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Antagonism

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89

Inhibitors & Agonists

1

Fluorescent Dyes

1

Biochemical Assay Reagents

7

Peptides

2

Inhibitory Antibodies

1

Natural
Products

5

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-50674
    INCB3344
    Maximum Cited Publications
    30 Publications Verification

    CCR Inflammation/Immunology Endocrinology
    INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
    INCB3344
  • HY-164535

    AMG 133

    Antibody-Drug Conjugates (ADCs) GLP Receptor Insulin Receptor Metabolic Disease
    Maridebart cafraglutide (AMG 133) is a long-acting peptide-antibody conjugate that combines GLP-1 receptor agonist with glucose-dependent insulinotropic polypeptide (GIP) receptor antagonism. Maridebart cafraglutide shows antagonist activity against human, cynomolgus monkey and rat GIPR with IC50 values of 46.4 nM, 26.5 nM, 822.3 nM, respectively. Maridebart cafraglutide shows agonist activity against human, cynomolgus monkey, rat and mouse GLP-1R with EC50 values of 24.4 pM, 5.7 pM, 2.4 pM and 123 pM, respectively. Maridebart cafraglutide can be used for the study of obesity and type 2 diabetes .
    Maridebart cafraglutide
  • HY-13290
    KN-62
    10+ Cited Publications

    CaMK P2X Receptor Metabolic Disease Cancer
    KN-62 is a selective and reversible inhibitor of calmodulin-dependent protein kinase II (CaMK-II) with a Ki of 0.9 μM for rat brain CaMK-II. KN-62 directly binds to the calmodulin binding site of CaMK-II. KN-62 displays noncompetitive antagonism at P2X7 receptors in HEK293 cells, with an IC50 value of approximately 15 nM.
    KN-62
  • HY-P99643

    UCB6114

    Dan family Cancer
    Ginisortamab (UCB6114) is a fully human IgG4P anti Gremlin-1 monoclonal antibody, with mean IC50 values of 8.2 nM and 9 nM against human and mouse gremlin-1, respectivly. Ginisortamab inhibits gremlin-1 antagonism of BMP signaling pathways. Ginisortamab has the potential for the research of gastrointestinal (GI) tumors .
    Ginisortamab
  • HY-108469
    BI-6015
    5 Publications Verification

    Orphan Nuclear Receptor Metabolic Disease Cancer
    BI-6015 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BI6015 represses insulin promoter activity through HNF4α antagonism. BI-6015 can be used for the research of cancer and diabetes .
    BI-6015
  • HY-16039
    AM095
    10+ Cited Publications

    LPL Receptor Inflammation/Immunology
    AM095 is a selective LPA1 receptor antagonist. The IC50 for AM095 antagonism of LPA-induced calcium flux of human or mouse LPA1-transfected CHO cells is 0.025 and 0.023 μM, respectively.
    AM095
  • HY-101908
    BMS CCR2 22
    1 Publications Verification

    CCR Inflammation/Immunology Endocrinology
    BMS CCR2 22 is a potent, specific and high affinity CC-type chemokine receptor 2 (CCR2) antagonist with excellent binding affinity (binding IC50 of 5.1 nM) and potent functional antagonism (calcium flux IC50 of 18 nM and chemotaxis IC50 of 1 nM) .
    BMS CCR2 22
  • HY-B1901

    (±)-Eperisone hydrochloride

    P2X Receptor Neurological Disease
    Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex .
    Eperisone hydrochloride
  • HY-A0081
    Fluphenazine dihydrochloride
    3 Publications Verification

    Dopamine Receptor SARS-CoV Sodium Channel Neurological Disease Cancer
    Fluphenazine dihydrochloride is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine dihydrochloride blocks neuronal voltage-gated sodium channels. Fluphenazine dihydrochloride acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine dihydrochloride can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine dihydrochloride can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
    Fluphenazine dihydrochloride
  • HY-119980
    Fluphenazine
    3 Publications Verification

    Sodium Channel Dopamine Receptor SARS-CoV Infection Neurological Disease Cancer
    Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
    Fluphenazine
  • HY-113906A

