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high-affinity ligand

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67

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Click Chemistry

Targets Recommended:
Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P1840
    Galanin Receptor Ligand M35

    		Neuropeptide Y Receptor Neurological Disease Endocrinology
    Galanin Receptor Ligand M35 is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
    Galanin Receptor Ligand M35
  • HY-112210
    Shield-1
    4 Publications Verification

    Shld1

    		 FKBP Others
    Shield-1 (Shld1) is a specific, cell-permeant and high-affinity ligand of FK506-binding protein-12 (FKBP), and reverses the instability by binding to mutated FKBP (mtFKBP), allowing conditional expression of mtFKBP-fused proteins. Shield-1 can stabilize proteins tagged with a mutated FKBP12-derived destabilization domain (DD) .
    Shield-1
  • HY-154844
    FAP Ligand 1

    		Others Cancer
    FAP Ligand 1 (FL), a high-affinity FAP small-molecule ligand, is used to target attached drugs to FAP-expressing fibroblasts and can be used in radiation imaging studies of targeted cancers .
    FAP Ligand 1
  • HY-P1840A
    Galanin Receptor Ligand M35 TFA

    		Neuropeptide Y Receptor Neurological Disease Endocrinology
    Galanin Receptor Ligand M35 TFA is a high-affinity ligand and antagonist of galanin receptor (Kd=0.1 nM). Galanin Receptor Ligand M35 TFA exerts a Ki values of 0.11 and 2.0 nM for human galanin receptor type 1 and 2, respectively .
    Galanin Receptor Ligand M35 TFA
  • HY-P5054
    Galanin (1-13)-Neuropeptide Y (25-36) amide

    		Neuropeptide Y Receptor Neurological Disease
    Galanin (1-13)-Neuropeptide Y (25-36) amide is a high-affinity ligand for galanin receptors, and galanin itself .
    Galanin (1-13)-Neuropeptide Y (25-36) amide
  • HY-162553
    GNE7599

    		Ligands for E3 Ligase Cancer
    GNE7599 is a high-affinity and orally active von Hippel-Lindau (VHL) ligand with a Kd of 540 pM. GNE7599 can be connected to the ligand for protein by a linker to form PROTACs .
    GNE7599
  • HY-121738
    TC AC 28

    		Epigenetic Reader Domain Cancer
    TC AC 28 is a high-affinity BET bromodomain ligand with Kd values of 40, 800 nM for Brd2(2), Brd2(1), respectively .
    TC AC 28
  • HY-155698
    Mz438

    		Others Others
    Mz438 is high-affinity and selective fluorescent CXCR2 ligand. Mz438 is a small-molecule-based fluorescent probe targeting the IABS of CXCR2 .
    Mz438
  • HY-P1887
    p5 Ligand for Dnak and DnaJ

    		HSP Infection
    p5 Ligand for Dnak and DnaJ is a nonapeptide, which corresponds to the main binding site for the 23-residue part of the presequence of mitochondrial aspartate aminotransferase. p5 Ligand for Dnak and DnaJ is a high-affinity ligand for DnaK and DnaJ .
    p5 Ligand for Dnak and DnaJ
  • HY-114306
    EC0489

    		Antifolate Cancer
    EC0489, a conjugate of folic acid and desacetyl vinblastine hydrazide, is a high-affinity ligand for the folate receptor (FR). Refractory or metastatic Tumor . Small molecule-agent conjugate (SMDC) .
    EC0489
  • HY-117379
    CHIR-2279

    		Adrenergic Receptor Others
    CHIR-2279 is a high-affinity ligand (Ki=5 nM) for the α1-adrenergic receptor and can be further studied as a drug lead compound .
    CHIR-2279
  • HY-P2112
    DOTA-NOC

    DOTA-Nal3-octreotide

    		 Radionuclide-Drug Conjugates (RDCs) Somatostatin Receptor Others
    DOTA-NOC (DOTA-Nal3-octreotide) is a high-affinity ligand of somatostatin receptor subtypes 2, 3 and 5. DOTA-NOC can be used for labeling with various radiometals, and development of radiopeptide imaging .
    DOTA-NOC
  • HY-101310
    SYM 2081

    		iGluR Neurological Disease
    SYM 2081 is a high-affinity ligand and potent, selective agonist of kainate receptors, inhibits [ 3H]-kainate binding with an IC50 of 35 nM, almost 3000- and 200-fold selectivity for kainate receptors over AMPA and NMDA receptors respectively .
    SYM 2081
  • HY-149933
    AM841

