Search Result
Results for "
high-affinity ligand
" in MedChemExpress (MCE) Product Catalog:
2
Isotope-Labeled Compounds
| Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-P1840
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Neuropeptide Y Receptor
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Neurological Disease
Endocrinology
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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 .
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- HY-112210
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Shld1
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FKBP
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Others
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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) .
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- HY-P5964A
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- HY-154844
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Biochemical Assay Reagents
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Cancer
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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 .
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- HY-P1840A
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Neuropeptide Y Receptor
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Neurological Disease
Endocrinology
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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 .
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- HY-P5964
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- HY-P5054
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- HY-162553
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Ligands for E3 Ligase
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Cancer
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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 .
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- HY-155698
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Fluorescent Dye
CXCR
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Others
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Mz438 is high-affinity and selective fluorescent CXCR2 ligand. Mz438 is a small-molecule-based fluorescent probe targeting the IABS of CXCR2 .
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- HY-121738
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- HY-P1887
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HSP
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Infection
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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 .
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- HY-114306
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Antifolate
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Cancer
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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) .
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- HY-117379
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Adrenergic Receptor
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Others
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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 .
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- HY-170789
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Histamine Receptor
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Neurological Disease
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H1R ligand-1 (Compound fragment 1) is a high-affinity ligand for the human histamine H1 receptor (H1R). H1R ligand-1 can be used as a scaffold to design and synthesize a set of derivatives to explore H1R binding kinetics .
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- HY-168440
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Ligands for Target Protein for PROTAC
Aurora Kinase
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Cancer
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Aurora-A ligand 1 is a high-affinity and specific Aurora-A inhibitor with a dissociation constant (Kd) value of 0.85 nM. Aurora-A ligand 1 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC Aurora-A degraders with antitumor activity. Aurora-A ligand 1 can be used for the synthesis of HLB-0532259 (HY-168439). HLB-0532259 shows anti-tumor activity against neuroblastoma .
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- HY-149933
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Cannabinoid Receptor
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Neurological Disease
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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 .
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- HY-P2112
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DOTA-Nal3-octreotide
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Others
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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 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-D1643
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Biochemical Assay Reagents
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Others
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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 .
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- HY-W020790
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sLeX
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Endogenous Metabolite
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Inflammation/Immunology
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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 .
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- HY-100982
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trans-4-Hydroxycrotonic acid; trans-γ-Hydroxycrotonic acid; T‐HCA
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GABA Receptor
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Neurological Disease
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(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 .
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- HY-100583
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- HY-176502
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FKBP
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Cancer
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FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels .
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- HY-D2413
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BODIPY FL PEG4-VH032
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Fluorescent Dye
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Others
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BODIPY FL VH032 is a high-affinity VHL fluorescent probe with a Kd value of 3.01 nM. BODIPY FL VH032 consists of von Hippel-Lindau (VHL) ligand VH032 (HY-120217) and BODIPY FL (HY-43520). BODIPY FL VH032 can be used for time-resolved fluorescence resonance energy transfer (TR-FRET) detection for high-throughput identification and characterization of VHL ligands with maximum excitation emission wavelength: 504/520 nm .
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- HY-101301A
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Imidazoline Receptor
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Neurological Disease
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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) .
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- HY-133486
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- HY-145938
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FAP
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Cancer
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OncoFAP is an ultra-high-affinity ligand of fibroblast activation protein (FAP) for targeting applications with pan-tumoral potential.
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- HY-103223
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NSC 710305
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Cytochrome P450
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Cancer
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Phortress is a high affinity AhR ligand that elicits antitumor activity by inducing transcription of CYP1A1 .