    GHSR Metabolic Disease
    (αR,8aS)-GSK1614343 is the isomer of GSK1614343 (HY-113906). GSK1614343 is the potent antagonist of growth hormone secretagogues type 1a (GHS1a) receptors .
    (αR,8aS)-GSK1614343
  • HY-136299
    Sepimostat
    2 Publications Verification

    FUT-187 free base

    iGluR Neurological Disease
    Sepimostat (FUT-187 free base) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat inhibits the Ifenprodil binding with a Ki value of 27.7?μM .
    Sepimostat
  • HY-P1812
    AUNP-12
    3 Publications Verification

    NP-12

    PD-1/PD-L1 Cancer
    AUNP-12 (NP-12) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
    AUNP-12
  • HY-P10571

    Melanocortin Receptor Metabolic Disease
    GPS1573 is a noncompetitive antagonist of melanocortin type 2 receptor (MC2R) that dose-dependently antagonizes ACTH-stimulated MC2R activity (IC50=66 nM). GPS1573 can be used in the study of Cushing's disease due to its highly selective antagonism of MC2R .
    GPS1573
  • HY-U00051

    Histamine Receptor Dopamine Receptor Neurological Disease
    Propiomazine is an orally active antihistamine agent. Propiomazine is a potent prolactin (PRL) release stimulant, whose effect depends on the antagonism of the dopaminergic system and can inhibit the secretion of luteinizing hormone (LH). Propiomazine is mainly used for anesthesia assistance, mental disorders and anxiety-induced sedation, and can also be used in research related to insomnia .
    Propiomazine
  • HY-13499

    CCR2 antagonist 5

    CCR Inflammation/Immunology
    JNJ-41443532 (CCR2 antagonist 5) is a selective, orally active hCCR2 inhibitor with good binding affinity (IC50=37 nM) and potent functional antagonism (chemotaxis IC50=30 nM). JNJ-41443532 displays a Ki of 9.6 µM for mCCR2 binding. JNJ-41443532 can be used in the research of inflammatory disease .
    JNJ-41443532
  • HY-151481

    FXR Metabolic Disease
    FXR antagonist 1 (compound F6) is an orally active and selective intestinal FXR antagonist (IC50=2.1 μM). FXR antagonist 1 selectively inhibits intestinal FXR signalling through antagonism of intestinal FXR and feedback activation of hepatic FXR to improve hepatic steatosis, inflammation and fibrosis in NASH (nonalcoholic steatohepatitis) models. FXR antagonist 1 can be used in NASH studies .
    FXR antagonist 1
  • HY-142066

    PKA ERK iGluR Neurological Disease
    4′-Demethylnobiletin is a bioactive metabolite that activates the PKA/ERK/CREB signaling pathway, enhances CRE-mediated transcription in hippocampal neurons, and reverses memory impairment associated with NMDA receptor antagonism by stimulating ERK signaling .
    4′-Demethylnobiletin
  • HY-117694

    CGRP Receptor Neurological Disease Inflammation/Immunology
    MK-8825 is an orally active, selective CGRP receptor antagonist with a Ki value of 47 pM for human CGRP receptors and 17 nM for rat CGRP receptors. MK-8825 blocks CGRP-stimulated cAMP responses and exhibits competitive-like antagonism. MK-8825 can be used in the research of migraine and temporomandibular joint disorders .
    MK-8825
  • HY-101725

    Ro 11-3128; Ro 11-3128/002

    Parasite Infection Neurological Disease
    Meclonazepam (Ro 11-3128) is a benzodiazepine compound with anxiolytic effect . Meclonazepam is active against immature S. mansoni. Meclonazepam (30 μM) eliminates 100% of immature parasites. Meclonazepam has a anti-schistosomal effect .
    Meclonazepam
  • HY-B1901R

    (±)-Eperisone hydrochloride (Standard)

    P2X Receptor Reference Standards Neurological Disease
    Eperisone (hydrochloride) (Standard) is the analytical standard of Eperisone (hydrochloride). This product is intended for research and analytical applications. Eperisone Hydrochloride ((±)-Eperisone hydrochloride) is an orally active antispastic agent with a vasodilator effect, used for the research of muscle stiffness and pain. Eperisone Hydrochloride is a potent and selectively P2X7 receptor antagonist, also shows antagonism for human P2X3. Eperisone Hydrochloride works by relaxing both skeletal muscles and vascularsmooth muscles, demonstrating a variety of effects such as reduction ofmyotonia, improvement of circulationand and suppression of the pain reflex .
    Eperisone hydrochloride (Standard)
  • HY-P991673

