM .
    RORγt inverse agonist 13
  • HY-142806

    ROR Inflammation/Immunology
    RORγt inverse agonist 26 is a potent reverse agonist of RORγt. RORγt inverse agonist 26 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 26 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 1) .
    RORγt inverse agonist 26
  • HY-142703

    ROR Inflammation/Immunology
    RORγt inverse agonist 28 is a potent reverse agonist of RORγt. RORγt inverse agonist 28 regulates the differentiation of Th17 cells and inhibits the production of IL-17. RORγt inverse agonist 28 has the potential for the research of inflammation and autoimmune diseases (extracted from patent WO2021228215A1, compound 6) .
    RORγt inverse agonist 28
  • HY-128573

    ROR Neurological Disease
    RORγt Inverse agonist 3 is a potent, selective and orally active RORγ inverse agonist, with EC50s of 0.22 μM and 0.15 μM for hRORγ and RORγt (human IL-17 cells), respectively .
    RORγt Inverse agonist 3
  • HY-133552

    ROR Inflammation/Immunology
    RORγt Inverse agonist 10 is a potent and orally bioavailable RORγt (retinoic acid receptor-related orphan nuclear receptor gamma t) inverse agonist, with an IC50 of 51 nM. RORγt is a major transcription factor of genes related to psoriasis pathogenesis such as IL-17A, IL-22, and IL-23R
    RORγt Inverse agonist 10
  • HY-118336

    Histamine Receptor Inflammation/Immunology
    VUF10497 is a potent histamine H4 receptor (H4R) inverse agonist with anti-inflammatory activity .
    VUF10497
  • HY-124225

    GABA Receptor Neurological Disease
    RU 33965 is an orally active benzodiazepine receptor weak partial inverse agonist .
    RU 33965
  • HY-160039

    LXR Cancer
    GAC0001E5 is an LXR inverse agonist. GAC0001E5 has antiproliferative activity and can be used in cancer research .
    GAC0001E5
  • HY-169001

    5-HT Receptor Neurological Disease
    5-HT2A/5-HT2C inverse agonist 1 is a potent and dual 5-HT2A and 5-HT2C receptor inverse agonist with a hERG inhibitions, thus avoiding cardiovascular risks. 5-HT2A/5-HT2C inverse agonist 1 shows significant antipsychotic efficacy in the MK-801 (HY-15084B)-induced mouse model. 5-HT2A/5-HT2C inverse agonist 1 is promising for research of psychosis .
    5-HT2A/5-HT2C inverse agonist 1
  • HY-160161

    PPAR Cancer
    BAY-5094 is a PPAR gamma (PPARG) inverse agonist. BAY-5094 has oral activity. BAY-5094 can be used in the research of luminal bladder cancer .
    BAY-5094
  • HY-137434

    ABBV-157

    ROR Inflammation/Immunology
    Cedirogant (ABBV-157) is an orally active RORγt inverse agonist. Cedirogant can be used for psoriasis research .
    Cedirogant
  • HY-119010

    Melatonin Receptor Neurological Disease
    UCM 549 is a melatonin MT2 receptor inverse agonist and a MT1 receptor antagonist .
    UCM 549
  • HY-14289
    Cimetidine
    2 Publications Verification

    SKF-92334

    Histamine Receptor Bacterial Endocrinology Cancer
    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
  • HY-14289R

    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-137061

    GHSR Metabolic Disease
    AZ-GHS-22 is a potent, non-CNS penetrant GHS-R1a inverse agonist (IC50=0.77 nM) .
    AZ-GHS-22
  • HY-P1432

    GHSR Metabolic Disease
    K-(D-1-Nal)-FwLL-NH2 is a high affinity, potent and inverse ghrelin receptor agonist (EC50=3.4 nM, Ki=4.9 nM). K-(D-1-Nal)-FwLL-NH2 can be used for the research of obesity .
    K-(D-1-Nal)-FwLL-NH2
  • HY-19770
    GSK2981278
    3 Publications Verification

    ROR Inflammation/Immunology
    GSK2981278 is a potent and selective RORγ inverse agonist. GSK2981278 inhibits activation of the il17 promoter and interferes RORγ-DNA binding .
    GSK2981278
  • 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-133128

    ROR Cancer
    FM26 (compound 25) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 264 nM. FM26 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells .
    FM26
  • HY-100369A

