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Results for "Alpha7 Nicotinic Receptors Inhibitors" in MCE Product Catalog:

245

Inhibitors & Agonists

37

Peptides

37

Natural
Products

Cat. No. Product Name Target Research Areas
  • HY-N1064
    Xanthoplanine

    nAChR Neurological Disease
    Xanthoplanine, isolated from theroot of Xylopia parviflora, fully inhibits the EC50 ACh responses of both alpha7 and alpha4beta2 nACh receptors with estimated IC50 values of 9 μM (alpha7) and 5 μM (alpha4beta2).
  • HY-12149
    A-867744

    nAChR Autophagy Neurological Disease
    A-867744 is a highly potent and selective type II positive allosteric modulator (PAM) of the alpha7 nicotinic acetylcholine receptors (nAChR) with an EC50 of 1.0 μM.
  • HY-128700
    Nicotinic acid mononucleotide

    Others Metabolic Disease
    Nicotinic acid mononucleotide (NAMN) is formed from nicotinic acid (NA) via the nicotinic acid phosphoribosyltransferase in the biosynthesis of NAD +. Nicotinate mononucleotide is a substrate for nicotinamide mononucleotide/Nicotinic acid mononucleotide adenylyltransferase.
  • HY-B1061
    Nicotinic acid N-oxide

    Others Cardiovascular Disease
    Nicotinic acid N-oxide is used to treat hyperlipoidemia.
  • HY-W001909
    Myosmine

    nAChR Metabolic Disease
    Myosmine, a specific tobacco alkaloid in nuts and nut products, has low affinity for a4b2 nicotinic acetylcholinergic receptors (nAChR) with a Ki of 3300 nM.
  • HY-108057A
    Facinicline hydrochloride

    RG3487 hydrochloride

    nAChR 5-HT Receptor Neurological Disease
    Facinicline hydrochloride (RG3487 hydrochloride) is an orally active nicotinic α7 receptor partial agonist, with a Ki of 6 nM for α7 human nAChR. Facinicline hydrochloride (RG3487 hydrochloride) improves cognition and sensorimotor gating in rodents. Facinicline hydrochloride (RG3487 hydrochloride) shows high affinity (antagonist) to 5-HT3Rs with a Ki value of 1.2 nM.
  • HY-110160
    Pozanicline dihydrochloride

    ABT-089 dihydrochloride

    nAChR Neurological Disease
    Pozanicline dihydrochloride (ABT-089 dihydrochloride) is an orally bioavailable nicotinic acetylcholine receptor (nAChR) agonist with a Ki of 16.7 nM for binding to [ 3H]cytisine sites. Pozanicline is an α4β2-selective nAChR agonist, which binds to rat brain α4β2 nAChR with a Ki of 17 nM while binding to α7 nAChR is insignificant.
  • HY-U00439
    Protein kinase inhibitors 1

    DYRK Cancer
    Protein kinase inhibitors 1 is a novel inhibitor of HIPK2 with an IC50 of 74 nM and Kd of 9.5 nM.
  • HY-136146
    SUVN-911

    nAChR Neurological Disease
    SUVN-911 is a potent, selective, brain penetrated and orally bioavailable neuronal nicotinic acetylcholine α4β2 receptor antagonist, with a Ki of 1.5 nM. SUVN-911 has antidepressant activity.
  • HY-P1271
    Catestatin

    nAChR Cardiovascular Disease
    Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-133027
    Myristyl nicotinate

    Tetradecyl nicotinate

    Others Cancer
    Myristyl nicotinate (Tetradecyl nicotinate) is an ester prodrug and a lipophilic derivative of Nicotinic acid. Myristyl nicotinate is being developed for delivery of Nicotinic acid into the skin for prevention of actinic keratosis and its progression to skin cancer. Myristyl nicotinate shows to stimulate epidermal differentiation in photodamaged skin, increasing skin NAD content and strengthening the skin barrier.
  • HY-P1271A
    Catestatin TFA

    nAChR Cardiovascular Disease
    Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure. Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release.
  • HY-B0403S
    Bupropion D9

    Dopamine Receptor Neurological Disease
    Bupropion D9 is a deuterium labeled Bupropion. Bupropion is an atypical antidepressant of the aminoketone group and inhibits dopamine, norepinephrine reuptake and blocks several nicotinic receptors.
  • HY-107457
    AZD-8529

    mGluR Neurological Disease
    AZD-8529 is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-107457A
    AZD-8529 mesylate

    mGluR Neurological Disease
    AZD-8529 mesylate is a potent, highly selective and orally bioavailable positive allosteric modulator of mGluR2, with an EC50 of 285 nM, and shows no positive allosteric modulator responses at 20-25 M on the mGluR1, 3, 4, 5, 6, 7, and 8 subtypes.
  • HY-133534
    PA-Nic TFA

    Others Others
    PA-Nic TFA is a photoactivatable nicotine, whcih can be photolyzed with ~405 nm laser flashes to efficiently release nicotine.
  • HY-10021
    Varenicline Tartrate

    CP 526555-18

    nAChR Neurological Disease
    Varenicline Tartrate(CP 526555;Champix) is a nicotinic receptor partial agonist; it stimulates nicotine receptors more weakly than nicotine itself does.
  • HY-B0150
    Nicotinamide

    Niacinamide; Nicotinic acid amide

    Endogenous Metabolite Sirtuin Neurological Disease Cancer
    Nicotinamide is a form of vitamin B3 that plays essential roles in cell physiology through facilitating NAD+ redox homeostasis and providing NAD+ as a substrate to a class of enzymes that catalyze non-redox reactions. Nicotinamide is an inhibitor of SIRT1.
  • HY-W015806
    3-Pyridineacetic acid

    Endogenous Metabolite Others
    3-Pyridineacetic acid is a higher homologue of nicotinic acid, a breakdown product of nicotine (and other tobacco alkaloids).
  • HY-B0143
    Niacin

    Nicotinic acid; Vitamin B3

    Autophagy Endogenous Metabolite Metabolic Disease
    Niacin (Vitamin B3) is a water-soluble vitamin and is part of the vitamin B group.
  • HY-B0979
    Lobeline hydrochloride

    α-Lobeline hydrochloride; L-Lobeline hydrochloride

    nAChR Neurological Disease
    Lobeline hydrochloride, a nicotinic receptor agonist, acting as a potent antagonist at both α3β2 and α4β2 neuronal nicotinic receptor subtypes.
  • HY-B1532
    Anabasine

    (S)-Anabasine

    nAChR Neurological Disease
    Anabasine is a nicotinic receptor agonist.
  • HY-U00281
    S16961

    S169611

    nAChR Neurological Disease
    S16961 is a nicotinic receptor agonist.
  • HY-B0379A
    Adiphenine hydrochloride

    nAChR Neurological Disease
    Adiphenine hydrochloride is a nicotinic receptor inhibitor, used as an antispasmodic drug.
  • HY-113353
    Nicotinuric acid

    Endogenous Metabolite Others
    Nicotinuric acid is an acyl glycine. Nicotinuric acid is a metabolite of nicotinic acid.
  • HY-N2197
    Hirsuteine

    Others Neurological Disease
    Hirsuteine is an indole alkaloid extracted from Uncaria genus. Hirsuteine non-competitively antagonizes nicotine-mediated dopamine release by blocking ion permeation through nicotinic receptor channel complexes.
  • HY-12641
    Pyrantel tartrate

    Parasite Antibiotic Infection
    Pyrantel tartrate is an antinematodal thiophene; nicotinic receptor agonist and can elicit spastic muscle paralysis in parasitic worms due to prolonged activation of the excitatory nicotinic acetylcholine (nACh) receptors on body wall muscle.
  • HY-113239
    Hydroxycotinine

    Endogenous Metabolite Metabolic Disease
    Hydroxycotinine is the main nicotine metabolite detected in smokers urine.
  • HY-U00139
    Cyclodrine hydrochloride

    mAChR nAChR Neurological Disease
    Cyclodrine hydrochloride is a cholinergic (muscarinic, nicotinic) (mAChR and nAChR) receptor antagonist.
  • HY-131005
    Ehp inhibitor 2

    Ephrin Receptor Cancer
    Ehp inhibitor 2 is a Eph family tyrosine kinase inhibitor.
  • HY-B0429
    Pancuronium dibromide

    nAChR Neurological Disease
    Pancuronium Dibromide is a bis-quaternary steroid that is a competitive nicotinic antagonist.
  • HY-16748
    Nelonicline

    ABT-126

    nAChR Neurological Disease
    Nelonicline (ABT-126) is a selective neuronal nicotinic receptor agonist.
  • HY-B0020
    Tropisetron Hydrochloride

    SDZ-ICS-930

    5-HT Receptor Neurological Disease
    Tropisetron Hydrochloride (SDZ-ICS-930) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
  • HY-B0570
    Decamethonium Bromide

    nAChR Neurological Disease
    Decamethonium Bromide is a nicotinic AChR partial agonist and neuromuscular blocking agent.
  • HY-B0072
    Tropisetron

    SDZ-ICS-930 free base

    5-HT Receptor nAChR Neurological Disease
    Tropisetron (SDZ-ICS-930 free base) is a selective 5-HT3 receptor antagonist and α7-nicotinic receptor agonist with an IC50 of 70.1 ± 0.9 nM for 5-HT3 receptor.
  • HY-B0569
    Hexamethonium Bromide

    nAChR Apoptosis Neurological Disease
    Hexamethonium Bromide is a non-depolarising ganglionic blocker, a nicotinic nACh (NN) receptor antagonist.
  • HY-B0406A
    Bethanechol chloride

    Carbamyl-β-methylcholine chloride

    mAChR Metabolic Disease
    Bethanechol Chloride (Carbamyl-β-methylcholine chloride) is a selective muscarinic receptor agonist without any effect on nicotinic receptors.
  • HY-B0406
    Bethanechol