    		Cannabinoid Receptor Neurological Disease
    AM841 is a high-affinity electrophilic ligand. AM841 interacts covalently with a cysteine in helix six and activates the CB1 cannabinoid receptor. AM841 reduces Forskolin (HY-15371)-stimulated cAMP accumulation. AM841 also slows gastrointestinal motility .
    AM841
  • HY-D1643
    5,5'-Dinitro BAPTA AM

    		Biochemical Assay Reagents Others
    5,5'-Dinitro BAPTA AM is a membrane-permeant, high-affinity calcium chelator, it can be used for investigation of the role of cytosolic Ca 2+. 5,5'-Dinitro BAPTA AM can be loaded by incubation into live cells, and is cleaved by cytosolic esterases to liberate the active tetra-carboxylate ligand .
    5,5'-Dinitro BAPTA AM
  • HY-W020790
    Sialyl-Lewis X

    sLeX

    		 Endogenous Metabolite Inflammation/Immunology
    Sialyl-Lewis X (sLeX) is a sialylated fucosylated tetrasaccharide, an endogenous antigen. Sialyl-Lewis X is a high-affinity ligand for selectins (E-, P-, and L-selectin) . Sialyl-Lewis X binds to ELAM-1 and CD62 and has the ability?to inhibits CD62-mediated neutrophil recruitment to sites of inflammation .
    Sialyl-Lewis X
  • HY-148476
    Tri-GalNAc-DBCO

    		LYTACs Others
    Tri-GalNAc-DBCO can bind to the desialic acid glycoprotein receptor (ASGPR) to drive protein downregulation and target protein degradation, where GalNAc is a high-affinity ligand for hepatocyte-specific ASGPR . Tri-GalNAc-DBCO is a click chemistry reagent, it contains a DBCO group that can undergo strain-promoted alkyne-azide cycloaddition (SPAAC) with molecules containing Azide groups.
    Tri-GalNAc-DBCO
  • HY-100583
    (-)-(S)-Equol

    		Estrogen Receptor/ERR Endogenous Metabolite Neurological Disease Metabolic Disease Cancer
    (-)-(S)-Equol is a high affinity ligand for estrogen receptor β with a Ki of 0.73 nM.
    (-)-(S)-Equol
  • HY-100982
    (E)-4-Hydroxycrotonic acid

    trans-4-Hydroxycrotonic acid; trans-γ-Hydroxycrotonic acid; T‐HCA

    		 Others Neurological Disease
    (E)-4-Hydroxycrotonic acid (T-HCA) is a high-affinity ligand for GHB binding sites, with a ki value of 1.1 μM. The introduction of diaryl substituents into (E)-4-Hydroxycrotonic acid significantly enhances its affinity for GHB binding sites, with ki values ranging from 0.023 to 0.075 μM. (E)-4-Hydroxycrotonic acid holds promise for optimizing GHB ligand structures and assisting in the development of effective three-dimensional pharmacophore models .
    (E)-4-Hydroxycrotonic acid
  • HY-101301A
    RS 45041-190 hydrochloride

    		Imidazoline Receptor Neurological Disease
    RS 45041-190 hydrochloride is a high-affinity ligand for I2 imidazoline receptors, with the pKis of 8.66, 9.37, 9.32, and 8.85 in rat, rabbit, dog and baboon kidney, respectively. RS 45041-190 hydrochloride shows moderate potency for the inhibition of monoamine oxidase A in vitro (pIC50= 6.12), but had much lower potency for monoamine oxidase B (pIC50 = 4.47) .
    RS 45041-190 hydrochloride
  • HY-133486
    GABAA receptor agent 1

    		GABA Receptor Neurological Disease
    GABAA receptor agent 1 is a high affinity ligand for GABAA receptor, with potent anticonvulsant activity .
    GABAA receptor agent 1
  • HY-145938
    OncoFAP

    		FAP Cancer
    OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
    OncoFAP
  • HY-103223
    Phortress

    NSC 710305

    		 Cytochrome P450 Cancer
    Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1 .
    Phortress
  • HY-122612
    SB-258585

    		5-HT Receptor Neurological Disease
    SB-258585 is a selective ligand with high affinity for the 5-HT6 receptor, with a pKi value of 8.53 .
    SB-258585
  • HY-100930
    L-693403 maleate

    		Sigma Receptor Neurological Disease
    L-693403 maleate is a high affinity and selective σ ligand. L-693403 maleate has the potential for physiological disease research .
    L-693403 maleate
  • HY-136280
    Panamesine

