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Antagonism

" in MedChemExpress (MCE) Product Catalog:

60

Inhibitors & Agonists

6

Peptides

1

Natural
Products

2

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13290
    KN-62
    5+ 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-50674
    INCB3344
    Maximum Cited Publications
    22 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-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-77111

    Others 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-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-120301

    Oxytocin Receptor Endocrinology
    L-366682, a cyclic hexapeptide, possesses antagonism of oxytocin .
    L-366682
  • 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-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-120188

    PPAR Others
    CC618 is a selective peroxisome proliferator-activated receptor (PPARβ/δ) antagonist that exhibits antagonism by covalently binding to PPARβ/δ receptors .
    CC618
  • 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
  • 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-136880

    Sgd 195/78

    5-HT Receptor Cardiovascular Disease
    Flufylline shows antihypertensive properties in spontaneously hypertensive rats and display antagonism towards 5-HT receptors in various animal models. Flufylline can be used for cardiovascular disease research .
    Flufylline
  • HY-164128

    Others Others
    AHL modulator-1 (compound 12) is a modulator of N-acylated L-homoserine lactone (AHL), with the agonism and antagonism of 21% and 42% in cellulase activity and 5% and 32% in potato macerationa, respectively .
    AHL modulator-1
  • HY-W650803

    A-57219

    Adrenergic Receptor Cardiovascular Disease
    Nemazoline (A-57219) is selective α-adrenergic agent with α1-agonist/α2-antagonist activity, which is used as a nasal decongestant. Nemazoline produces decongestion by α1-mediated contraction of capacitance vessels, but not compromises blood flow by virtue of α2-antagonism. Nemazoline also blocks endogenous noradrenaline-mediated α 2-constriction of the resistance vessels .
    Nemazoline
  • HY-163703

    Dopamine Receptor Neurological Disease
    D4R antagonist-2 (compound 33) is a D4R antagonist. D4R antagonist-2 has a IC50 value of 210 nM, and a Ki value of 59 nM for D4R. D4R antagonist-2 can be used in the Parkinson's disease research .
    D4R antagonist-2
  • 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-16039
    AM095
    5+ 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-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-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-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-P0262A

    Neuropeptide Y Receptor Neurological Disease Metabolic Disease
    Galantide TFA is a reversible and non-specific galanin (GAL) receptor antagonist. Galantide TFA dose-dependently shows antagonism to galanin-induced K + conductance with an IC50 value of 4 nM. Galantide TFA can be used for the research of neurological disease and hormone metabolism research .
    Galantide TFA
  • HY-161896

    Others Neurological Disease
    Transcription factor-IN-1 (Compound 4e) is an inhibitor for transcription factor. Transcription factor-IN-1 exhibits anticonvulsant activity by antagonism with pentylenetetrazole (PTZ) (ED50 =34.5 mg/kg). Transcription factor-IN-1 exhibits antidepressant effects in rat models .
    Transcription factor-IN-1
  • HY-101908

    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-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-161273

    TRP Channel Neurological Disease
    TRPV1 antagonist 6 (compound 51) is a mode-selective antagonist for transient receptor potential vanilloid member 1 (TRPV1), which shows antagonism with IC50 of 2.85 nM to capsaicin activation and 28.48 % inhibition against proton activation at a 3 µM concentration .
    TRPV1 antagonist 6
  • HY-117881

    Opioid Receptor Neurological Disease
    CJ-15208 is a potent and selective κ-opioid receptor antagonist with significant opioid activity. CJ-15208 exhibited strong analgesic effects in the warm water tail withdrawal test in mice and was mediated through multiple opioid receptors. The stereoisomers of CJ-15208 exhibited different opioid activity characteristics, for example, one stereoisomer exhibited κ-opioid receptor antagonism, while the other exhibited δ-opioid receptor antagonism. All stereoisomers of CJ-15208 had no significant effects on respiration. The stereoisomers of CJ-15208 did not lead to the development of drug tolerance, which makes it potential in the further development of safe opioid analgesics .
    CJ-15208
  • HY-136299
    Sepimostat
    1 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-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-W424730

    Others Others
    HA-966 hydrochloride is a glycine site antagonist of the NMDA receptor, exhibiting non-competitive antagonism on NMDA responses. HA-966 hydrochloride effectively blocks the enhancement of NMDA responses by glycine in a competitive manner. HA-966 hydrochloride plays a significant role in mediating the antagonist action at the glycine modulatory site of the NMDA receptor.
    HA-966 hydrochloride
  • HY-108469
    BI-6015
    3 Publications Verification

    Orphan 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-P10571

    Melanocortin Receptor Endocrinology
    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-155706

    Opioid Receptor Dopamine Receptor Inflammation/Immunology
    MOR agonist-2 (compound 46) is a antagonist of D3R and agonist of MOR (Ki: 7.26 nM and 564 nM, respectively). MOR agonist-2 has the potential to produce analgesic effects through MOR partial agonism. MOR agonist-2 reduces opioid-misuse liability via D3R antagonism .
    MOR agonist-2
  • 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-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-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-144608

    Opioid Receptor Neurological Disease
    Mu opioid receptor antagonist 3 (compound 26) is a potent and selective μ opioid receptor (MOR) antagonist with a Ki of 0.24 nM and an EC50 of 0.54 nM. Mu opioid receptor antagonist 3 has remarkable CNS antagonism against morphine, and precipitated fewer withdrawal symptoms than Naloxone. Mu opioid receptor antagonist 3 can be used for researching opioid use disorders (OUD) .
    Mu opioid receptor antagonist 3
  • 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-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-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-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-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-B1901

    (±)-Eperisone hydrochloride

    Others 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-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-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-107564

    VUF 4702 dihydrobromide

    Histamine Receptor Inflammation/Immunology
    Impentamine dihydrobromide (VUF 4702 dihydrobromide) is a histamine H3 receptor antagonist with potential antihistamine activity. Impentamine dihydrobromide shows the strongest selective H3 antagonism among a series of 4(5)-(ω-aminoalkyl)-1H-imidazole compounds. The pA2 value of impentamine dihydrobromide is 8.4, showing its high efficacy in guinea pig jejunum. Impentamine dihydrobromide has a specific antagonistic binding site with the H3 receptor .
    Impentamine dihydrobromide
  • HY-A0081
    Fluphenazine dihydrochloride
    1 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

    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

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