    Carbamyl-β-methylcholine

    mAChR Neurological Disease
    Bethanechol is a parasympathomimetic choline carbamate that selectively stimulates muscarinic receptors without any effect on nicotinic receptors.
  • HY-B0942
    Benzethonium chloride

    nAChR Neurological Disease
    Benzethonium chloride inhibit human recombinant α7 and α4β2 neuronal nicotinic acetylcholine receptors in Xenopus oocytes.
  • HY-N2332A
    Methyllycaconitine citrate

    MLA

    nAChR Infection
    Methyllycaconitine citrate is a specific antagonist of α7 neuronal nicotinic acetylcholine receptor (α7nAChR).
  • HY-121879
    SHP836

    Phosphatase Cancer
    SHP836 is a SHP2 allosteric inhibitor, with an IC50 of 12 μM for the full length SHP2.
  • HY-N0443
    N-Methylcytisine

    Caulophylline

    nAChR Inflammation/Immunology
    N-Methylcytisine (Caulophylline), a tricyclic quinolizidine alkaloid, exerts hypoglycaemic, analgesic and anti-inflammatory activities. N-methylcytisine is a selective ligand of nicotinic receptors of acetylcholine in the central nervous system and has a high affinity (Kd = 50 nM) to nicotinic acetylcholine receptors (nAChR) from squid optical ganglia.
  • HY-14565
    Pozanicline

    ABT-089

    nAChR Neurological Disease
    Pozanicline (ABT-089) selectively activate neuronal nicotinic acetylcholine receptor (nAChR) subtypes, is a novel cholinergic agent that is a partial agonist at α4β2* nAChRs (Ki=16 nM) and shows high selectivity for α6β2* and α4α5β2 nAChR subtypes, the binding affinity (Ki, rat) for Pozanicline to [ 3H] cytisine sites is 16.7 nM. Pozanicline reverses nicotine withdrawal-induced cognitive deficits, may be an effective component of novel therapeutic strategies for nicotine addiction.
  • HY-W008350
    (+)-Sparteine

    nAChR Neurological Disease
    (+)-Sparteine is a natural alkaloid acting as a ganglionic blocking agent. (+)-Sparteine competitively blocks nicotinic ACh receptor in the neurons.
  • HY-15430A
    Encenicline hydrochloride

    EVP-6124 (hydrochloride)

    nAChR Neurological Disease
    Encenicline hydrochloride (EVP-6124 hydrochloride) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
  • HY-15430
    Encenicline

    EVP-6124

    nAChR Neurological Disease
    Encenicline (EVP-6124) is a novel partial agonist of α7 neuronal nicotinic acetylcholine receptors (nAChRs).
  • HY-B1178
    Cotinine

    (-)-Cotinine; (S)-Cotinine; NIH-10498

    Endogenous Metabolite Others
    Cotinine is an alkaloid found in tobacco and is also the predominant metabolite of nicotine, used as a biomarker for exposure to tobacco smoke.
  • HY-107675
    Desformylflustrabromine hydrochloride

    Deformylflustrabromine hydrochloride; dFBr hydrochloride

    nAChR Neurological Disease
    Desformylflustrabromine hydrochloride is a selective agonist of α4β2 neuronal nicotinic acetylcholine receptor (nAChR) with a pEC50 of 6.48.
  • HY-14774
    Monepantel

    AAD1566

    nAChR Cancer
    Monepantel is organic anthelmintic, and acts as a positive allosteric modulator of a nematode-specific clade of nicotinic acetylcholine receptor (nAChR) subunits.
  • HY-B0827
    Dinotefuran

    MTI-446

    Parasite nAChR Infection
    Dinotefuran is an insecticide of the neonicotinoid class, its mechanism of action involves disruption of the insect's nervous system by inhibiting nicotinic acetylcholine receptors.
  • HY-A0009
    Galanthamine hydrobromide

    Galantamine hydrobromide

    AChE Apoptosis Neurological Disease
    Galanthamine hydrobromide is a long-acting, centrally active acetylcholinesterase(AChE) inhibitor (IC50 = 410 nM) and allosteric potentiator at neuronal nicotinic ACh receptors.
  • HY-14564A
    GTS-21 dihydrochloride

    DMXB-A; DMBX-anabaseine

    nAChR Inflammation/Immunology
    GTS-21 dihydrochloride is a selective α7 nicotinic acetylcholine receptor agonist, has recently been established as a promising treatment for inflammation.
  • HY-A0127
    Etofibrate

    Others Metabolic Disease
    Etofibrate is the ethandiol-1,2 diester of the nicotinic and clofibric acids. Etofibrate has been shown to be a potent hypolipidemic agent in animal and human.
  • HY-N3610
    Coclaurine

    nAChR Neurological Disease
    Coclaurine is a class of tetrahydroisoquinoline alkaloids isolated from Sarcopetalum harveyanum. Coclaurine is a nicotinic acetylcholine receptor (nAChRs) antagonist.
  • HY-19373
    RWJ-445167

    3DP-10017

    Thrombin Factor Xa Cardiovascular Disease
    RWJ-445167 (3DP-10017) is a dual inhibitor of thrombin and factor Xa with Ki of 4.0 nM and 230 nM, respectively, exhibiting potent antithrombotic activity.
  • HY-16787
    ICA-121431

    Sodium Channel Cardiovascular Disease
    ICA-121431 is a nanomolar potent and broad-spectrum voltage-gated sodium channel (Nav) blocker, shows equipotent selectivity for human Nav1.1 and Nav1.3 subtypes with IC50 values of 13 nM and 23 nM, respectively. ICA-121431 shows less potent inhibition of Nav1.2 (IC50=240 nM) and 1,000 fold selectivity against Nav1.4, Nav1.6, and the TTX-resistant human Nav1.5 and Nav1.8 channels (IC50s >10 µM).
  • HY-P1365
    α-Conotoxin MII

    α-CTxMII

    nAChR Neurological Disease
    α-Conotoxin MII (α-CTxMII), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII (α-CTxMII) potently blocks β3-containing neuronal nicotinic receptors .
  • HY-B0823
    Acetamiprid

    nAChR Neurological Disease
    Acetamiprid is a neonicotinoid insecticide used worldwide. Acetamiprid is a nicotinic acetylcholine receptor (nAChR) agonist, and is shown to be associated with neuromuscular and reproductive disorders.
  • HY-10019
    Varenicline

    CP 526555

    nAChR Neurological Disease
    Varenicline (CP 526555) is a potent partial agonist for α4β2 nicotinic acetylcholine receptor (nAChR) with an EC50 value of 2.3 μM. Varenicline is a full agonist for α3β4 and α7 nAChRs with EC50 values of 55 μM and 18 μM, respectively. Varenicline is a nicotinic ligand based on the structure of cytisine, has the potential for smoking cessation treatment.
  • HY-P1365A
    α-Conotoxin MII TFA

    α-CTxMII TFA

    nAChR Neurological Disease
    α-Conotoxin MII TFA (α-CTxMII TFA), a 16-amino acid peptide from the venom of the marine snail Conus magus, potently blocks nicotinic acetylcholine receptors (nAChRs) composed of α3β2 subunits, with an IC50 of 0.5 nM. α-Conotoxin MII TFA (α-CTxMII TFA) potently blocks β3-containing neuronal nicotinic receptors .
  • HY-124540B
    (Rac)-ABT-202 dihydrochloride

    nAChR Neurological Disease
    (Rac)-ABT-202 dihydrochloride is a racemate of ABT-202. ABT-202 is an agonist of nicotinic acetylcholine receptors (nAChRs) and can be used as an analgesic.
  • HY-N2338
    Cholesterol myristate

    Cholesteryl myristate; Cholesteryl tetradecanoate

    nAChR GABA Receptor Potassium Channel Endogenous Metabolite Cancer
    Cholesterol myristate is a natural steroid present in traditional Chinese medicine. Cholesterol myristate binds to several ion channels such as the nicotinic acetylcholine receptor, GABAA receptor, and the inward-rectifier potassium ion channel.
  • HY-U00439A
    Protein kinase inhibitors 1 hydrochloride

    (E)-5-((2-Oxo-6'-(piperazin-1-yl)-1,2-dihydro-[3,3'-bipyridin]-5-yl)methylene)thiazolidine-2,4-dione hydrochloride

    DYRK Cancer
    Protein kinase inhibitors 1 hydrochloride is a potent HIPK2 inhibitor, with IC50s of 136 and 74 nM for HIPK1 and HIPK2, and a Kd of 9.5 nM for HIPK2.
  • HY-14824
    Sofiniclin

    ABT 894

    nAChR Neurological Disease
    Sofiniclin (ABT 894), an agonist of nicotinic acetylcholine receptor (nAChR), is used as a potential non-stimulant research for attention-deficit/hyperactivity disorder (ADHD).
  • HY-W012037
    8-Hydroxyquinoline hemisulfate

    8-Quinolinol hemisulfate

    Bacterial Antibiotic Infection
    8-Hydroxyquinoline hemisulfate (8-Quinolinol hemisulfate) is a monoprotic bidentate chelating agent, exhibits antiseptic, disinfectant, and pesticide properties, functioning as a transcription inhibitor.
  • HY-103673
    AMPD2 inhibitor 1

    Adenosine Deaminase Neurological Disease
    AMPD2 inhibitor 1 is an adenosine monophosphate deaminase 2 (AMPD2) inhibitor, used in the research of sugar craving, salt craving, umami craving, and addictions including drug, tobacco, nicotine and alcohol addictions.
  • HY-12560D
    PNU-282987 S enantiomer free base

    nAChR Others
    PNU-282987 S enantiomer free base is the S-enantiomer of PNU-282987 free base. PNU-282987 is an α7 nicotinic acetylcholine receptor (α7 nAChR) agonist.
  • HY-10680
    MK-6892