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- HY-122612
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- HY-100930
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- HY-112429
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HJB97
2 Publications Verification
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Ligands for Target Protein for PROTAC
Epigenetic Reader Domain
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Cancer
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HJB97 is a high-affinity BET inhibitor with Ki values of 0.9 nM (BRD2 BD1), 0.27 nM (BRD2 BD2), 0.18 nM (BRD3 BD1), 0.21 nM (BRD3 BD2), 0.5 nM (BRD4 BD1), and 1.0 nM (BRD4 BD2) . HJB97 can serve as a ligand for target protein (Ligands for Target Protein for PROTAC) for the development of PROTAC BET degraders with antitumor activity . HJB97 can be used for the synthesis of BETd-260 (HY-101519).
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- HY-172563
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Ligands for E3 Ligase
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Others
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BTR2000, a specifically KLHL20 ligand, is capable of binding to the KLHL20 Kelch domain with high affinity. BTR2000 can be used as a ligand for E3 ligase for the synthesis of BTR2004 (HY-172562) .
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- HY-136280
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EMD 57445
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Sigma Receptor
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Neurological Disease
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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 .
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- HY-100583R
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- HY-D1027
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Monodansyl cadaverine
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Autophagy
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Others
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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 .
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- HY-P99188
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CNTO 888
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CCR
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Cancer
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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 .
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- HY-115953
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Dopamine Receptor
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Neurological Disease
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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) .
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- HY-B1033
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5-HT Receptor
Dopamine Receptor
Sodium Channel
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Neurological Disease
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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 .
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- HY-P1464
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Amylin (rat)
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Amylin Receptor
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Metabolic Disease
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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.
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- HY-U00180
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Adenosine Receptor
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Neurological Disease
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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).
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- HY-139516
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AZ13040214; NAV4614
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Amyloid-β
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Others
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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 .
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- HY-P99307
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AMG-203; Anti-Human CSF2 Recombinant Antibody
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c-Fms
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Inflammation/Immunology
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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 .
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- HY-120842
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mAChR
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Neurological Disease
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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 .
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- HY-118438
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Aryl Hydrocarbon Receptor
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Inflammation/Immunology
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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 .
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- HY-P99036
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- HY-174440
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PSMA
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Cancer
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BWD is a PSMA ligand (IC50 = 35.86). BWD exhibits excellent in vitro stability and high affinity. BWD can enhance tumor uptake and retention. BWD can inhibit tumor growth in vivo. BWD can be studied in anticancer research .
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- HY-B1033R
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5-HT Receptor
Dopamine Receptor
Sodium Channel
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Neurological Disease
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Metergoline (Standard) is the analytical standard of Metergoline. This product is intended for research and analytical applications. 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 .
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- HY-N0927
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Tetrahydrocolumbamine; (S)-Tetrahydrocolumbamine
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Dopamine Receptor
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Others
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(-)-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 .
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- HY-170994
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Imidazoline Receptor
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Neurological Disease
Inflammation/Immunology
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I2-IRs ligand-1 (Compound 12d) is an orally active and BBB-penetrable compound. I2-IRs ligand-1 has a high affinity for imidazoline I2 receptors (I2-IRs) (pKi: 9.98). I2-IRs ligand-1 can improve cognitive impairment in senescent mice and exhibits analgesic, anti-inflammatory, and neuroprotective activities. I2-IRs ligand-1 can be used for the research of Alzheimer's disease and related pain disorders .
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- HY-13956S
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U 72107-d4
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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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 .
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- HY-173291
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Tau Protein
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Neurological Disease
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Tau ligand-1 (Compound 75) is a ligand for aggregated tau protein that can penetrate the blood-brain barrier . In tissues from patients with Alzheimer's disease, progressive supranuclear palsy, corticobasal degeneration, and Pick's disease, Tau ligand-1 exhibits high affinity for aggregated tau protein, with equilibrium dissociation constant (KD) values ranging from 1 to 3.8 nM . Tau ligand-1 can serve as a potential positron emission tomography (PET) tracer and holds promise for application in positron emission tomography imaging studies of tau-related diseases in the central nervous system .
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- HY-13956C
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(R)-U 72107
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PPAR
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Neurological Disease
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(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 .
