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Allosteric antagonists

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48

Inhibitors & Agonists

3

Isotope-Labeled Compounds

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-145684
    EP2 receptor antagonist-1

    		Prostaglandin Receptor Inflammation/Immunology
    EP2 receptor antagonist-1 (compound 1) is a potent, reversible, and agonist dependent allosteric prostaglandin EP2 receptor antagonist. EP2 receptor antagonist-1 shows anti-inflammatory effects .
    EP2 receptor antagonist-1
  • HY-129946
    Dopamine D2 receptor antagonist-1

    		Dopamine Receptor Neurological Disease
    Dopamine D2 receptor antagonist-1 is a negative allosteric modulator (NAM) of the dopamine D2 receptor (D2R) with sub-mM affinity .
    Dopamine D2 receptor antagonist-1
  • HY-50081
    CCR2-RA-[R]
    4 Publications Verification

    		 CCR Inflammation/Immunology Endocrinology
    CCR2-RA-[R] is an allosteric antagonist of the C-C chemokine receptor type 2 (CCR2) with an IC50 of 103 nM.
    CCR2-RA-[R]
  • HY-123617
    AZ8838

    		Protease Activated Receptor (PAR) Inflammation/Immunology
    AZ8838 is a potent, competitive, allosteric, orally active non-peptide small molecule antagonist of PAR2 with a pKi of 6.4 for hPAR2 .
    AZ8838
  • HY-19904
    Adomeglivant
    4 Publications Verification

    LY2409021

    		 GCGR Metabolic Disease
    Adomeglivant (LY2409021) is a potent, selective glucagon receptor (GluR) allosteric antagonist. Adomeglivant is widely used in the research for type 2 diabetes mellitus .
    Adomeglivant
  • HY-133555
    mGluR2 antagonist 1

    		mGluR Neurological Disease
    mGluR2 antagonist 1 is a highly potent, orally bioavailable and selective class of mGluR2 negative allosteric modulator (IC50 of 9 nM) with excellent brain permeability .
    mGluR2 antagonist 1
  • HY-19519A
    Ladarixin sodium
    1 Publications Verification

    DF 2156A

    		 CXCR Infection Inflammation/Immunology Cancer
    Ladarixin sodium (DF 2156A) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin sodium can be used for the research of COPD and asthma .
    Ladarixin sodium
  • HY-110179
    PSNCBAM-1

    		Cannabinoid Receptor Metabolic Disease
    PSNCBAM-1 is a selective CB1 receptor allosteric antagonist with an EC50 of 0.1 μM. PSNCBAM-1 can be used in the researches of obesity .
    PSNCBAM-1
  • HY-100979
    W-84 dibromide

    HDMPPA

    		 mAChR Others
    W-84 (dibromide) is a potent allosteric modulator of M2-cholinoceptors, which retards [ 3H]N-methylscopolamine dissociation. W-84 dibromide can stabilize cholinergic antagonist-receptor complexes. W-84 (dibromide) is a non-competitive muscarinic acetylcholine receptors antagonist with allosteric effects. W-84 (dibromide) protects over additively against an organophosphate-intoxication when applied in combination with atropine .
    W-84 dibromide
  • HY-121094
    Androgen receptor allosteric antagonist 1

    		Estrogen Receptor/ERR Cancer
    Androgen receptor allosteric antagonist 1(compound D36)is a a llosteric, competitive androgen receptor (AR) antagonist with the Ki of 9 μM. Androgen receptor allosteric antagonist 1 inhibits R1881-mediated transcription and proliferation and can be used for study of prostate cancer .
    Androgen receptor allosteric antagonist 1
  • HY-100405
    FTIDC

    		mGluR Neurological Disease
    FTIDC is an orally active, noncompetitive, selective allosteric metabotropic glutamate receptor (mGluR) 1 antagonist with an IC50 of 5.8 nM for human mGluR1a. FTIDC has no species differences in its antagonistic activity on recombinant human, mouse, and rat mGluR1 .
    FTIDC
  • HY-19519
    Ladarixin
    1 Publications Verification