    GPR109A Cancer
    MK-6892 is a potent, selective, and full agonist for the high affinity nicotinic acid (NA) receptor GPR109A. Ki and GTPγS EC50 of MK-6892 on the Human GPR109A is 4 nM and 16 nM, respectively.
  • HY-B0820
    Nitenpyram

    nAChR Neurological Disease
    Nitenpyram is a calss of neonicotinoid and an insect nicotinic acetylcholine receptor (nAChR) agonist with an IC50 of 14 nM. Nitenpyram is an oral fast-acting insecticide used to suppress sucking insects on companion animals.
  • HY-100806
    Kynurenic acid

    Quinurenic acid

    iGluR Endogenous Metabolite Apoptosis Inflammation/Immunology Neurological Disease Endocrinology
    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
  • HY-107512
    Kynurenic acid sodium

    iGluR Apoptosis Inflammation/Immunology Neurological Disease Endocrinology
    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
  • HY-110241
    Dianicline dihydrochloride

    nAChR Neurological Disease
    Dianicline dihydrochloride is a α4β2 nicotinic acetylcholine receptor partial agonist, a class of drugs that includes varenicline and cytisine for smoking cessation. Dianicline dihydrochloride increases cessation rates in a dose-dependent manner.
  • HY-N0584A
    Anisodamine hydrobromide

    6-Hydroxyhyoscyamine hydrobromide

    mAChR Inflammation/Immunology
    Anisodamine hydrobromide (6-Hydroxyhyoscyamine hydrobromide), a belladonna alkaloid, is a non-subtype-selective muscarinic and a nicotinic cholinoceptor antagonist. Anisodamine hydrobromide shows antioxidant, anti-inflammatory properties.
  • HY-135813
    LtaS-IN-1

    Bacterial Infection
    LtaS-IN-1 (compound 1771) is a potent small-molecule inhibitor of Lipoteichoic acid (LTA) synthesis in multidrug-resistant (MDR) E. faecium and by altering the cell wall morphology. LtaS-IN-1 alone inhibits Enterococcus.spp 28 strains with varying MIC values ranging from 0.5 μg/mL to 64 μg/mL. LtaS-IN-1 combination with antibiotics abolishs multidrug-resistant E. faecium growth almost completely.
  • HY-125957
    A-3 hydrochloride

    PKA Casein Kinase CaMK PKC Others
    A-3 hydrochloride is a potent, cell-permeable, reversible, ATP-competitive non-selective antagonist of various kinases. It against PKA (Ki=4.3 µM), casein kinase II (Ki=5.1 µM) and myosin light chain kinase (MLCK) (Ki=7.4 µM). A-3 hydrochloride also inhibits PKC and casein kinase I with Ki values of 47 µM and 80 µM, respectively.
  • HY-P1269
    α-Conotoxin AuIB

    nAChR Neurological Disease
    α-Conotoxin AuIB, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
  • HY-107688A
    UB-165 fumarate

    nAChR Neurological Disease
    UB-165 fumarate is a nAChR agonist, being a full agonist of the α3β2 isoform and a partial agonist of the α4β2* isoform, with a Ki value of 0.27 nM for nicotine binding in rat brain.
  • HY-12560A
    PNU-282987

    nAChR Neurological Disease
    PNU-282987 is a selective α7 nicotinic acetylcholine receptor7 nAChR) agonist with Ki of 26 nM; no affinity for α1β1γδ and α3β4 nAChRs (IC50 ≥ 60 μM).
  • HY-P1269A
    α-Conotoxin AuIB TFA

    nAChR Neurological Disease
    α-Conotoxin AuIB TFA, a potent and selective α3β4 nicotinic acetylcholine receptor (nAChR) antagonist, blocks α3β4 nAChRs expressed in Xenopus oocytes with an IC50 of 0.75 μM.
  • HY-13225A
    Rivanicline

    RJR-2403; (E)-Metanicotine

    nAChR Neurological Disease
    Rivanicline (RJR-2403; (E)-Metanicotine) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 36000 nM).
  • HY-107670
    Dihydro-β-erythroidine hydrobromide

    DHβE hydrobromide

    nAChR Neurological Disease
    Dihydro-β-erythroidine (DHβE) hydrobromide is a potent, orally active, and competitive antagonist of neuronal nAChRs. Dihydro-β-erythroidine hydrobromide shows selectivity for α4β4 and α4β2 nAChRs, with IC50s of 0.19 and 0.37 μM, respectively. Antidepressant-like activities.
  • HY-125901
    D-Tubocurarine chloride pentahydrate

    nAChR Neurological Disease
    D-Tubocurarine chloride pentahydrate is the chloride salt form of Tubocurarine, a nicotinic acetylcholine receptors (AChR) antagonist, and can be used as a skeletal muscle relaxant during surgery or mechanical ventilation. D-Tubocurarine chloride pentahydrate is also a potent neuromuscular blocking agent.
  • HY-101918
    DS-1040 Tosylate

    Others Cardiovascular Disease
    DS-1040 Tosylate is an orally active, selective inhibitor of activated thrombin-activatable fibrinolysis inhibitor (TAFIa) with IC50s of 5.92 nM and 8.01 nM for human and rat TAFIa. DS-1040 Tosylate is a fibrinolysis enhancer for thromboembolic diseases.
  • HY-18728
    STF-31

    GLUT Autophagy Cancer
    STF-31 is a selective inhibitor of glucose transporter 1 (GLUT1), with an IC50 of 1μM[1][2].
  • HY-128420
    Lobeline sulfate

    α-Lobeline sulfate; L-Lobeline sulfate

    Endogenous Metabolite Neurological Disease
    Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) is a nonstimulant medication that can alter dopamine uptake in brain. Lobeline sulfate (α-Lobeline sulfate; L-Lobeline sulfate) inhibits nicotine-induced hyperactivity and is effective in smoking cessation.
  • HY-P1268
    α-Conotoxin PIA

    nAChR Neurological Disease
    α-Conotoxin PIA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
  • HY-P1268A
    α-Conotoxin PIA TFA

    nAChR Neurological Disease
    α-Conotoxin PIA TFA is a nicotinic acetylcholine receptor (nAChR) antagonist isolated from Conus purpurascens that targets nAChR subtypes containing α6 and α3 subunits. α-Conotoxin PIA has the potential for the research of Parkinson’s disease, and schizophrenia。
  • HY-13225
    Rivanicline oxalate

    RJR-2403 oxalate; (E)-Metanicotine oxalate

    nAChR Neurological Disease
    Rivanicline oxalate (RJR-2403 oxalate; (E)-Metanicotine oxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
  • HY-13225B
    Rivanicline hemioxalate

    RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate

    nAChR Neurological Disease
    Rivanicline hemioxalate (RJR-2403 hemioxalate; (E)-Metanicotine hemioxalate) is a neuronal nicotinic receptor agonist, showing high selectivity for the α4β2 subtype (Ki=26 nM); > 1,000 fold selectivity than α7 receptors(Ki= 3.6 μM).
  • HY-106901A
    Asoxime dichloride

    HI-6

    nAChR Neurological Disease
    Asoxime dichloride (HI-6) is an antagonist to acetylcholine receptors (AChRs) including the nicotinic receptor, α7 nAChR. Asoxime dichloride involves in modulating immunity response. Asoxime dichloride (HI-6) can be used as an antigen and improves vaccination efficacy in the nervous system.
  • HY-15583
    Auristatin F

    Microtubule/Tubulin ADC Cytotoxin Cancer
    Auristatin F is a potent cytotoxin. Auristatin F, a potent microtubule inhibitor and vascular damaging agent (VDA), can be used in antibody-drug conjugates (ADC).
  • HY-N7108
    7-Hydroxyflavone

    Others Inflammation/Immunology
    7-Hydroxyflavone is a flavonoid isolated from M. indica, with anti-inflammatory activity. 7-Hydroxyflavone protects renal cells from nicotine (NIC)-associated cytotoxicity via the ERK/Nrf2/HO-1 pathway.
  • HY-122470
    Stampidine

    Reverse Transcriptase HIV Infection
    Stampidine is a nucleoside reverse transcriptase inhibitor (NRTI) with potent and broad-spectrum anti-HIV activity. Stampidine inhibits the laboratory HIV-1 strain HTLVIIIB (B-envelope subtype) and primary clinical isolates with IC50s of 1 nM and 2 nM, respectively. Stampidine also inhibits NRTI-resistant primary clinical isolates and NNRTI-resistant clinical isolates with IC50s of 8.7 nM and 11.2 nM, respectively.
  • HY-75502
    Rotigotine

    N-0437; N-0923

    Dopamine Receptor Adrenergic Receptor 5-HT Receptor Neurological Disease Endocrinology
    Rotigotine (N-0437; N-0923) is a full agonist of dopamine receptor, a partial agonist of the 5-HT1A receptor, and an antagonist of the α2B-adrenergic receptor, with Kis of 0.71 nM, 4-15 nM, and 83 nM for the dopamine D3 receptor and D2, D5, D4 receptors, and dopamine D1 receptor.
  • HY-10020
    Varenicline Hydrochloride

    CP 526555 hydrochloride

    nAChR Neurological Disease
    Varenicline Hydrochloride (CP 526555 hydrochloride) is a high affinity, selective α4β2 nicotine acetylcholine receptor (nAChR) partial agonist and full α7 nAChR agonist. Varenicline Hydrochloride is also a potent partial agonist of α6β2 nAChR in striatum of rats with a Ki value of 0.12 nM.
  • HY-11007
    GNF-2