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- HY-115462
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Prostaglandin Receptor
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Inflammation/Immunology
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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 .
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- HY-N0443
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Caulophylline
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nAChR
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Inflammation/Immunology
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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 .
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- HY-176501
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FKBP
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Cancer
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FKBP12 ligand-2 (compound d) is a high affinity ligand targeting FKBP12. FKBP12 ligand-2 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-2 can be used for selective cancer research based on differences in intracellular presenter protein levels .
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- HY-173045
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5-HT Receptor
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Cancer
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5-HT5AR/5-HT6R ligand-1 (Compound PP10) is a ligand for serotonin receptors, showing high affinity for 5-HT5A and 5-HT6 receptors, with Ki values of 59 nM and 96 nM, respectively. 5-HT5AR/5-HT6R ligand-1 exhibits certain antiproliferative activity against tumor cells and can be used in the study of cancer .
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- HY-100723
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Amyloid-β
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Neurological Disease
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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 .
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- HY-P99257
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ASKP 1240
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TNF Receptor
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Inflammation/Immunology
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Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with high affinity (Kd: 0.24 nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection .
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- HY-130245
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PCSK9
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Metabolic Disease
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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 .
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- HY-120236
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Sigma Receptor
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Neurological Disease
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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 .
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- HY-13956B
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U 72107 potassium
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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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 .
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- HY-155514
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Influenza Virus
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Inflammation/Immunology
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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 .
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- HY-13956
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Pioglitazone
Maximum Cited Publications
31 Publications Verification
U 72107
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PPAR
Ferroptosis
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Metabolic Disease
Cancer
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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 .
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- HY-P1520
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GnRH Receptor
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Neurological Disease
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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 .
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- HY-P99345
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TSR-042
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PD-1/PD-L1
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Cancer
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Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
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- HY-P1520A
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GnRH Receptor
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Neurological Disease
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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 .
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- HY-W042920A
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Adrenergic Receptor
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Neurological Disease
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TDIQ hydrochloride is an analog of Amphetamine with high affinity for α2-adrenergic receptor. TDIQ hydrochloride is a selective α2-adrenoceptor ligand with the Ki values of 75 nM, 95 nM, and 65 nM for α2A-, α2B-, and α2C-adrenergic receptors, respectively .
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- HY-103141
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5-HT Receptor
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Neurological Disease
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SB-258585 is a high affinity ligand for the 5-HT6 receptor. SB-258585 binds highly to a single receptor population in a human cell line that recombines 5-HT6 receptors. SB-258585 can be used to label recombinant and natural 5-HT6 receptor .
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- HY-13956S1
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Isotope-Labeled Compounds
PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the 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 .
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- HY-122607
-
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Mitochondrial Metabolism
TSPO
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Inflammation/Immunology
Cancer
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DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model .
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- HY-124892A
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Acetyl-AF64
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Histone Acetyltransferase
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Neurological Disease
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Acetylethylcholine mustard hydrochloride (Acetyl-AF64) is an inhibitor of choline acetyl-transferase that reduces the contraction frequency of the myotubes by inhibiting the synthesis of acetylethylcholine (Ach) with the half-maximal inhibitory concentration (IC50) of 1.22 mM. Acetylethylcholine mustard hydrochloride is an irreversible ligand for the high affinity choline transport system. Acetylethylcholine mustard hydrochloride is also a cholinotoxin. Acetylethylcholine mustard hydrochloride is a precursor for ethylcholine mustard aziridinium ion .
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- HY-N0443R
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Caulophylline (Standard)
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Reference Standards
nAChR
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Inflammation/Immunology
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N-Methylcytisine (Standard) is the analytical standard of N-Methylcytisine. This product is intended for research and analytical applications. 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 .