    GABA Receptor Neurological Disease
    DMCM hydrochloride is a nonselective full inverse agonist of benzodiazepine. DMCM shows bnding afinity at human recombinant GABAA αxβ3γ2 receptor subtypes with Kis of 10 nM, 13 nM, 7.5 nM, 2.2 nM for α1, α2, α3, and α5 ?receptors, respectively .
    DMCM hydrochloride
  • HY-119464
    MRL-871
    1 Publications Verification

    ROR Cancer
    MRL-871 (compound 3) is a potent and allosteric retinoic acid receptor-related orphan receptor γt (RORγt) inverse agonists with an IC50 of 12.7 nM. MRL-871 has a distinct isoxazole chemotype and effectively reduces IL-17a mRNA production in EL4 cells .
    MRL-871
  • HY-116247

    PPAR Metabolic Disease Inflammation/Immunology
    ST247 a potent PPARβ/δ inverse agonist. ST247 has a higher affinity to PPARβ/δ. ST247 modulates expression of the activation marker CCL2 in the opposite direction. ST247 efficiently induces the interaction with corepressors. ST247 inhibits the agonist-induced transcriptional activity of PPARβ/δ .
    ST247
  • HY-108529
    BMS493
    4 Publications Verification

    RAR/RXR Metabolic Disease
    BMS493 is an inverse pan-retinoic acid receptor (RAR) agonist. BMS493 increases nuclear corepressor interaction with RARs. BMS493 also could prevent retinoic acid-induced differentiation . BMS493 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    BMS493
  • HY-121852

    SCH-225336

    Cannabinoid Receptor Inflammation/Immunology
    SCH 336 is a potent, selective, inverse and orally active CB2 agonist. SCH 336 inhibits BaF3/CB2 migration. SCH 336 significantly inhibits the migration of leukocytes in vivo. SCH 336 blocks ovalbumin-induced lung eosinophilia in mice .
    SCH 336
  • HY-110329

    Others Cancer
    ML179 (SR-1309) is a inverse LRH1 (Liver receptor homologue-1) agonist with IC50 of 320 nM. ML179 shows anti-proliferation activity in MDA-MB-231 cells. ML179 has the potential for the research of ER-negative breast cancer .
    ML179
  • HY-100991

    ZK 39106; LSU-65

    GABA Receptor Neurological Disease
    FG 7142 (ZK 39106; LSU-65), a non-selectively benzodiazepine inverse agonist, has high affinity for the α1 subunit-containing GABAA receptor (Ki=91 nM). FG 7142 (ZK 39106; LSU-65) also modulates GABA-induced chloride flux at GABAA receptors expressing the α1 subunit (EC50= 137 nM). FG 7142 (ZK 39106; LSU-65) can increase tyrosine hydroxylation and cause upregulation of?β-adrenoceptors in mouse cerebral cortex .
    FG 7142
  • 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-116603

    5-HT Receptor Others
    SB-236057 is an inverse agonist of the 5-HT1B receptor that exhibits strong skeletal teratogenicity in rodents and rabbits. SB-236057 affects gene expression during embryonic development through interference with the Notch signaling pathway and interaction with r-esp1. SB-236057 induces somatic patterning and tail extension defects in rat embryos during early organogenesis .
    SB-236057
  • HY-110186

    Adenosine Receptor Metabolic Disease
    PQ-69 is a potent and selective adenosine A1 receptor antagonist with inverse agonist activity. PQ-69 binds to hA1 receptor with a Ki value of 0.96 nM, is 217-fold more selective compared with hA2A receptors (Ki=208 nM) and >1,000-fold selectivity over hA3 receptor (Ki >100 μM). PQ-69 can be used for the research of renal dysfunction .
    PQ-69
  • 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-10559
    Nelotanserin
    2 Publications Verification

    APD125

    5-HT Receptor Neurological Disease Cancer
    Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.
    Nelotanserin
  • HY-116521

    PPAR Metabolic Disease
    SR2595 is an inverse agonist of PPARγ with an IC50 of 30 nM .
    SR2595
  • HY-B0188

    Mianserine

    Histamine Receptor Neurological Disease Endocrinology
    Mianserin is a H1 receptor inverse agonist and is a psychoactive agent of the tetracyclic antidepressant.
    Mianserin
  • HY-12664

    Others Others
    AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
    AF64394
  • HY-119208

    CXCR Others
    VUF11211 is an allosteric inverse CXCR3 agonist with a Kd of 0.65 nM .
    VUF11211

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