    LuAG13909

    Androgen Receptor Inflammation/Immunology
    Asedebart is a CHO-expressed human antibody that targets Adrenocorticotropic hormone (ACTH). Asedebart blocks the binding of ACTH to its receptor through antagonism. Asedebart has huIgG1 heavy chain and huκ light chain, with a predicted molecular weight (MW) of 145 kDa. The isotype control for Asedebart can refer to Human IgG1 kappa, Isotype Control (HY-P99001). Asedebart can be used for inflammatory diseases such as psoriasis and ulcerative colitis research .
    Asedebart
  • HY-77111
    cis-INCB3344
    1 Publications Verification

    CCR Drug Isomer Inflammation/Immunology Endocrinology
    cis-INCB3344 is the isomer of INCB3344 (HY-50674), and can be used as an experimental control. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity.
    cis-INCB3344
  • HY-N7740

    P2Y Receptor Endogenous Metabolite Others
    Adenosine 2',5'-diphosphate sodium is a competitive P2Y1 antagonist. Adenosine 2',5'-diphosphate sodium exhibits non-selective antagonism at recombinant and human platelet P2X1 receptors .
    Adenosine 2',5'-diphosphate sodium
  • HY-121037

    EGM1

    Phosphodiesterase (PDE) Cancer
    Eggmanone (EGM1) is a potent and selective phosphodiesterase 4 (PDE4) antagonist with an IC50 of 72 nM for PDE4D3. Eggmanone shows approximately 40- to 50-fold selective for PDE4D3 over other PDEs. Eggmanone exerts its Hh-inhibitory effects through selective antagonism of PDE4, leading to protein kinase A activation and subsequent Hh blockade .
    Eggmanone
  • HY-135439

    5-HT Receptor Neurological Disease
    SB-203186 is a highly selective 5-HT4 receptor antagonist. SB-203186 exhibits a potent competitive antagonistic effect, with its pKB value being 8.3 in the isolated right atrium model of piglets. SB-203186 can dose-dependently shift the 5-HT-induced tachycardia curve to the right, and does not inhibit the maximum response. SB-203186 is an efficient 5-HT₄ antagonist in pig and human atria, but has no significant inhibitory effect in rat atria. SB-203186 can be used for the study of diseases such as arrhythmias and abnormal myocardial contraction .
    SB-203186
  • HY-135447

    Prostaglandin Receptor Others
    BM-531 is a dual-acting agent for thromboxane receptor (TXA2) antagonism and thromboxane synthase inhibition. BM-531 exerts anti-aggregatory effects on human citrated platelet-rich plasma (PRP), inhibiting Arachidonic acid (HY-109590A)-induced aggregation with an ED100 of 0.125 μM and U-46619 (HY-108566)-induced aggregation with an ED50 of 0.482 μM. BM-531 inhibits high-K +-induced contraction of porcine uterine smooth muscle .
    BM-531
  • HY-119980S

    Isotope-Labeled Compounds Sodium Channel Dopamine Receptor SARS-CoV Others
    Fluphenazine-d8 is the deuterium labeled Fluphenazine. Fluphenazine is a potent, orally active phenothiazine-based dopamine receptor antagonist. Fluphenazine blocks neuronal voltage-gated sodium channels. Fluphenazine acts primarily through antagonism of postsynaptic dopamine-2 receptors in mesolimbic, nigrostriatal, and tuberoinfundibular neural pathways. Fluphenazine can antagonize Methylphenidate-induced stereotyped gnawing and inhibit climbing behaviour in mice. Fluphenazine can be used for researching psychosis and painful peripheral neuropathy associated with diabetes and has potential to inhibit SARS-CoV-2 .
    Fluphenazine-d8
  • HY-P5175

    mAChR Neurological Disease
    Muscarinic toxin 7 is a peptide toxin with selective and noncompetitive antagonism at the muscarinic M1 receptor .
    Muscarinic toxin 7
  • HY-125839