    Bcr-Abl SARS-CoV Cancer
    GNF-2 is a highly selective, allosteric, non-ATP competitive inhibitor of Bcr-Abl. GNF-2 inhibits Ba/F3.p210 proliferation with an IC50 of 138 nM .
  • HY-107676
    SIB-1553A

    nAChR Neurological Disease
    SIB-1553A is an orally bioavailable nicotinic acetylcholine receptors (nAChRs) agonist, with selectivity for β4 subunit-containing nAChRs. SIB-1553A is also a selective neuronal nAChR ligand. SIB-1553A is a cognitive enhancer, and has therapeutic potential for the symptomatic treatment of Alzheimer’s disease and other cognitive disorders.
  • HY-B1510S
    Acrivastine D7

    BW825C D7

    Histamine Receptor Endocrinology Inflammation/Immunology
    Acrivastine D7 (BW825C D7) is a deuterium labeled Acrivastine. Acrivastine is a short acting histamine 1 receptor antagonist.
  • HY-P1868A
    α2β1 Integrin Ligand Peptide TFA

    Integrin Others
    α2β1 Integrin Ligand Peptide TFA interacts with the α2β1 integrin receptor on the cell membrane and mediates extracellular signals into cells. It is a potential antagonist of collagen receptors.
  • HY-P1106A
    K41498 TFA

    CFTR Cardiovascular Disease
    K41498 TFA is a potent and highly selective CRF2 receptor antagonist with Ki values of 0.66 nM, 0.62 nM and 425 nM for human CRF, CRF and CRF1 receptors respectively hypotension. K41498 TFA is an analogues of antisauvagine-30 (aSvg-30), inhibits sauvagine-stimulated cAMP accumulation in hCRF- and hCRF-expressing cells. K41498 TFA can be used for hypotension study.
  • HY-N7247
    Thiochrome

    mAChR Metabolic Disease
    Thiochrome, a natural oxidation product and metabolite of thiamine, is a selective M4 muscarinic receptor of acetylcholine (ACh) affinity enhancer. Thiochrome has neutral cooperativity with ACh at M1 to M3 receptors.
  • HY-P1167A
    [Orn5]-URP TFA

    Urotensin Receptor Cardiovascular Disease
    [Orn5]-URP TFA is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC50 of 7.24. [Orn5]-URP TFA displays no agonist activity[1] [2] .
  • HY-P1167
    [Orn5]-URP

    Urotensin Receptor Cardiovascular Disease
    [Orn5]-URP is a potent and selective pure antagonist of Urotensin-II receptor (UT), with an pEC50 of 7.24. [Orn5]-URP displays no agonist activity[1] [2] .
  • HY-N2326
    (±)-Anatoxin A fumarate

    nAChR Neurological Disease
    (±)-Anatoxin A fumarate is a natural alkaloid isolated from freshwater cyanobacterium.(±)-Anatoxin A fumarate is a potent nicotinic receptor agonist and exhibits Ki values of 1.25 nM and 1.84 μM for binding to putative α4β2-type nAChR and α7-type nAChR in rat brain membranes, respectively. (±)-Anatoxin A fumarate stimulates [ 3H]-dopamine release from rat striatal synaptosomes (EC50=134 nM).
  • HY-P1335
    CTAP

    Opioid Receptor Neurological Disease
    CTAP is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP can be used for the study of L-DOPA-induced dyskinesia (LID).
  • HY-103407A
    PD 168568 dihydrochloride

    Dopamine Receptor Neurological Disease
    PD 168568 dihydrochloride is an orally active and selective D4 dopamine receptor antagonist, with a Ki of 8.8 nM.
  • HY-P1335A
    CTAP TFA

    Opioid Receptor Neurological Disease
    CTAP TFA is a potent, highly selective, and brain penetrant μ opioid receptor antagonist (IC50=3.5 nM) and displays over 1200-fold selectivity over δ opioid (IC50=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID).
  • HY-135329
    Solifenacin D5 hydrochloride

    mAChR Neurological Disease
    Solifenacin D5 hydrochloride is a deuterium labeled Solifenacin hydrochloride. Solifenacin hydrochloride is a muscarinic receptor antagonist with pKis of 7.6, 6.9 and 8.0 for M1, M2 and M3 receptors, respectively.
  • HY-135588
    Raloxifene 6,4'-Bis-β-D-glucuronide

    Others Metabolic Disease
    Raloxifene 6,4'-Bis-β-D-glucuronide (compound IV) is a metabolite of Raloxifene. Raloxifene is a selective estrogen receptor antagonist for the prevention of osteoporosis.
  • HY-129995A
    TSHR antagonist S37a

    TSH Receptor Endocrinology
    TSHR antagonist S37a is a highly selective thyrotropin receptor (TSHR) antagonist, with potential for the treatment of Graves' orbitopathy.
  • HY-130842
    β-Naphthoflavone-CH2-Br

    β-NF-CH2-Br

    Ligand for E3 Ligase Cancer
    β-Naphthoflavone-CH2-Br (β-NF-CH2-Br) is an arylhydrocarbon receptor (AhR) ligand. β-Naphthoflavone-CH2-Br can be used to synthesize the PROTAC β-NF-JQ1(HY-130256).
  • HY-P1329A
    CTOP TFA

    Opioid Receptor Neurological Disease
    CTOP TFA is a peptide that acts as a μ-opioid receptor antagonist.
  • HY-14415
    SR8278

    Others Metabolic Disease
    SR8278 is a competitive nuclear heme receptor REV-ERB synthetic antagonist. SR8278 inhibits the REV-ERBα transcriptional repression activity with an EC50 of 0.47μM. SR8278 is used to regulate the metabolism in organisms and study biological rhythm.
  • HY-P1329
    CTOP

    Opioid Receptor Neurological Disease
    CTOP is a peptide that acts as a μ-opioid receptor antagonist.
  • HY-110303
    Xanthine amine congener dihydrochloride

    XAC dihydrochloride

    Adenosine Receptor Neurological Disease
    Xanthine amine congener dihydrochloride (XAC dihydrochloride) is a potent Adenosine A1 receptor and A2 receptor antagonist with IC50 values of 1.8 and 114 nM, respectively. Xanthine amine congener acts as a convulsant agent in mice model.
  • HY-133011
    nAChR agonist 1

    nAChR Neurological Disease
    nAChR agonist 1 is a potent, brain-permeable, and orally efficacious positive allosteric modulator of α7 nicotinic acetylcholine receptor7 nAChR). nAChR agonist 1 has the EC50 of 0.32 µM in a Ca 2+ mobilization assay (PNU-282987-induced, FLIPR based) in human IMR-32 neuroblastoma cells that endogenously express α7 nAChR. nAChR agonist 1 can be develpoped for the treatment of Alzheimer’s disease.
  • HY-101348
    L-741626

    Dopamine Receptor Neurological Disease
    L-741626 is a selective D2 dopamine receptor antagonist, with the Ki values of 2.4, 100 and 220 nM for human D2, D3 and D4 receptors respectively.
  • HY-15656S
    Ceritinib D7

    LDK378 D7

    ALK Insulin Receptor IGF-1R Cancer Endocrinology
    Ceritinib D7 (LDK378 D7) is a deuterium labeled Ceritinib. Ceritinib is a selective, orally bioavailable and ATP-competitive ALK tyrosine kinase inhibitor.
  • HY-124759
    CCR1 antagonist 9

    CCR Inflammation/Immunology
    CCR1 antagonist 9 is a potent and selective CCR1 antagonist with an IC50 of 6.8 nM in calcium flux assay.
  • HY-108495
    CYM50308

    LPL Receptor Cardiovascular Disease
    CYM50308 is a potent, selective and high affinity sphingosine-1-phosphate receptor 4 (S1P4-R) agonist with an EC50 of 56 nM. CYM50308 displays 37-fold more selective for S1P4-R than S1P5-R. CYM50308 has no activity at S1P1-R, S1P2-R and S1P3-R subtypes at concentrations up to 25 μM.
  • HY-17497S
    Acebutolol D7

    Adrenergic Receptor Endocrinology Cardiovascular Disease
    Acebutolol D7 is a deuterium labeled Acebutolol. Acebutolol is a selective β1 adrenergic receptor antagonist used in the treatment of hypertension, angina pectoris and cardiac arrhythmias.
  • HY-101299A
    Dihydrexidine

    DAR-0100

    Dopamine Receptor Neurological Disease
    Dihydrexidine (DAR-0100) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist with an IC50 of 10 nM for D1 receptor. Dihydrexidine exhibits potent antiparkinsonian activity.
  • HY-W040146
    Propionylpromazine hydrochloride

    Propiopromazine hydrochloride

    Dopamine Receptor Neurological Disease
    Propionylpromazine hydrochloride (Propiopromazine hydrochloride), a dopamine receptor D2 (DRD2) antagonist, can be used in the research of Parkinson disease.
  • HY-133045
    VHL Ligand 8

    Ligand for E3 Ligase Cancer
    VHL Ligand 8 is a VHL ligand. VHL Ligand 8 can be used to synthesize ARD-266 (HY-133020), a highly potent and VHL E3 ligase-based androgen receptor (AR) PROTAC degrader. ARD-266 effectively induces degradation of AR protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
  • HY-133189
    Bis-propargyl-PEG9

    PROTAC Linker Endocrinology
    Bis-propargyl-PEG9 is a PEG-based PROTAC linker used in the synthesis of PROTACs. Bis-propargyl-PEG9 can be used to synthesize the bivalent estrogen receptor ligands.
  • HY-12222
    Obeticholic acid

    INT-747; 6-ECDCA; 6-Ethylchenodeoxycholic acid

    FXR Autophagy Others
    Obeticholic acid (INT-747) is a potent, selective and orally active FXR agonist with an EC50 of 99 nM. Obeticholic acid has anticholeretic and anti-inflammation effect. Obeticholic acid also induces autophagy.
  • HY-128128
    ASN04421891

    Others Neurological Disease
    ASN04421891 is a potent GPR17 receptor modulator, with an EC50 of 3.67 nM in [35S]GTPγS binding assay. ASN04421891 can be used for neurodegenerative diseases research.
  • HY-133014
    RIP2 kinase inhibitor 1

