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inverse

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465

Inhibitors & Agonists

34

Fluorescent Dyes

3

Biochemical Assay Reagents

10

Peptides

10

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15

Isotope-Labeled Compounds

155

Click Chemistry

3

Oligonucleotides

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-108529
    BMS493
    5+ Cited Publications

    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-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-13421
    SR1001
    5+ Cited Publications

    REV-ERB ROR Inflammation/Immunology
    SR1001 is a selective RORα and RORγt inverse agonist with Kis 172 and 111 nM, respectively.
    SR1001
  • HY-14413
    SR3335
    10+ Cited Publications

    ML 176

    ROR Metabolic Disease
    SR3335 (ML 176) is a selective RORα inverse agonist that directly binds to RORα with a Ki of 220 nM .
    SR3335
  • HY-12584

    PF-05190457

    GHSR Metabolic Disease Endocrinology
    PF-5190457 (PF-05190457) is a potent and selective ghrelin receptor inverse agonist with a pKi of 8.36 .
    PF-5190457
  • HY-12199
    Pitolisant
    2 Publications Verification

    Tiprolisant

    Histamine Receptor Neurological Disease Endocrinology
    Pitolisant is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
    Pitolisant
  • HY-12199B
    Pitolisant hydrochloride
    2 Publications Verification

    Ciproxidine; BF 2649

    Histamine Receptor Neurological Disease Endocrinology
    Pitolisant hydrochloride is a potent and selective nonimidazole inverse agonist at the recombinant human histamine H3 receptor (Ki=0.16 nM).
    Pitolisant hydrochloride
  • HY-16972
    SR9243
    5+ Cited Publications

    LXR Cancer
    SR9243 is a liver-X-receptor (LXR) inverse agonist that induces LXR-corepressor interaction.
    SR9243
  • HY-16998
    SR2211
    1 Publications Verification

    ROR Inflammation/Immunology
    SR2211 is a potent, selective synthetic RORγ modulator and functions as an inverse agonist, with a Ki of 105 nM and an IC50 of ~320 nM.
    SR2211
  • HY-134599

    Biochemical Assay Reagents Cancer
    (2E)-TCO-PNB ester is an active reaction substrate with the properties of trans-cyclooctene derivatives. The core chemical property of (2E)-TCO-PNB ester is its ability to undergo efficient inverse electron-demand Diels-Alder (IEDDA) cycloaddition with tetrazine groups. (2E)-TCO-PNB ester can be used in ligation reactions to verify the integrity of tetrazine groups, and also serves as a key synthetic raw material for the preparation of the prodrug TCO-DOX. (2E)-TCO-PNB ester is applied in research related to drug synthesis and bioorthogonal chemistry .
    (2E)-TCO-PNB ester
  • 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-12664
    AF64394
    1 Publications Verification

    Orphan GPCR Others
    AF64394 is a GPR3 inverse agonist, with a pIC50 of 7.3.
    AF64394
  • 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-19770
    GSK2981278
    4 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-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-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-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-156354

    Orphan GPCR 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-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-102075A

    ROR Inflammation/Immunology
    TMP778 is a potent and selevtive RORγt inverse agonist, with an IC50 of 7 nM in FRET assay.
    TMP778
  • HY-148352
    BAY-4931
    1 Publications Verification

    PPAR Cancer
    BAY-4931 is a potent, covalent and selective PPARγ inverse-agonist with an IC50 of 0.17 nM .
    BAY-4931
  • 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-114411

    Estrogen Receptor/ERR Cancer
    ERRγ inverse agonist 1 (Compound 12) is a selective ERRγ inverse agonist with an IC50 value of 0.040 μM against ERRγ. ERRγ inverse agonist 1 inhibits the activity of ERRγ at the functional level. ERRγ inverse agonist 1 can be used in the research of anaplastic thyroid cancer .
    ERRγ 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-160039

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

    Nuclear Hormone Receptor 4A/NR4A Cancer
    ML179 (SR-1309) is a inverse LRH1/NR5A2 (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-151759