    DF 2156A free base

    		 CXCR Inflammation/Immunology Cancer
    Ladarixin (DF 2156A free base) is an orally active, allosteric non-competitive and dual CXCR1 and CXCR2 antagonist. Ladarixin can be used for the research of COPD and asthma .
    Ladarixin
  • HY-119217
    AZ084
    2 Publications Verification

    		 CCR Inflammation/Immunology Endocrinology Cancer
    AZ084 is a potent, selective, allosteric and oral active CCR8 allosteric antagonist, with a Ki of 0.9 nM. Has potential to treat asthma . AZ084 restrains the formation of the immunologically tolerant pre-metastatic niche (PMN) and tumor cells metastasis in lung by downregulating Treg differentiation. AZ084 can be used in studies of asthma and cancer .
    AZ084
  • HY-112874
    BMS-681

    		CCR Neurological Disease Inflammation/Immunology Cancer
    BMS-681 is an orthosteric antagonist of CC chemokine receptor 2 (CCR2). BMS-681 restricts the movement of the extracellular end of TM6 by stabilizing TM7. TM7 and TM6 are the main components of the orthosteric binding site. BMS-681 can be used to study inflammatory neurodegenerative diseases and cancer .
    BMS-681
  • HY-139202
    XVA143

    		Integrin Inflammation/Immunology
    XVA143, an α/β I-like allosteric antagonist, inhibits LFA-1 dependent firm adhesion, while at the same time it enhances adhesion in shear flow and rolling both in vitro and in vivo .
    XVA143
  • HY-13848
    AZD8797
    10+ Cited Publications

    KAND567

    		 CX3CR1 CXCR Inflammation/Immunology Endocrinology Cancer
    AZD8797 (KAND567) is an allosteric non-competitive and orally active antagonist of the human CX3CR1 receptor; antagonizes CX3CR1 and CXCR2 with Kis of 3.9 and 2800 nM, respectively .
    AZD8797
  • HY-118238
    Remeglurant

    MRZ-8456

    		 mGluR Neurological Disease
    Remeglurant (MRZ-8456) acts as a selective, orally active and allosteric antagonist of the mGlu5 receptor, with an IC50 of 13 nM. Remeglurant (MRZ-8456) can be used in the research for dyskinesia in Parkinson’s disease (PD) .
    Remeglurant
  • HY-118967
    VUANT1

    VU0183254

    		 HCN Channel Others
    VUANT1 (VU0183254) is an allosteric antagonist of insect odorant receptor ion channels, which has the activity of inhibiting insect odorant receptor signaling. VUANT1 can inhibit the activation of insect odorant receptors through allosteric regulation, which is important for the study of the molecular mechanism of insect olfactory signaling. Although it may be of limited use in insect control programs, it can be used as a pharmacological tool to study related mechanisms.
    VUANT1
  • HY-13831
    BPTU

    BMS-646786

    		 P2Y Receptor Neurological Disease Cancer
    BPTU (BMS-646786) is a non-nucleotide P2Y1 receptor allosteric antagonist with antithrombotic activity. BPTU is able to block the P2Y1 receptor located at the neuromuscular junction of the gastrointestinal tract .
    BPTU
  • HY-110237
    BX430

    		P2X Receptor Calcium Channel Cardiovascular Disease
    BX430 is a potent and selective noncompetitive allosteric human P2X4 receptor channels antagonist with an IC50 of 0.54 μM. BX430 has species specificity. BX430 is used for chronic pain and cardiovascular disease.
    BX430
  • HY-118356
    WIN 62,577

    		Neurokinin Receptor mAChR Neurological Disease
    WIN 62,577 is a rat-specific, but non-human, NK1 receptor antagonist. WIN 62,577 interacts with M1-M4 mAChRs and is an allosteric enhancer of acetylcholine affinity targeting the M3 receptor.
    WIN 62,577
  • HY-103556
    YM-202074 fumarate

    		mGluR Neurological Disease
    YM-202074 fumarate is a selective, allosteric metabotropic glutamate receptor type 1 (mGluR1) antagonist with high affinity and neuroprotective properties in vivo. YM-202074 fumarate binds to the allosteric site of rat mGluR1 with a Ki value of 4.8 nM. YM-202074 fumarate also inhibits mGluR1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 value of 8.6 nM. YM-202074 fumarate can be used in stroke research .
    YM-202074 fumarate
  • HY-10198
    Navarixin
    20+ Cited Publications