    RIP kinase Inflammation/Immunology
    RIP2 kinase inhibitor 1 (compound 11) is a potent and selective receptor interacting protein 2 (RIP2) kinase inhibitor with an IC50 of 0.03 μM for RIP2 FP. RIP2 kinase inhibitor 1 is used for autoinflammatory disorders.
  • HY-13418A
    Dorsomorphin

    Compound C; BML-275

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin (Compound C) is a selective and ATP-competitive AMPK inhibitor (Ki=109 nM in the absence of AMP). Dorsomorphin (BML-275) selectively inhibits BMP type I receptors ALK2, ALK3, and ALK6. Dorsomorphin induces autophagy.
  • HY-100658
    Didesmethyl cariprazine

    5-HT Receptor Dopamine Receptor Neurological Disease
    Didesmethyl cariprazine is a metabolite of Cariprazine and acts as the predominant circulating active moiety. Didesmethyl cariprazine has a long half-life of 1-3 weeks. Cariprazine is a antipsychotic drug candidate that exhibits high affinity for the D3 and D2 receptors, and moderate affinity for the 5-HT1A receptor.
  • HY-108258A
    PSN 375963 hydrochloride

    GPR119 Endocrinology
    PSN 375963 hydrochloride is a potent GPR119 agonist, with EC50s of 8.4 and 7.9 μM for human and mouse GPR119, respectively. PSN 375963 hydrochloride shows similar potency to the endogenous agonist oleoylethanolamide (OEA).
  • HY-101299B
    Dihydrexidine hydrochloride

    DAR-0100 hydrochloride

    Dopamine Receptor Neurological Disease
    Dihydrexidine hydrochloride (DAR-0100 hydrochloride) is a high potent, selective and full efficacy D1-like dopamine receptor (D1/D5) agonist, with an IC50 of 10 nM for D1 receptor. Dihydrexidine hydrochloride exhibits potent antiparkinsonian activity.
  • HY-N0050
    Allomatrine

    (+)-Allomatrine

    Others Neurological Disease
    Allomatrine ((+)-Allomatrine) is an alkaloid from the bark of Sophora japonica. Allomatrine has antinociceptive properties mediated mainly through the activation ofκ-opioid receptors.
  • HY-B0098S
    Doxazosin D8

    UK 33274 D8

    Adrenergic Receptor Endocrinology Cardiovascular Disease
    Doxazosin D8 (UK 33274 D8) is a deuterium labeled Doxazosin (UK 33274). Doxazosin is a quinazoline-derivative that selectively antagonizes postsynaptic α1 adrenergic receptors.
  • HY-115613
    ML-180

    SR1848

    Others Cancer
    ML-180 (SR1848) is a potent orphan nuclear receptor liver receptor homolog 1 (LRH-1; NR5A2) inverse agonist with an IC50 of 3.7 µM. ML-180 is inactive for steroidogenic factor-1 (SF-1; NR5A1; IC50>10 µM). ML-180 has the potential for LRH-1-dependent cancers.
  • HY-122872
    MKK7-COV-9

    p38 MAPK Cancer
    MKK7-COV-9 is a potent and selective covalent inhibitor of MKK7 and targets a specific protein–protein interaction of MKK7. MKK7-COV-9 blocks primary B cell activation in response to LPS with an EC50 of 4.98 μM.
  • HY-P1345A
    TLQP-21 TFA

    Complement System Endocrinology Neurological Disease
    TLQP-21 TFA, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8μM). TLQP-21 TFA activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 TFA is used for the research in regulation of nociception and other relevant physiologic functions.
  • HY-P1345
    TLQP-21

    Complement System Endocrinology Neurological Disease
    TLQP-21, a VGF-derived peptide endowed of endocrine and extraendocrine properties, is a potent G-protein-coupled receptor complement-3a receptor 1 (C3aR1) agonist (EC50: mouse TLQP-21=10.3 μM; human TLQP-21=68.8 μM). TLQP-21 activates C3aR1 to induce an increase of intracellular Ca 2+. TLQP-21 is used for the research in regulation of nociception and other relevant physiologic functions.
  • HY-14551
    Osanetant

    SR142801

    Neurokinin Receptor Neurological Disease
    Osanetant (SR142801) is a selective NK3 receptor antagonist. Osanetant produces anxiolytic- and antidepressant-like effects and is researched for schizophrenia.
  • HY-12206
    Thioperamide

    MR-12842

    Histamine Receptor Neurological Disease
    Thioperamide (MR-12842) is a potent, orally available, brain penetrant and selective H3 receptor antagonist with a Ki of 4.3 nM for inhibition of [ 3H]histamine release. Thioperamide inhibits [ 3H]histamine synthesis with a Ki of 31 nM.
  • HY-13418
    Dorsomorphin dihydrochloride

    Compound C dihydrochloride; BML-275 dihydrochloride

    AMPK TGF-β Receptor Autophagy Cancer
    Dorsomorphin dihydrochloride (BML-275 dihydrochloride; Compound C dihydrochloride) is a potent, selective and ATP-competitive AMPK inhibitor, with a Ki of 109 nM. Dorsomorphin dihydrochloride inhibits BMP pathway by targeting the type I receptors ALK2, ALK3, and ALK6. Dorsomorphin dihydrochloride induces autophagy.
  • HY-128113
    AG-09/1

    Others Inflammation/Immunology
    AG-09/1 is a specific formyl peptide receptor 1 (FPR1) agonist. N-formyl peptide receptors (FPR) are important in host defense.
  • HY-103090
    NPS ALX Compound 4a

    5-HT Receptor Neurological Disease
    NPS ALX Compound 4a is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM.
  • HY-90010
    Tolterodine tartrate

    Kabi-2234; PNU-200583E

    mAChR Neurological Disease
    Tolterodine Tartrate (Kabi-2234; PNU-200583E) is a potent muscarinic receptor antagonist and shows selectivity for the urinary bladder over salivary glands in vivo.
  • HY-133113
    7-Desmethyl-agomelatine

    5-HT Receptor Neurological Disease
    7-Desmethyl-agomelatine is a metabolite of Agomelatine. Agomelatineis a potent agonist at melatonin receptors (MT1 and MT2), and also is an antagonist of 5-HT2C.
  • HY-P1302A
    Orphanin FQ(1-11) TFA

    Opioid Receptor Neurological Disease
    Orphanin FQ(1-11) TFA, a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) TFA has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) TFA is analgesic in CD-1 mice.
  • HY-13728
    Plevitrexed

    ZD 9331; BGC9331

    Thymidylate Synthase Cancer
    Plevitrexed (ZD 9331; BGC 9331) is an orally active and potent thymidylate synthase (TS) inhibitor with a Ki of 0.44 nM. Plevitrexed is taken up via the α-folate receptor as well as the reduced folate carrier. Plevitrexed is used for gastric cancer in clinical.
  • HY-P1302
    Orphanin FQ(1-11)

    Opioid Receptor Neurological Disease
    Orphanin FQ(1-11), a orphanin FQ or nociceptin (OFQ/N) fragment, is a potent NOP receptor (ORL-1; OP4) agonist, with a Ki of 55 nM. Orphanin FQ(1-11) has no affinity for μ, δ, κ1 and κ3 receptors (Ki>1000 nM). Orphanin FQ(1-11) is analgesic in CD-1 mice.
  • HY-103090A
    NPS ALX Compound 4a dihydrochloride

    5-HT Receptor Neurological Disease
    NPS ALX Compound 4a dihydrochloride is a potent and selective 5-hydroxytryptamine6 (5-HT6) receptor antagonist, with an IC50 of 7.2 nM and a Ki of 0.2 nM.
  • HY-N7272
    Cirsimarin

    Phosphodiesterase (PDE) Metabolic Disease
    Cirsimarin is a potent antilipogenic flavonoid isolated from Microtea debilis. Cirsimarin exerts potent antilipogenic effect and decreases adipose tissue deposition in mice. The lipolytic activity of Cirsimarin resulting from both its antagonist activity on adenosin A1 receptor and its inhibitory effect on phosphodiesterase.
  • 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.
  • HY-B1494
    Picrotoxinin

    Chloride Channel GABA Receptor Neurological Disease
    Picrotoxinin, a potent convulsant, is a chloride channel blocker. Picrotoxinin is a noncompetitive GABAA receptor antagonist, which negatively modulates the action of GABA on GABAA receptors.
  • HY-135147
    ONC206

    Dopamine Receptor Cancer Neurological Disease
    ONC206 is an analogue of TRAIL inducer ONC201. ONC206 is a selective antagonist of the D2-like dopamine receptors (DRD2/3/4) at nanomolar concentrations. ONC206 has broad-spectrum anti-tumor activity.
  • HY-10847A
    SB-277011 dihydrochloride

    SB-277011A dihydrochloride

    Dopamine Receptor Neurological Disease
    SB-277011 dihydrochloride (SB-277011A dihydrochloride) is a potent, selective, orally bioavailable and brain penetrate dopamine D3 receptor antagonist, with pKis of 8.0, 6.0, <5.2 and 5.9 for D3, D2, 5-HT1B, and 5-HT1D receptors, respectively.
  • HY-N1919
    Ajmalicine

    Raubasine

    Adrenergic Receptor AChE Cardiovascular Disease Endocrinology
    Ajmalicine (Raubasine) is found in herbs of Catharanthus roseus, is an antihypertensive drug used in the treatment of high blood pressure, decreases peripheral resistance and blood pressure. Ajmalicine (Raubasine) is an adrenolytic drug which preferentially blocks alpha 1-adrenoceptor than alpha 2-adrenoceptor. Ajmalicine (Raubasine) is an reversible non-competitive nicotine receptor antagonist with an IC50 of 72.3 μM. Ajmalicine (Raubasine) acts preferentially at postsynaptic sites, competitively antagonizes the effect of noradrenaline on postsynaptic alpha-adrenoceptor with a pA2 value of 6.57, blocks the inhibitory effect of clonidine with an pA2 value of 6.2.
  • HY-15310
    Ivermectin