    Fluorescent Dye Cancer
    Sulfo-Cy5-TCO is a water-soluble sulfonated Cy5 fluorescent reagent containing trans-cyclooctene (TCO). Sulfo-Cy5-TCO undergoes an inverse electron demand Diels‑Alder reaction with tetrazine-labeled fixed breast cancer cells to achieve cell labeling. Sulfo-Cy5-TCO is used for fluorescent labeling and imaging of biological samples such as proteins and cells .
    Sulfo-Cy5-TCO
  • HY-131338
    RORγt inverse agonist 13
    1 Publications Verification

    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-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-160258

    GDP-Fucose-Am-Tz

    Biochemical Assay Reagents Others
    GDP-Fucose-Tz (GDP-Fucose-Am-Tz) is a non-natural GDP-fucose analog bearing a Tetrazine group. As a precursor, GDP-Fucose-Tz enables the synthesis of GDP-fucose-ssDNA probes via inverse electron demand Diels-Alder reaction. GDP-Fucose-Tz participates in chemoenzymatic reactions to prepare GDP-fucose-Herceptin derivatives through conjugation with TCO-Herceptin .
    GDP-Fucose-Tz
  • 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-175822

    5-HT Receptor Neurological Disease
    5-HT2A inverse agonist-1 is a 5-HT2A receptor inverse agonist with a IC50 of 5.5 nM. 5-HT2A inverse agonist-1 shows minimal hERG inhibition. 5-HT2A inverse agonist-1 can be used for the research of neurological disease, such as Parkinson’s disease .
    5-HT2A inverse agonist-1
  • HY-136100

    ADC Linker Cancer
    TCO-PEG1-Val-Cit-PABC-PNP is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). TCO-PEG1-Val-Cit-PABC-PNP is a click chemistry reagent, which contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups .
    TCO-PEG1-Val-Cit-PABC-PNP
  • HY-136100A

    ADC Linker Cancer
    TCO-PEG1-Val-Cit-PABC-PNP TFA is a cleavable 1 unit PEG ADC linker used in the synthesis of antibody-drug conjugates (ADCs). TCO-PEG1-Val-Cit-PABC-PNP TFA is a click chemistry reagent, which contains a TCO group that can undergo an inverse electron demand Diels-Alder reaction (iEDDA) with molecules containing Tetrazine groups .
    TCO-PEG1-Val-Cit-PABC-PNP TFA
  • 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-157006A

    Biochemical Assay Reagents Others
    TCO-PEG3-NH2 is a click chemistry reagent that contains a TCO group and undergoes the inverse electron-demand Diels-Alder (iEDDA) reaction with tetrazine-containing molecules .
    TCO-PEG3-NH2
  • HY-W012472

    Environmental Pollutants Biochemical Assay Reagents Others
    1,3,5-Triisopropylbenzene is a symmetric aromatic hydrocarbon compound. 1,3,5-Triisopropylbenzene serves as a saturated crosslinker to participate in the "inverse vulcanization" reaction of elemental sulfur. 1,3,5-Triisopropylbenzene acts as a probe molecule to evaluate the external surface acidity and accessibility of zeolite materials. 1,3,5-Triisopropylbenzene is also used as fuel and fuel additive, lubricant and lubricant additive, as well as micelle swelling agent .
    1,3,5-Triisopropylbenzene
  • HY-128604

    ROR Cancer
    XY101 is a potent, selective, metabolically stable and orally available RORγ inverse agonist with an IC50 of 30 nM and a Kd of 380 nM .
    XY101
  • HY-175490

    ROR Inflammation/Immunology
    RORγ inverse agonist 2 (Compound 15) is a potent inverse agonist of the retinoic acid receptor-related orphan receptor RORγ, with IC50 values of 0.4 and 0.9 μM for Gal4-RORγ and full-length RORγ, respectively. RORγ inverse agonist 2 is useful in the study of autoimmune diseases .
    RORγ inverse agonist 2
  • HY-177712

    ROR Inflammation/Immunology
    RORγt inverse agonist 36 (S configuration of Compound 16) is a RORγt inverse agonist. RORγt inverse agonist 36 can be used for the research of inflammation and immunology .
    RORγt inverse agonist 36
  • 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-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-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-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-116521

    PPAR Metabolic Disease
    SR2595 is an inverse agonist of PPARγ with an IC50 of 30 nM .
    SR2595
  • HY-119208

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

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