    Glucocorticoid Receptor Inflammation/Immunology Endocrinology
    OP-3633 is a potent and selective steroidal glucocorticoid receptor (GR) antagonist with an IC50 of 29 nM, with inhibition of GR transcriptional activity. OP-3633 exhibits low progesterone receptor (PR) agonism and androgen receptor (AR) antagonism .
    OP-3633
  • HY-136299A

    FUT-187

    iGluR Neurological Disease
    Sepimostat dimethanesulfonate (FUT-187) exhibits neuroprotective activity via NR2B N-methyl-D-aspartate receptor antagonism at the Ifenprodil-binding site of the NR2B subunit. Sepimostat dimethanesulfonate inhibits the Ifenprodil binding with a Ki value of 27.7 µM .
    Sepimostat dimethanesulfonate
  • HY-119971

    Nuclear Hormone Receptor 4A/NR4A Metabolic Disease Cancer
    BIM5078 is a hepatocyte nuclear factor 4α (HNF4α) antagonist that can inhibit the expression of known HNF4α target genes. BIM5078 represses insulin promoter activity through HNF4α antagonism. BIM5078 can be used for the research of cancer and diabetes .
    BIM5078
  • HY-171012

    NSC 335504

    STING Inflammation/Immunology
    Clonixeril (NSC 335504) is a non-nucleotide hSTING modulator. Clonixeril has weak agonist activity at micromolar concentrations and results in antagonism of the hSTING WT pathway at low femtomolar (10 -15 M) and in some cases even attomolar (10 -18 M) concentrations. Clonixeril reduces hSTING oligomerization at a concentration of 1 aM-1 pM .
    Clonixeril
  • HY-156734

    SARS-CoV Virus Protease Infection
    D-4-77 is a potent inhibitor of SARS-CoV-2 Mpro with an IC50 value of 0.95 μM. D-4-77 has antiviral active with an EC50 value of 0.49 μM. D-4-77 suppresses SARS-CoV-2 Mpro -induced antagonism of the host NF-κB innate immune response .
    D-4-77
  • HY-148038

    5-HT Receptor Neurological Disease
    5-HT3 antagonist 5 is a quinoxalin-2-carboxamide compound, a 5-HT3 receptor antagonist. 5-HT3 antagonist 5 exerts antagonism on 5-HT3 agonist and 2-methyl-5-HT, and shows anti-depressant effect in mice .
    5-HT3 antagonist 5
  • HY-P1812A
    AUNP-12 TFA
    3 Publications Verification

    NP-12 TFA

    PD-1/PD-L1 Cancer
    AUNP-12 TFA (NP-12 TFA) is a peptide antagonist of the PD-1 signaling pathway, displays equipotent antagonism toward PD-L1 and PD-L2 in rescue of lymphocyte proliferation and effector functions. AUNP-12 TFA exhibits immune activation, excellent antitumor activity, and potential for better management of immune-related adverse events (irAEs) .
    AUNP-12 TFA
  • HY-144286

    CXCR Infection
    CXCR4 antagonist 3 (compound 12a) is a potent antagonist of CXCR4 with an IC50 of 11 nM. CXCR4 antagonist 3 is a congener of TIQ15. CXCR4 antagonist 3 demonstrates the best overall properties including CXCR4 antagonism, CYP 2D6 inhibition, metabolic stability, and permeability. CXCR4 antagonist 3 has the potential for the research of human immunodeficiency virus .
    CXCR4 antagonist 3
  • HY-144607

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 2 (compound 25) is a potent, selective and blood-brain barrier (BBB) penetrant μ opioid receptor (MOR) antagonist with a Ki of 0.37 nM and an EC50 of 0.44 nM. Mu opioid receptor antagonist 2 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 2 can be used for researching opioid use disorders (OUD) .
    Mu opioid receptor antagonist 2
  • HY-144609

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 4 (compound 31) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.38 nM and an EC50 of 1.07 nM. Mu opioid receptor antagonist 4 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 4 Mu opioid receptor antagonist 4 can be used for researching opioid use disorders (OUD) .
    Mu opioid receptor antagonist 4
  • HY-101317A