    MK-933

    Parasite HIV Mitophagy HSV SARS-CoV Antibiotic Autophagy Infection Cancer
    Ivermectin (MK-933) is a broad-spectrum anti-parasite agent. Ivermectin (MK-933) is a specific inhibitor of Impα/β1-mediated nuclear import and has potent antiviral activity towards both HIV-1 and dengue virus. It is a positive allosteric effector of P2X4 and the α7 neuronal nicotinic acetylcholine receptor (nAChRs). Ivermectin also inhibits bovine herpesvirus1 (BoHV-1) replication and inhibits BoHV-1 DNA polymerase nuclear import. Ivermectin is a candidate therapeutic against SARS-CoV-2/COVID-19.
  • HY-14325
    L-745870

    Dopamine Receptor Neurological Disease
    L-745870 is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
  • HY-42849
    Sultopride

    LIN-1418

    Dopamine Receptor Neurological Disease
    Sultopride (LIN-1418) is a selective antagonist of dopamine D2 receptor.
  • HY-130492
    ARCC-4

    PROTAC Androgen Receptor Cancer
    ARCC-4 is a low-nanomolar androgen receptor (AR) degrader based on PROTAC, with a DC50 of 5 nM. ARCC-4 is an enzalutamide-based von Hippel-Lindau (VHL)-recruiting AR PROTAC and outperforms enzalutamide. ARCC-4 effectively degrades clinically relevant AR mutants associated with antiandrogen therapy.
  • HY-107380A
    PGlu-3-methyl-His-Pro-NH2 TFA

    A-42872 TFA

    Others Endocrinology
    PGlu-3-methyl-His-Pro-NH2 TFA (A-42872 TFA), the modified thyrotropin-releasing hormone (TRH) peptide, enhances binding to pituitary TRH receptors and increases stimulation of thyroid-stimulating hormone (TSH) release from the pituitary. The in vitro permeability of PGlu-3-methyl-His-Pro-NH2 TFA through rat skin is increased in the presence of enhancers Ethanol and Cineole.
  • HY-70081A
    Sumanirole maleate

    U-95666E; PNU-95666

    Dopamine Receptor Neurological Disease
    Sumanirole maleate (U-95666E; PNU-95666E) is a highly selective D2 receptor full agonist with an ED50 of about 46 nM. Sumanirole was developed for the treatment of Parkinson's disease and restless leg syndrome.
  • HY-106224
    Orexin A (human, rat, mouse)

    Orexin Receptor (OX Receptor) Neurological Disease
    Orexin A human, rat, mouse, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse has a role in the regulation of feeding behavior. Orexin A human, rat, mouse is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
  • HY-14648
    Dexamethasone

    Hexadecadrol; Prednisolone F

    Glucocorticoid Receptor SARS-CoV Autophagy Complement System Mitophagy Bacterial Antibiotic Cancer Infection Endocrinology Inflammation/Immunology
    Dexamethasone (Hexadecadrol) is a glucocorticoid receptor agonist. Dexamethasone also significantly decreases CD11b, CD18, and CD62L expression on neutrophils, and CD11b and CD18 expression on monocytes. Dexamethasone is highly effective in the control of COVID-19 infection.
  • HY-103187
    HEMADO

    Adenosine Receptor Cancer Inflammation/Immunology
    HEMADO is a potent and selective adenosine A3 receptor agonist with a Ki of 1.1 nM at the human A3 subtype.
  • HY-P1112A
    Sarafotoxin S6a TFA

    Endothelin Receptor Neurological Disease Cardiovascular Disease
    Sarafotoxin S6a TFA , a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a TFA elicits the pig coronary artery with an EC50 value of 7.5 nM.
  • HY-110278
    ADX71743

    mGluR Neurological Disease
    ADX71743 is a highly selective, noncompetitive and brain-penetrant metabotropic glutamate receptor 7 negative allosteric modulator (mGlu7 NAM). ADX71743 has anxiolytic-like activity.
  • HY-106224A
    Orexin A (human, rat, mouse) (TFA)

    Orexin Receptor (OX Receptor) Neurological Disease
    Orexin A human, rat, mouse TFA, a 33 amino acid excitatory neuropeptide, orchestrates diverse central and peripheral processes. Orexin A human, rat, mouse TFA is a specific, high-affinity agonist for G-protein-coupled receptor OX1R. Orexin A human, rat, mouse TFA has a role in the regulation of feeding behavior. Orexin A human, rat, mouse TFA is an effective anti-nociceptive and anti-hyperalgesic agent in mice and rats.
  • HY-101372A
    Oxotremorine M iodide

    mAChR Neurological Disease
    Oxotremorine M iodide is a potent and non-selective muscarinic acetylcholine receptor (mAChR) agonist. Oxotremorine M iodide potentiates NMDA receptors by muscarinic receptor dependent and independent mechanisms.
  • HY-P2307
    Tat-NR2Baa

    iGluR NO Synthase Neurological Disease
    Tat-NR2BAA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
  • HY-70002B
    Enzalutamide carboxylic acid

    MDV3100 carboxylic acid

    Drug Metabolite Cancer
    Enzalutamide carboxylic acid (MDV3100 carboxylic acid) is an inactive metabolite of Enzalutamide (MDV3100). Enzalutamide is an androgen receptor (AR) antagonist.
  • HY-42849A
    Sultopride hydrochloride

    LIN-1418 hydrochloride

    Dopamine Receptor Neurological Disease
    Sultopride hydrochloride (LIN-1418 hydrochloride) is a selective antagonist of dopamine D2 receptor.
  • HY-P2307A
    Tat-NR2Baa TFA

    iGluR NO Synthase Neurological Disease
    Tat-NR2BAA TFA is the control peptide of Tat-NR2B9c (HY-P0117), inactive. The sequence of Tat-NR2BAA TFA is similar to Tat-NR2B9c, but it has a double-point mutation in the COOH terminal tSXV motif, making it incapable of binding PSD-95. Tat-NR2B9c is a membrane-permeant peptide and disrupts PSD-95/NMDAR binding, correlate with uncoupling NR2B- and/or NR2A-type NMDARs from PSD-95.
  • HY-14325B
    L-745870 hydrochloride

    Dopamine Receptor Neurological Disease
    L-745870 hydrochloride is a potent, selective, brain-penetrant and orally active dopamine D4 receptor antagonist with a Ki of 0.43 nM. L-745870 hydrochloride shows weaker affinity for D2 (Ki of 960 nM) and D3 (Ki of 2300 nM) receptors, and exhibits moderate affinity for 5-HT2 receptors, sigma sites and α-adrenoceptors.
  • HY-P1112
    Sarafotoxin S6a

    Endothelin Receptor Neurological Disease Cardiovascular Disease
    Sarafotoxin S6a, a sarafotoxin analogue, is a endothelin receptor agonist and has an ETA/ETB selectivity profile similar to that of Endothelin-3 (HY-P0204). Sarafotoxin S6a elicits the pig coronary artery with an EC50 value of 7.5 nM.
  • HY-133044
    Boc-Pip-alkyne-Ph-COOH

    PROTAC Linker Cancer
    Boc-Pip-alkyne-Ph-COOH is a PROTAC linker, which refers to the alkyl/ether composition. Boc-Pip-alkyne-Ph-COOH can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 effectively induces degradation of androgen receptor (AR) protein in AR-positive LNCaP, VCaP, and 22Rv1 prostate cancer cell lines with DC50 values of 0.2-1 nM.
  • HY-111269
    AZD8848

    Toll-like Receptor (TLR) Inflammation/Immunology
    AZD8848 is a selective toll-like receptor 7 (TLR7) antedrug agonist which is developed for the research of asthma and allergic rhinitis.
  • HY-14903
    Ulimorelin

    TZP-101

    GHSR Adrenergic Receptor Metabolic Disease
    Ulimorelin (TZP-101) is a ghrelin receptor (GRLN) agonist with an EC50 of 29 nM and a Ki of 16 nM. Ulimorelin is a prokinetic agent and causes vasorelaxation through competitive antagonist action at α1-adrenoceptors. Ulimorelin stimulates intestinal motility and is used for malnutrition.
  • HY-76569
    Desfesoterodine

    PNU-200577; 5-Hydroxymethyl Tolterodine

    mAChR Neurological Disease
    Desfesoterodine (PNU-200577) is a potent and selective muscarinic receptor (mAChR) antagonist with a KB and a pA2 of 0.84 nM and 9.14, respectively. Desfesoterodine is a major pharmacologically active metabolite of Tolterodine (PNU-200583; HY-A0024) and Fesoterodine (HY-70053). Desfesoterodine improves cerebral infarction induced detrusor overactivity in rats.
  • HY-100634
    4-Hydroxypropranolol hydrochloride

    (±)-4-hydroxy Propranolol hydrochloride

    Adrenergic Receptor Neurological Disease
    4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol. 4-Hydroxypropranolol hydrochlorid is of comparable potency to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
  • HY-108847
    Etanercept

    TNF Receptor Inflammation/Immunology
    Etanercept, a dimeric fusion protein that binds TNF, acts as a TNF inhibitor. Etanercept competitively inhibits the binding of both TNF-α and TNF-β to cell surface TNF receptors, rendering TNF biologically inactive. Etanercept shows efficacy against rheumatoid arthritis, juvenile idiopathic arthritis, and plaque psoriasis.
  • HY-135892
    GNE-1858