    SCH 527123; MK-7123

    		 CXCR Inflammation/Immunology Endocrinology Cancer
    Navarixin (SCH 527123) is a potent, allosteric and orally active antagonist of both CXCR1 and CXCR2, with Kd values of 41 nM for cynomolgus CXCR1 and 0.20 nM, 0.20 nM, 0.08 nM for mouse, rat and cynomolgus monkey CXCR2, respectivelly .
    Navarixin
  • HY-10046
    Plerixafor
    Maximum Cited Publications
    67 Publications Verification

    AMD 3100; JM3100; SID791

    		 CXCR HIV Infection Inflammation/Immunology Endocrinology Cancer
    Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM .
    Plerixafor
  • HY-103111
    MMPIP hydrochloride

    		mGluR Neurological Disease
    MMPIP hydrochloride is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP hydrochloride acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP hydrochloride alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .
    MMPIP hydrochloride
  • HY-107503
    MMPIP

    		mGluR Neurological Disease
    MMPIP is an allosteric metabotropic glutamate receptor 7 (mGluR7) selective antagonist (KB values 24 -30 nM). MMPIP acts as a pharmacological tool for elucidating the roles of mGluR7 on central nervous system functions. MMPIP alleviates pain and normalizes affective and cognitive behavior in neuropathic mice .
    MMPIP
  • HY-50688
    SB-265610
    2 Publications Verification

    		 CXCR Inflammation/Immunology
    SB-265610 is a selective, competitive, nonpeptide and allosteric CXCR2 antagonist. SB-265610 blocks rat cytokine-induced neutrophil chemoattractant-1 (CINC-1)-induced calcium mobilization and neutrophil chemotaxis with IC50s of 3.7 nM and 70 nM, respectively .
    SB-265610
  • HY-B0520A
    Benztropine mesylate
    5 Publications Verification

    Benzatropine mesylate; Benzotropine mesylate; Benztropine methanesulfonate

    		 Dopamine Receptor mAChR Histamine Receptor Neurological Disease Cancer
    Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
    Benztropine mesylate
  • HY-133073
    CCR7 Ligand 1

    CCR7-Cmp2105

    		 CCR Ligands for Target Protein for PROTAC Cancer
    CCR7 Ligand 1 (CCR7-Cmp2105) is an allosteric Ligand and antagonist for human CC chemokine receptor 7 (CCR7) with a Kd of 3 nM. CCR7 Ligand 1, thiadiazole-dioxide ligan, suppresses arrestin binding in response to activation by CCL19 with an IC50 of 7.3 μM .
    CCR7 Ligand 1
  • HY-B0520
    Benztropine

    Benzatropine; Benzotropine

    		 Dopamine Receptor mAChR Histamine Receptor Cancer
    Benztropine (Benzatropine; Benzotropine) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research . Benztropine is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
    Benztropine
  • HY-15445
    CTEP
    2 Publications Verification

    RO 4956371; mGluR5 inhibitor

    		 mGluR Neurological Disease
    CTEP (RO 4956371) is a novel, long-acting, orally bioavailable allosteric antagonist of mGlu5 receptor with IC50 of 2.2 nM, and shows > 1000-fold selectivity over other mGlu receptors. CTEP is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    CTEP
  • HY-10046S
    Plerixafor-d4

    		Isotope-Labeled Compounds CXCR HIV Infection Inflammation/Immunology Endocrinology Cancer
    Plerixafor-d4 is the deuterium labeled Plerixafor. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM[1][2][3][4][7].
    Plerixafor-d4
  • HY-10046R
    Plerixafor (Standard)

    		CXCR HIV Infection Inflammation/Immunology Endocrinology Cancer
    Plerixafor (Standard) is the analytical standard of Plerixafor. This product is intended for research and analytical applications. Plerixafor (AMD 3100) is a selective CXCR4 antagonist with an IC50 of 44 nM. Plerixafor, an immunostimulant and a hematopoietic stem cell (HSC) mobilizer, is an allosteric agonist of CXCR7. Plerixafor inhibits HIV-1 and HIV-2 replication with an EC50 of 1-10 nM .
    Plerixafor (Standard)
  • HY-15469
    GW791343 dihydrochloride