    EMD 57445

    		 Sigma Receptor Neurological Disease
    Panamesine (EMD 57445) is a sigma receptor ligand, which has a high affinity (IC50 6 nM) and selectivity for sigma binding sites. Panamesine is a potential atypical neuroleptic agent .
    Panamesine
  • HY-D1027
    Dansylcadaverine
    5+ Cited Publications

    Monodansyl cadaverine

    		 Autophagy Others
    Dansylcadaverine (Monodansyl cadaverine) is an autofluorescent compound used for the labeling of autophagic vacuoles. Dansylcadaverine, a high affinity substrate of transglutaminases, can block the receptor-mediated endocytosis of many ligands .
    Dansylcadaverine
  • HY-P99188
    Carlumab

    CNTO 888

    		 CCR Cancer
    Carlumab (CNTO 888) is a human anti-CCL2 (chemokine ligand 2) antibody with high affinity. Carlumab can be used in cancer research, particularly in prostate cancer .
    Carlumab
  • HY-115953
    Dopamine D3 receptor ligand-1

    		Dopamine Receptor Neurological Disease
    Dopamine D3 receptor ligand is a potent, selective and high affinity ligand for Dopamine D3 receptor with 89-fold selective for D3 over D2 (D3 Ki= 8 nM, D2 Ki= 715 nM) .
    Dopamine D3 receptor ligand-1
  • HY-U00180
    KF21213

    		Adenosine Receptor Neurological Disease
    KF21213 is a highly selective ligand for mapping CNS adenosine A2A receptors. KF21213 shows a high affinity for the adenosine A2A receptors (Ki=3.0 nM).
    KF21213
  • HY-P1464
    Amylin, amide, rat

    Amylin (rat)

    		 Amylin Receptor Metabolic Disease
    Amylin, amide, rat is a potent and high affinity ligand of Amylin receptor AMY1 and AMY3 receptors and variably of AMY2 receptors; binding studies are generally used for the latter receptor.
    Amylin, amide, rat
  • HY-B1033
    Metergoline
    1 Publications Verification

    		 5-HT Receptor Dopamine Receptor Sodium Channel Neurological Disease
    Metergoline is a serotonin (5-HT) receptor and dopamine receptors antagonist, with pKis of 8.64, 8.75 and 8.75 for 5-HT2A, 5-HT2B and 5-HT2C, respectively. Metergoline is a high-affinity ligand for the h5-HT7 receptor, with a Ki of 16 nM. Metergoline is also a reversible neural Na + channels inhibitor. Metergoline is commonly used for the research of seasonal affective disorder, prolactin hormone regulation .
    Metergoline
  • HY-139516
    AZD4694 Precursor

    AZ13040214; NAV4614

    		 Amyloid-β Others
    AZD4694 Precursor (AZ13040214) is the precursor of [ 18F] AZD4694 for the synthesis of [ 18F] AZD4694, an amyloid-β imaging ligand with high affinity for amyloid-β plaques .
    AZD4694 Precursor
  • HY-P99307
    Namilumab

    AMG-203; Anti-Human CSF2 Recombinant Antibody

    		 c-Fms Inflammation/Immunology
    Namilumab (AMG203) is a human IgG1 monoclonal antibody that binds with high affinity to the GM-CSF ligand, potently neutralizing GM-CSF. Namilumab can be used for the research of rheumatoid arthritis .
    Namilumab
  • HY-D2270
    Halo tag TMR

    		Fluorescent Dye Others
    Halo tag TMR is a fluorescent dye composed of Halo tag ligand molecules and TMR. Halo tag can rapidly form stable covalent binding with Halo protein with high specificity and high affinity .
    Halo tag TMR
  • HY-120842
    RLH-033

    		mAChR Neurological Disease
    RLH-033 is a potent and selective ligand for the sigma 1 recognition site. RLH-033 has high affinity for sigma 1 sites labeled by [ 3H](+)-pentazocine with a Ki of 50 pM .
    RLH-033
  • HY-118438
    10-Cl-BBQ

    		Aryl Hydrocarbon Receptor Inflammation/Immunology
    10-Cl-BBQ is a high affinity AhR ligand with immunosuppressive activity. 10-Cl-BBQ promotes cytosol to nuclear translocation of AhR and activates the AhR-regulated reporter gene at nanomolar concentrations .
    10-Cl-BBQ
  • HY-N0927
    (-)-Isocorypalmine

    Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine

    		 Dopamine Receptor Others
    (-)-Isocorypalmine (Tetrahydrocolumbamine), isolated from the crude base fraction of Corydalis chaerophylla, is a dopamine receptor ligand . Recombinant CYP719A21 displays strict substrate specificity and high affinity (Km=4.63 ± 0.71 μM) for (-)-Isocorypalmine .
    (-)-Isocorypalmine
  • HY-13956S
    Pioglitazone-d4