    SB-205607

    Opioid Receptor Metabolic Disease
    TAN-67 (SB-205607) is a non-peptidic delta-opioid receptor agonist that exhibits significant antinociceptive activity in both diabetic and non-diabetic mice. TAN-67 demonstrates a marked and dose-dependent reduction in acetic acid-induced abdominal constrictions, with a notably stronger effect in diabetic mice compared to their non-diabetic counterparts. TAN-67's antinociceptive properties are primarily mediated through the activation of delta 1-opioid receptors, as indicated by the pronounced antagonism observed upon administration of a selective delta 1-opioid receptor antagonist.
    TAN-67
  • HY-112740

    Leukotriene Receptor Inflammation/Immunology
    SC-53228 is an orally active human leukotriene B4 receptor (LTB4 receptor) antagonist. SC-53228 exerts its anti-inflammatory effect by specifically blocking the LTB4 receptor and inhibiting neutrophil infiltration. SC-53228 has demonstrated significant efficacy and good safety in various inflammatory models. SC-53228 can be used for a variety of inflammatory diseases, such as psoriasis and ulcerative colitis .
    SC-53228
  • HY-149387

    Dopamine Receptor Opioid Receptor Inflammation/Immunology
    D3R/MOR antagonist 2 (Compound 121) is a D3R/MOR antagonist (Ki: 361 nM and 85.2 nM respectively). D3R/MOR antagonist 2 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
    D3R/MOR antagonist 2
  • HY-149386

    Dopamine Receptor Opioid Receptor Inflammation/Immunology
    D3R/MOR antagonist 1 (Compound 114) is a D3R/MOR antagonist (Ki: 46.5 nM and 691 nM respectively). D3R/MOR antagonist 1 has the potential to produce analgesic effects through MOR partial agonism, reduce opioid-misuse liability via D3R antagonism .
    D3R/MOR antagonist 1
  • HY-19012

    Adrenergic Receptor Cardiovascular Disease
    N-1518 is an α and β adrenergic receptor blocker that has competitive antagonism against β1 and α1 receptors, but does not show selectivity for β1 receptors, but shows about 20-fold selectivity for α1 receptors. N-1518 has vasodilatory effects and can be used in the research field of hypertension treatment .
    N-1518
  • HY-120810

    DDP-225 hydrate hydrochloride

    5-HT Receptor Neurological Disease
    MCI-225 (DDP-225) hydrate hydrochloride is a selective and orally active noradrenaline (NA) reuptake inhibitor with 5-HT3 receptor antagonism. MCI-225 hydrate hydrochloride has antidepressant-like and anxiolytic-like properties. MCI-225 hydrate hydrochloride can be used for the study of anxiety disorder .
    MCI-225 hydrate hydrochloride
  • HY-120301

    Oxytocin Receptor Endocrinology
    L-366682, a cyclic hexapeptide, possesses antagonism of oxytocin .
    L-366682
  • HY-50674A

    CCR Inflammation/Immunology
    INCB3344 R-isomer is the R-isomer of INCB3344. INCB3344 is a potent, selective and orally bioavailable CCR2 antagonist with IC50 values of 5.1 nM (hCCR2) and 9.5 nM (mCCR2) in binding antagonism and 3.8 nM (hCCR2) and 7.8 nM (mCCR2) in antagonism of chemotaxis activity .
    INCB3344 R-isomer
  • HY-159080

    Parasite Infection
    HgCht2-IN-1 (compound 1516b) is a HgCht2 inhibitor that successfully inhibits the antagonism of cyst nematodes against nitrogen-fixing rhizobia and phosphate-absorbing arbuscular mycorrhizal symbionts. HgCht2-IN-1 can be used in the study of cyst nematode antagonism against microbial symbionts .
    HgCht2-IN-1
  • HY-115844

    Opioid Receptor Endogenous Metabolite Neurological Disease
    LY-99335 is an anesthetic antagonist with behavioral inhibitory activity. LY-99335 exhibits large dose separation at specific doses, indicating its potential in anesthetic antagonism .
    LY-99335
  • HY-124910

    Histamine Receptor Adrenergic Receptor Cardiovascular Disease
    BU-E-75 is a guanidine-type H2 receptor agonist that exhibits antagonism at postsynaptic α-adrenoceptors, which can relax the noradrenaline-precontracted vessels .
    BU-E-75

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