    		P2X Receptor Neurological Disease
    GW791343 dihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 dihydrochloride can enhance ATP rhythm. GW791343 dihydrochloride can be used in study of neurological disease .
    GW791343 dihydrochloride
  • HY-15470
    GW791343 trihydrochloride

    		P2X Receptor Neurological Disease
    GW791343 trihydrochloride is a potent human P2X7 receptor negative allosteric modulator (exhibits species-specific activity), produces a non-competitive antagonist effect on human P2X7 receptor, with a pIC50 of 6.9-7.2. GW791343 trihydrochloride can enhance ATP rhythm. GW791343 trihydrochloride can be used in study of neurological disease .
    GW791343 trihydrochloride
  • HY-B0520AR
    Benztropine (mesylate) (Standard)

    Benzatropine mesylate (Standard); Benzotropine mesylate (Standard); Benztropine methanesulfonate (Standard)

    		 Dopamine Receptor mAChR Histamine Receptor Neurological Disease Cancer
    Benztropine (mesylate) (Standard) is the analytical standard of Benztropine (mesylate). This product is intended for research and analytical applications. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects .
    Benztropine (mesylate) (Standard)
  • HY-B0520AS1
    Benztropine-d3 mesylate

    		Dopamine Receptor Histamine Receptor mAChR Cancer
    Benztropine-d3 (mesylate) is the deuterium labeled Benztropine mesylate[1]. Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[2][3].
    Benztropine-d3 mesylate
  • HY-116723
    CFMMC

    		mGluR Neurological Disease
    CFMMC is a selective allosteric metabotropic glutamate receptor 1 (mGluR1) antagonist. CFMMC inhibits L-glutamate-induced intracellular Ca 2+ mobilization ([Ca 2+]i) in Chinese hamster ovary cells expressing recombinant human mGluR1a with an IC50 value of 50 nM. CFMMC is promising for research of various central nervous system disorders, such as schizophrenia, epilepsy, anxiety, pain, cognitive dysfunction and drug abuse .
    CFMMC
  • HY-110152
    LSN2463359

    		mGluR Neurological Disease
    LSN2463359 is positive allosteric modulator of metabotropic glutamate 5 (mGlu5). LSN2463359 attenuates aspects of the behavioral response to administration of the competitive NMDA receptor antagonist. LSN2463359 selectively attenuates reversal learning deficits observed in the neurodevelopmental MAM E17 model . LSN2463359 is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
    LSN2463359
  • HY-B0520AS
    Benztropine-13C,d3 mesylate

    		Isotope-Labeled Compounds Dopamine Receptor mAChR Histamine Receptor Neurological Disease Cancer
    Benztropine- 13C,d3 (mesylate) is the 13C- and deuterium labeled Benztropine (mesylate). Benztropine mesylate (Benzatropine mesylate) is an orally active centrally acting anticholinergic agent that can be used for Parkinson's disease research. Benztropine mesylate is an anti-histamine agent and a dopamine re-uptake inhibitor. Benztropine mesylate is also a human D2 dopamine receptor allosteric antagonist. Benztropine mesylate also has anti-CSCs (cancer stem cells) effects[1][2].
    Benztropine-13C,d3 mesylate
  • HY-129636A
    (E/Z)-CLH304a

    GABAB receptor antagonist 1

    		 GABA Receptor ERK Neurological Disease
    (E/Z)-CLH304a (GABAB receptor antagonist 1) is a mixture of (E)-CLH304a and (Z)-CLH304a. (E)-CLH304a (CLH304a; HY-129636) is a specific and noncompetitive GABAB receptor negative allosteric modulator (NAM). CLH304a inhibits Baclofen (HY-B0007)-induced ERK1/2 phosphorylation in HEK293 cells overexpressing GABAB receptors .
    (E/Z)-CLH304a
  • HY-107510
    YM-230888