    U 72107-d4

    		 PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone-d4 is a deuterium labeled Pioglitazone. Pioglitazone (U 72107) is a potent and selective PPARγ agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively[1].
    Pioglitazone-d4
  • HY-N0443
    N-Methylcytisine
    1 Publications Verification

    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 .
    N-Methylcytisine
  • HY-115462
    PGN-9856

    		Prostaglandin Receptor Inflammation/Immunology
    PGN-9856 is a selective and high affinity (pKi ≥ 8.3) ligand at EP2 receptor. PGN-9856 is a potetn and non-prostanoid EP2 receptor agonist (pEC50 ≥ 8.5). PGN-9856 shows anti-inflammatory and anti-glaucoma activities .
    PGN-9856
  • HY-13956C
    (R)-Pioglitazone

    (R)-U 72107

    		 PPAR Neurological Disease
    (R)-Pioglitazone ((+)-pioglitazone) is the R enantiomer of Pioglitazone (HY-13956). (R)-Pioglitazone is an orally active and selective peroxisome proliferator-activated receptor (PPARγ) agonist with high affinity binding to the PPARγ ligand-binding domain. (R)-Pioglitazone can be used for the research of Alzheimer's disease .
    (R)-Pioglitazone
  • HY-100723
    THK-523

    		Amyloid-β Neurological Disease
    THK-523 has demonstrated its high affinity and selectivity for tau pathology both in vitro and in vivo. 18F-THK523 is a potent tau imaging radiotracer.? 18F-THK523 is a potent in vivo tau imaging ligand for Alzheimer's disease .
    THK-523
  • HY-130245
    PCSK9 degrader 1

    		PCSK9 Metabolic Disease
    PCSK9 degrader 1 (Compound 16) is a small molecule ligand for proprotein convertase substilisin-like/kexin type 9 (PCSK9) and shows high affinity to PCSK9 with a Ki of 107 nM. PCSK9 degrader 1 can involve in a protein-protein interaction with the low-density lipoprotein (LDL) receptor .
    PCSK9 degrader 1
  • HY-120236
    KSCM-5

    		Others Neurological Disease
    KSCM-5 is a sigma receptor ligand with high affinity activity on sigma-1 receptor. The Ki value of KSCM-5 is about 34nM, showing significant selectivity. KSCM-5 has potential application value in compound development, especially for diseases related to sigma receptors .
    KSCM-5
  • HY-13956
    Pioglitazone
    Maximum Cited Publications
    27 Publications Verification

    U 72107

    		 PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone (U 72107) is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone can be used in diabetes research .
    Pioglitazone
  • HY-13956B
    Pioglitazone potassium

    U 72107 potassium

    		 PPAR Ferroptosis Metabolic Disease Cancer
    Pioglitazone (U 72107) potassium is an orally active and selective PPARγ (peroxisome proliferator-activated receptor) agonist with high affinity binding to the PPARγ ligand-binding domain with EC50 of 0.93 μM and 0.99 μM for human and mouse PPARγ, respectively. Pioglitazone potassium can be used in diabetes research .
    Pioglitazone potassium
  • HY-155514
    HA-IN-1

    		Influenza Virus Inflammation/Immunology
    HA-IN-1 (compound 5g) is a Hemagglutinin (HA) ligand with high affinity, targeting to the trypsin cleavage site of HA. HA-IN-1 inhibits HA-mediated membrane fusion and reduces the pulmonary virus titer in vivo. HA-IN-1 is a potential influenza A virus (IAV) inhibitor, and an anti-influenza agent .
    HA-IN-1
  • HY-P1520
    Prolactin Releasing Peptide (1-31), human

    		GnRH Receptor Neurological Disease
    Prolactin Releasing Peptide (1-31), human is a high affinity GPR10 ligand that cause the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
    Prolactin Releasing Peptide (1-31), human
  • HY-P1520A
    Prolactin Releasing Peptide (1-31), human acetate

    		GnRH Receptor Neurological Disease
    Prolactin Releasing Peptide (1-31), human (acetate) is a high affinity GPR10 ligand that causes the release of the prolactin. Prolactin Releasing Peptide (1-31) binds to GPR10 for human and rats with Ki values of 1.03 nM and 0.33 nM, respectively. Prolactin Releasing Peptide (1-31) can be used for the research of the hypothalamo-pituitary axis .
    Prolactin Releasing Peptide (1-31), human acetate

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