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- HY-100539
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Dopamine Receptor
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Others
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PD 128907 is a D3 receptor ligand with activities of activating dopamine receptors, inhibiting cell firing, and inhibiting dopamine release. The active (+) enantiomer of PD 128907 has high affinity and selectivity for rat D3 dopamine receptors. PD 128907 inhibits cell firing in the ventral tegmental area and substantia nigra pars compacta with EC50 values of 33nM and 38nM, respectively. PD 128907 also inhibits dopamine release in the caudate putamen with an EC50 of 66nM. However, the selective D2 receptor antagonist L-741,626 has high affinity for receptors activated by PD 128907, indicating that the effects of PD 128907 are more likely on D2 autoreceptors rather than D3 dopamine receptor subtypes.
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- HY-13956R
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U 72107 (Standard)
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Reference Standards
PPAR
Ferroptosis
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Metabolic Disease
Cancer
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Pioglitazone (Standard) is the analytical standard of Pioglitazone. This product is intended for research and analytical applications. 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 .
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- HY-103453
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Estrogen Receptor/ERR
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Endocrinology
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(R)-DPN (compound 3) is a selective ERβ ligand with EC50s of 2.9, 0.8 nM for ERα and ERβ, respectively. (R)-DPN shows a very high affinity and potency preference for ERβ over ERα. (R)-DPN shows cytoxicity for HEC-1 and U2OS cells with EC50s of 286, 205 nM, respectively .
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- HY-P99189
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IMC-A12; NSC742460
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IGF-1R
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Cancer
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Cixutumumab (IMC-A12) is a human anti-IGF-1R monoclonal antibody with high affinity that inhibits ligand-dependent receptor activation and downstream signaling. Cixutumumab also mediates the internalization and degradation of IGF-IR. Cixutumumab shows broad-spectrum anti-tumour activity and can be used in studies of cancers such as lung cancer, malignancies, leukaemia, non-small cell lung cancer and prostate cancer .
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- HY-176035
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PROTACs
Epigenetic Reader Domain
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Cancer
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MS479 is a BRD4 PROTAC degrader. MS479 binds BRD4-BD2 and GLP with high affinities (BRD4-BD2: Kd = 200 nM; GLP: Kd = 306 nM). MS479 can reduce the protein level of BRD4 short isoform. MS479 recruits the E3 ligase SPOP by directly binding its substrate GLP as a bridge protein. MS479 can be used to inhibit the proliferation of colorectal cancer cells. (Pink: BRD4 ligand (HY-78695); Blue: GLP ligand (HY-176036); Black: linker (HY-176037); GLP ligand+linker: HY-176038) .
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- HY-130245A
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PCSK9
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Metabolic Disease
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(R,R)-PCSK9 degrader 1 is the isomer of PCSK9 degrader 1 (HY-130245). 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 .
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- HY-152576
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Cannabinoid Receptor
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Inflammation/Immunology
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CB2R agonist 1 is a selective ligand of cannabinoid receptor subtype 2 (CB2R) with an EC50 value of 0.56 µM. CB2R agonist 1 has high affinity and excellent selectivity for human CB2R and CB1R respectively. CB2R agonist 1 regulates the production of pro-inflammatory cytokines and anti-inflammatory cytokines and play an immunomodulatory role .
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- HY-173138
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Monoamine Oxidase
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Neurological Disease
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FCOB02 is a monoamine oxidase B (MAO-B) ligand. FCOB02 can be labeled as [18F]FCOB02, a 4-methylcoumarin-like targeting probe. [18F]FCOB02 has a high affinity for MAO-B with an IC50 of 10.68 nM. [18F]FCOB02 can be used in specific MAO-B imaging as well as quantitative analysis in vivo .
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- HY-101170
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Imidazoline Receptor
Apoptosis
TNF Receptor
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Neurological Disease
Inflammation/Immunology
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BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research .
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- HY-14353
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LXR
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Neurological Disease
Inflammation/Immunology
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GSK-9772 is a Liver X Receptor (LXR) modulator of the N-phenyl tertiary amine class (NPTAs) with high affinity for LXR β ligand (IC50=30 nM). GSK-9772 has anti-inflammatory activity by binding to LXR, specifically by interacting with the region associated with the transcriptional repression function of the receptor, thereby inhibiting the expression of pro-inflammatory genes. GSK-9772 can be used in the study of inflammatory and neurodegenerative diseases .