    Others Inflammation/Immunology
    GNE-1858 is a potent and ATP-competitive hematopoietic progenitor kinase-1 (HPK1) inhibitor, with IC50s of 1.9 nM, 1.9 nM, and 4.5 nM for wild-type and the active mimetic mutants HPK1-TSEE and HPK1-SA, respectively.
  • HY-12598
    (S)-3,5-DHPG

    mGluR Neurological Disease
    (S)-3,5-DHPG is a weak, but selective group I metabotropic glutamate receptors (mGluRs) agonist with Ki values of 0.9 µM and 3.9 µM for mGluR1a and mGluR5a, respectively. (S)-3,5-DHPG exhibits anxiolytic activity in rats subjected to hypoxia.
  • HY-P2287
    Cortagine

    CRFR Neurological Disease
    Cortagine is a specific corticotropin-releasing factor receptor subtype 1 (CRF1) agonist with an IC50 of 2.6 nM for rCRF1. Cortagine is an anxiolytic and antidepressive drug in the mouse model.
  • HY-100369A
    DMCM hydrochloride

    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.
  • HY-136181
    YNT-185 dihydrochloride

    Orexin Receptor (OX Receptor) Neurological Disease
    YNT-185 dihydrochloride is a nonpeptide, selective orexin type-2 receptor (OX2R) agonist, with EC50s of 0.028 and 2.75 μM for OX2R and OX1R, respectively. YNT-185 dihydrochloride ameliorates narcolepsy-cataplexy symptoms in mouse models.
  • HY-103200
    SR59230A hydrochloride

    Adrenergic Receptor Metabolic Disease Cardiovascular Disease
    SR59230A hydrochloride is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.
  • HY-B0649
    Propofol

    2,6-Diisopropylphenol

    GABA Receptor Endogenous Metabolite Neurological Disease
    Propofol potently and directly activates GABAA receptor and inhibits glutamate receptor mediated excitatory synaptic transmission. Propofol has antinociceptive properties and is used for sedation and hypnotic.
  • HY-122203
    PCS1055 dihydrochloride

    mAChR AChE Neurological Disease
    PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [ 3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively.
  • HY-100672
    SR59230A

    Adrenergic Receptor Metabolic Disease Cardiovascular Disease
    SR59230A is a potent, selective, and blood-brain barrier penetrating β3-adrenergic receptor antagonist with IC50s of 40, 408, and 648 nM for β3, β1, and β2 receptors, respectively.
  • HY-19608
    GSK1016790A

    TRP Channel Calcium Channel Metabolic Disease Cardiovascular Disease
    GSK1016790A is a potent and selective transient receptor potential vanilloid 4 (TRPV4) channel agonist. GSK1016790A can elicit Ca 2+ influx and elevate intracellular Ca 2+ in HEK cells.
  • HY-112055
    DIM-C-pPhOH

    Apoptosis Cancer
    DIM-C-pPhOH is a nuclear receptor 4A1 (NR4A1) antagonist. DIM-C-pPhOH inhibits cancer cell growth and mTOR signaling, induce apoptosis and cellular stress. DIM-C-pPhOH reduces cell proliferation with IC50 values of 13.6 μM and 13.0 μM for ACHN cells and 786-O cells, respectively.
  • HY-133046
    VHL Ligand-Linker Conjugates 17

    E3 Ligase Ligand-Linker Conjugate Cancer
    VHL Ligand-Linker Conjugates 17 incorporates a VHL ligand for the E3 ubiquitin ligase, and a PROTAC linker. VHL Ligand-Linker Conjugates 17 can be used in the synthesis of a series of PROTACs, such as ARD-266 (HY-133020). ARD-266 is a highly potent androgen receptor (AR) PROTAC degrader.
  • HY-113313
    Aldosterone

    Endogenous Metabolite Cardiovascular Disease
    Aldosterone is the primary mineralocorticoid. Aldosterone is a steroid hormone, and it is synthesized and secreted in response to renin-angiotensin system activation (RAS) or high dietary potassium by the zona glomerulosa (ZG) of the adrenal cortex. Aldosterone activity is dependent by the binding and activation of the cytoplasmic/nuclear mineralocorticoid receptor (MR) at cellular level.
  • HY-133073
    CCR7 Ligand 1

    CCR7-Cmp2105

    CCR Ligand 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.
  • HY-16489A
    Terodiline hydrochloride

    mAChR Calcium Channel Neurological Disease
    Terodiline hydrochloride is an M1-selective muscarinic receptor (mAChR) antagonist with Kbs of 15, 160, 280, and 198 nM in rabbit vas deferens (M1), atria (M2), bladder (M3) and ileal muscle (M3), respectively. Terodiline hydrochloride also is a Ca 2+ blocker. Terodiline hydrochloride acts as a treatment for urinary frequency and urge incontinence.
  • HY-126941
    Hecogenin acetate

    Opioid Receptor Neurological Disease
    Hecogenin acetate is a steroidal sapogenin-acetylated with anti-inflammatory and antinociceptive. Hecogenin acetate shows potential antihyperalgesic activity, inhibiting descending pain and acting in opioid receptors.
  • HY-14569
    CDPPB

    mGluR Neurological Disease
    CDPPB is a potent, selective and brain penetrant positive allosteric modulator of the metabotropic glutamate receptor subtype 5 (mGluR5), with an EC50 of 27 nM in Chinese hamster ovary cells expressing human mGluR5. CDPPB may provide an approach for development of antipsychotic agents.
  • HY-100991
    FG 7142

    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.
  • HY-19589
    JTS-653

    TRP Channel Inflammation/Immunology Neurological Disease
    JTS-653 is a highly potent and selective transient receptor potential vanilloid 1 (TRPV1) antagonist in vitro and in vivo. JTS-653 attenuates chronic pain refractory to non-steroidal anti-inflammatory agents.
  • HY-119486
    Tavapadon

    PF-06649751; CVL-751

    Dopamine Receptor Neurological Disease
    Tavapadon (PF-06649751; CVL-751) is an orally active and highly selective dopamine D1/D5 receptor partial agonist. Tavapadon is effective in enabling movement and reducing disability and has the potential for Parkinson's disease.
  • 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.
  • HY-N6932
    Voacamine

    Cannabinoid Receptor P-glycoprotein Cancer Metabolic Disease
    Voacamine, an indole alkaloid, isolated from Voacanga Africana, exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.
  • HY-108625
    SHA 68

    Neuropeptide Y Receptor Neurological Disease
    SHA 68 is a potent and selective non-peptide neuropeptide S receptor (NPSR) antagonist with IC50s of 22.0 and 23.8 nM for NPSR Asn 107 and NPSR Ile 107, respectively. SHA 68 has limited the blood-brain barrier (BBB) penetration and the activity in neuralgia.
  • HY-15319
    AMG 487

    CXCR Cancer Inflammation/Immunology Endocrinology
    AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
  • HY-N2080
    Songorine

    GABA Receptor Cancer
    Songorine is a diterpenoid alkaloid isolated from the genus Aconitum. Songorine is a GABAA receptor antagonist in rat brain and has anti cancer, antiarrhythmic and anti-inflammatory activities. Songorine has the potential for the treatment of Epithelial ovarian cancer (EOC).
  • HY-100634S
    4-Hydroxypropranolol D7 hydrochloride

    (±)-4-hydroxy Propranolol D7 hydrochloride

    Adrenergic Receptor Neurological Disease
    4-Hydroxypropranolol D7 hydrochloride ((±)-4-hydroxy Propranolol D7 hydrochloride) is a deuterium labeled 4-Hydroxypropranolol hydrochloride. 4-Hydroxypropranolol hydrochlorid is an active metabolite of Propranolol, with potency comparable to Propranolol. 4-Hydroxypropranolol hydrochlorid inhibits β1- and β2-adrenergic receptors with pA2 values of 8.24 and 8.26, respectively. 4-Hydroxypropranolol hydrochlorid has intrinsic sympathomimetic activity, membrane stabilizing activity and potent antioxidant properties.
  • HY-130992
    Androgen receptor antagonist 1

    Androgen Receptor Ligand for Target Protein for PROTAC Cancer
    Androgen receptor antagonist 1 is an orally available full androgen receptor (AR) antagonist with an IC50 of 59 nM. Androgen receptor antagonist 1 (Compound 6) can be used in the synthesis of PROTAC AR degraders, which results 24% and 47 % AR protein degradation in LNCaP cells at 1 μM and 10 μM, respectively.
  • HY-116330A
    Hyperforin dicyclohexylammonium salt

    Hyperforin DCHA

    TRP Channel Calcium Channel Neurological Disease
    Hyperforin dicyclohexylammonium salt (Hyperforin DCHA) is a transient receptor canonical 6 (TRPC6) channels activator. Hyperforin dicyclohexylammonium salt modulates Ca 2+ levels by activating Ca 2+-conducting non-selective canonical TRPC6 channels. Hyperforin dicyclohexylammonium salt shows antidepressant effect.
  • HY-13965
    Parmodulin 2

    ML161

    Protease-Activated Receptor (PAR) Cardiovascular Disease
    Parmodulin 2 (ML161) is an allosteric inhibitor of protease-activated receptor 1 (PAR1) with an IC50 of 0.26 μM. Parmodulin 2 is a potent and non-competitive inhibitor of SFLLRN-induced P-selectin expression leading to inhibition of platelet aggregation in vitro and platelet thrombus formation in vivo.
  • HY-B0589C
    (3S,5S)-Atorvastatin

    Cytochrome P450 Metabolic Disease
    (3S,5S)-Atorvastatin is a inactive enantiomer of Atorvastatin. (3S,5S)-Atorvastatin can activate pregnane X receptor (PXR). Atorvastatin is an orally active HMG-CoA reductase inhibitor, has the ability to effectively decrease blood lipids.
  • HY-15319A
    (±)-AMG 487

    CXCR Cancer
    (±)-AMG 487 is a racemate of AMG 487. AMG 487 is an orally active and selective antagonist of CXC chemokine receptor 3 (CXCR3) which inhibits the binding of CXCL10 and CXCL11 to CXCR3 with IC50s of 8.0 and 8.2 nM, respectively.
  • HY-136561
    GRK5-IN-2