    		mGluR Neurological Disease
    YM-230888 is an orally active, selective and allosteric mGlu1 receptor antagonist with a Ki of 13 nM. YM-230888 inhibits mGlu1-mediated inositol phosphate production in rat cerebellar granule cells with an IC50 of 13 nM. YM-230888 shows antinociceptive response in Streptozotocin (HY-13753)-induced hyperalgesia models. YM-230888 significantly reduces pain parameters in complete Freund's adjuvant (HY-153808)-induced arthritic pain models .
    YM-230888
  • HY-100588
    VU0364770

    		mGluR Neurological Disease
    VU0364770 is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
    VU0364770
  • HY-100588A
    VU0364770 hydrochloride

    		mGluR Neurological Disease
    VU0364770 hydrochloride is a selective and potent positive allosteric modulator (PAM) of mGlu4. VU0346770 hydrochloride exhibits EC50s of 290 nM and 1.1 μM at rat mGlu4 and human mGlu4 receptor, respectively. VU0364770 hydrochloride exhibits antagonist activity at mGlu5 with a potency of 17.9 μM and PAM activity at mGlu6 with a potency of 6.8 μM. VU0364770 hydrochloride also possesses activity at MAO with Ki values of 8.5 and 0.72 μM for human MAO-A and human MAO-B, respectively .
    VU0364770 hydrochloride
  • HY-165125
    (S)-VU0637120

    		Neuropeptide Y Receptor Metabolic Disease
    (S)-VU0637120 is a Y4R antagonist that effectively reduces the binding response of its endogenous ligand, pancreatic polypeptide (PP), on Y4R, with an IC50 value of 2.7 μM. (S)-VU0637120 binds to the allosteric site of Y4R, which is located in the core region of the Y4R transmembrane structure, near the binding pocket of pancreatic polypeptide (PP), with a KB value of 300-400 nM. (S)-VU0637120 holds potential for research in the field of metabolic diseases .
    (S)-VU0637120
  • HY-111052
    AZD7325

    		GABA Receptor Cytochrome P450 Neurological Disease Inflammation/Immunology
    AZD7325 is a potent and orally active partial selective PAM of GABAAα2 and Aα3 receptor (Ki=0.3 and 1.3 nM, respectively), and has less antagonistic efficacy at the Aα1 and Aα5 receptor subtypes . AZD7325 is a moderate CYP1A2 and a potent CYP3A4 inducer in vitro . AZD7325 has the potential for the investigation of anxiety and dravet syndrome . PAM: positive allosteric modulator.
    AZD7325
  • HY-157998
    mG2N001

    		mGluR Src Others
    mG2N001 is a negative allosteric modulator (NAM) (IC50: 93 nM) of the metabotropic glutamate receptor mGluR2 and binds to mGluR2 as an antagonist (Ki: 63 nM). mG2N001 is microparticle- and plasma-stable, and its radioisotope [11C]mG2N001 can be used in PET imaging. [11C]mG2N001 has good brain heterogeneity and brain penetration, and can selectively accumulate in mGluR2-rich regions, producing high-contrast brain images .
    mG2N001
  • HY-122575
    Aurintricarboxylic acid
    2 Publications Verification

    		 P2X Receptor Influenza Virus Topoisomerase MicroRNA Apoptosis Infection Neurological Disease Inflammation/Immunology
    Aurintricarboxylic acid is a nanomolar-potency, allosteric antagonist with selectivity towards αβ-methylene-ATP-sensitive P2X1Rs and P2X3Rs, with IC50s of 8.6 nM and 72.9 nM for rP2X1R and rP2X3R, respectively . Aurintricarboxylic acid is a potent anti-influenza agent by directly inhibiting the neuraminidase . Aurintricarboxylic acid is an inhibitor of topoisomerase II and apoptosis . Aurintricarboxylic acid is a selective inhibitor of the TWEAK-Fn14 signaling pathway . Aurintricarboxylic acid also acts as a cystathionine-lyase (CSE) inhibitor with an IC50 of 0.6 μM . Aurintricarboxylic acid is a modifier of miRNAs that regulate miRNA function, with an IC50 of 0.47 µM .
    Aurintricarboxylic acid

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