    Others Metabolic Disease
    GRK5-IN-2 (compound 707), a pyridine-based bicyclic compound, is a potent G-protein-coupled receptor kinase 5 (GRK5) inhibitor. GRK5-IN-2 regulates the expression and/or release of insulin and is useful for the metabolic disease research.
  • HY-124733
    LIT-001 free base

    Oxytocin Receptor Neurological Disease
    LIT-001 free base is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 free base improves social interaction in a mouse model of autism.
  • HY-100234A
    DREADD agonist 21 dihydrochloride

    mAChR Neurological Disease
    DREADD agonist 21 dihydrochloride is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
  • HY-124733A
    LIT-001

    Oxytocin Receptor Neurological Disease
    LIT-001 is the first nonpeptide oxytocin receptor (OT-R) agonist (EC50=55 nM; Ki=226 nM). LIT-001 improves social interaction in a mouse model of autism.
  • HY-100371
    (RS)-MCPG

    Alpha-MCPG

    mGluR Neurological Disease
    (RS)-MCPG (alpha-MCPG) is a competitive and selective group I/group II metabotropic glutamate receptor (mGluR) antagonist. (RS)-MCPG blocks theta-burst stimulation (TBS)-induced shifts in both juvenile and neonatal rat hippocampal neurons.
  • HY-113962
    7α,25-Dihydroxycholesterol

    7α,25-OHC

    EBI2/GPR183 Endogenous Metabolite Inflammation/Immunology
    7α, 25-dihydroxycholesterol (7α,25-OHC) is a potent and selective agonist and endogenous ligand of the orphan GPCR receptor EBI2 (GPR183). 7α, 25-dihydroxycholesterol is highly potent at activating EBI2 (EC50=140 pM; Kd=450 pM). 7α, 25-dihydroxycholesterol can serve as a chemokine directing migration of B cells, T cells and dendritic cells.
  • HY-133552
    RORγt Inverse agonist 10

    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
  • HY-103476
    Ro15-4513

    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.
  • HY-135303
    GLPG1205

    GPR84 Inflammation/Immunology
    GLPG1205 is potent, selective and orally active GPR84 (a G-protein-coupled receptor) antagonist with a favorable PK/PD profile. GLPG1205 has anti-inflammatory activity and is used for the treatment of pulmonary fibrosis.
  • HY-100234
    DREADD agonist 21

    mAChR Neurological Disease
    DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM).
  • HY-P1471
    Adrenomedullin (AM) (22-52), human

    22-52-Adrenomedullin (human)

    CGRP Receptor Cardiovascular Disease
    Adrenomedullin (AM) (22-52), human, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist, and also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
  • HY-P1471A
    Adrenomedullin (AM) (22-52), human TFA

    22-52-Adrenomedullin (human) (TFA)

    CGRP Receptor Cardiovascular Disease
    Adrenomedullin (AM) (22-52), human (22-52-Adrenomedullin human) TFA, an NH2 terminal truncated adrenomedullin analogue, is an adrenomedullin receptor antagonist. Adrenomedullin (AM) (22-52), human also antagonizes the calcitonin generelated peptide (CGRP) receptor in the hindlimb vascular bed of the cat.
  • HY-N0686
    Pseudoprotodioscin

    Fatty Acid Synthase (FASN) MicroRNA Metabolic Disease
    Pseudoprotodioscin, a furostanoside, inhibits SREBP1/2 and microRNA 33a/b levels and reduces the gene expression regarding the synthesis of cholesterol and triglycerides.
  • HY-118743
    KMN-80

    Prostaglandin Receptor Metabolic Disease
    KMN-80, a derivative of PGE1 (HY-B0131), is a selective and potent agonist of EP4 receptor with an IC50 and a Ki of 3 nM and 2.35 nM, respectively. KMN-80 is against EP3 receptor with an IC50 of 1.4 μM and >10 μM for all other prostanoid receptors.
  • HY-121538
    CUDA

    Epoxide Hydrolase PPAR Cardiovascular Disease
    CUDA is a potent inhibitor of soluble epoxide hydrolase (sEH), with IC50s of 11.1 nM and 112 nM for mouse sEH and human sEH, respectively. CUDA selectively increases peroxisome proliferator-activated receptor (PPAR) alpha activity. CUDA may be valuable for the research of cardiovascular disease.
  • HY-120944
    BAY-7598

    MMP Inflammation/Immunology
    BAY-7598 is a potent, orally bioavailable, and selective MMP12 inhibitor probe with IC50s of 0.085, 0.67 and 1.1 nM for human MMP12, murine MMP12, and rat MMP12, respectively.
  • HY-135880A
    OMDM-4

    Endogenous Metabolite Neurological Disease
    OMDM-4 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki 17.7 μM.
  • HY-135882
    OMDM-6

    TRP Channel Cannabinoid Receptor Endogenous Metabolite Neurological Disease
    OMDM-6 is a hybrid agonist of vanilloid receptor type 1 (VR1, TRPV1) (EC50=75 nM) and cannabinoid receptor type 1 (CB1) (Ki=3.2 μM). OMDM-6 inhibits anandamide cellular uptake (ACU) with a Ki of 7.0 μM.
  • HY-111615A
    J-2156 TFA

    Somatostatin Receptor Neurological Disease
    J-2156 TFA is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 TFA is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
  • HY-121557
    OMDM-1

    Endogenous Metabolite Neurological Disease
    OMDM-1 is a potent, selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 2.4 μM.
  • HY-135881
    OMDM-5

    TRP Channel Endogenous Metabolite Neurological Disease
    OMDM-5 is a selective inhibitor of anandamide cellular uptake (ACU), with a Ki of 4.8 μM. OMDM-5 is also a potent vanilloid receptor type 1 (VR1, TRPV1) agonist, with an EC50 of 75 nM, and shows weakly active as cannabinoid receptor type 1 (CB1) ligand (Ki=4.9 μM).
  • HY-135880
    OMDM-3

    Endogenous Metabolite Neurological Disease
    OMDM-3 is a selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 16.6 μM.
  • HY-P1319
    Nociceptin(1-7)

    Opioid Receptor Inflammation/Immunology
    Nociceptin (1-7) is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) combines with nociceptin reduces hyperalgesia in vivo.
  • HY-14886
    Fasitibant chloride

    MEN16132 free base

    Bradykinin Receptor Neurological Disease Cardiovascular Disease
    Fasitibant chloride (MEN16132 free base) is a potent and selective nonpeptide bradykinin B2 receptor (B2R) antagonist. Fasitibant chloride reduces joint pain and diminishes joint oedema in Carrageenan-induced arthritis rat model.
  • HY-103342
    OMDM-2

    Endogenous Metabolite Neurological Disease
    OMDM-2 is a potent, selective and metabolically stable inhibitor of anandamide cellular uptake (ACU), with a Ki of 3.0 μM.
  • HY-P1319A
    Nociceptin(1-7) TFA

    Opioid Receptor Inflammation/Immunology
    Nociceptin (1-7) TFA is the N-terminal bioactive fragment of nociceptin (HY-P0183). Nociceptin (1-7) TFA is a potent ORL1 (NOP) receptor agonist with antinociceptive activity. Nociceptin (1-7) TFA combines with nociceptin reduces hyperalgesia in vivo.
  • HY-111615
    J-2156

    Somatostatin Receptor Neurological Disease
    J-2156 is a high potent, selective somatostatin receptor type 4 (SST4 receptor) agonist with IC50s of 0.05 nM and 0.07 nM for human and rat SST4 receptors, respectively. J-2156 is used for the relief of mechanical allodynia and mechanical hyperalgesia in the ipsilateral hindpaws in rats.
  • HY-70053A
    Fesoterodine L-mandelate

    mAChR Metabolic Disease Neurological Disease
    Fesoterodine L-mandelate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine L-mandelate is used for the overactive bladder (OAB).
  • HY-N0179
    Ecdysone

    α-Ecdysone

    Endogenous Metabolite Apoptosis Metabolic Disease
    Ecdysone (α-Ecdysone), a major steroid hormone in insects and herbs, triggers mineralocorticoid receptor (MR) activation and induces cellular apoptosis. Ecdysone plays essential roles in coordinating developmental transitions and homeostatic sleep regulation through its active metabolite 20-hydroxyecdysone (Crustecdysone; 20E; HY-N6979).
  • HY-A0030
    Fesoterodine fumarate

    mAChR Metabolic Disease Neurological Disease
    Fesoterodine Fumarate is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine Fumarate is used for the overactive bladder (OAB).
  • HY-70053
    Fesoterodine

    mAChR Metabolic Disease Neurological Disease
    Fesoterodine is an orally active, nonsubtype selective, competitive muscarinic receptor (mAChR) antagonist with pKi values of 8.0, 7.7, 7.4, 7.3, 7.5 for M1, M2, M3, M4, M5 receptors, respectively. Fesoterodine is used for the overactive bladder (OAB).
  • HY-110155
    LM11A-31 dihydrochloride

    Others Neurological Disease
    LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist. LM11A-31 dihydrochloride is an amino acid derivative with high blood-brain barrier permeability and blocks p75-mediated cell death. M11A-31 dihydrochloride reverses cholinergic neurite dystrophy in Alzheimer's disease mouse models with mid- to late-stage disease progression.
  • HY-110155A
    (Rac)-LM11A-31 dihydrochloride

    Others Neurological Disease
    (Rac)-LM11A-31 dihydrochloride is an isomer of LM11A-31 dihydrochloride. LM11A-31 dihydrochloride, a non-peptide p75 NTR (neurotrophin receptor p75) modulator, is an orally active and potent proNGF (nerve growth factor) antagonist.
  • HY-122575
    Aurintricarboxylic acid

    P2X Receptor Influenza Virus Topoisomerase Infection Inflammation/Immunology Neurological Disease
    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.