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- HY-122607R
-
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Mitochondrial Metabolism
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Inflammation/Immunology
Cancer
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DPA-714 (Standard) is the analytical standard of DPA-714. This product is intended for research and analytical applications. DPA-714 is a high affinity translocator protein (TSPO) ligand (Ki=7 nM), which is designed with a fluorine atom in its structure, allowing labelling with fluorine -18 and in vivo imaging using positron emission tomography. 18FDPA-714 successfully evaluates for the specific imaging of inflammation in various models of neuroinflammation and in a brain tumor model .
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- HY-101393A
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(±)-CGP 12177 hydrochloride
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Adrenergic Receptor
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Cardiovascular Disease
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CGP 12177 ((±)-CGP 12177) hydrochloride is a β Adrenergic Receptor Ligand. CGP 12177 hydrochloride is a high affinity antagonist of β1- and β2-AR. CGP 12177 hydrochloride is also shown to interact, with a lower affinity, with the β3-AR and to exhibit a partial agonist activity on rodent and human β3-AR. CGP 12177 hydrochloride exhibits partial agonist properties for α1-AR in rat pulmonary artery .
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- HY-P10762
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LDC 10B
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Peptide-Drug Conjugates (PDCs)
Folate Receptor (FR)
TRP Channel
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Cancer
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CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) conjugated to MMAE (HY-15162), targeting Folate receptor α (FRα) and TRPV6. CBP-1008 binds to FRα with high affinity and TRPV6 with low affinity. CBP-1008 has antitumor activity, and can be used in advanced solid tumor research (eg: colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma and follicular dendritic cell sarcoma) .
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- HY-101170R
-
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Reference Standards
Imidazoline Receptor
Apoptosis
TNF Receptor
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Neurological Disease
Inflammation/Immunology
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BU224 (hydrochloride) (Standard) is the analytical standard of BU224 (hydrochloride). This product is intended for research and analytical applications. BU224 hydrochloride is a selective and high affinity imidazoline I2 receptor ligand, with a Ki of 2.1 nM. BU224 hydrochloride is sometimes used as an I2 receptor antagonist. BU224 hydrochloride exerts neuroprotective effects, with anti-inflammatory and anti-apoptotic properties. BU224 hydrochloride improves memory in 5XFAD mice, enlarging dendritic spines and reducing Aβ-induced changes in NMDARs. BU224 hydrochloride can be used for Alzheimer's disease research .
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- HY-116450
-
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Dopamine Receptor
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Neurological Disease
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TISCH is a potent and selective iodinated ligand with high affinity and selectivity for CNS D1 dopamine receptors. TISCH showed a Kd value of 0.205 nM in rat striatal tissue, indicating its effectiveness in biological activity. TISCH is able to easily cross the blood-brain barrier and show distribution in specific areas with D1 receptor density. TISCH is considered to be useful as a pharmacological tool for characterizing D1 dopamine receptors. When labeled with I-123, TISCH has the potential to be used as an in vivo imaging agent for CNS D1 dopamine receptors .
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- HY-121579
-
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PPAR
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Others
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L-764406 is a non-thiazolidinedione (TZD)-type PPARg nuclear receptor ligand with high affinity. L-764406 has significant binding ability to PPARg (IC50=70 nM). L-764406 exhibited partial agonist activity and induced expression of the adipocyte-specific gene aP2 in chimeric receptors expressing the PPARg LBD and the corresponding reporter gene, as well as in 3T3-L1 cells. In contrast, L-764406 showed no activity in cells transfected with chimeric receptors containing PPARa or PPARd LBDs .
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- HY-118124
-
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Endogenous Metabolite
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Others
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2-Iodoestradiol is a potent human sex hormone binding globulin (SHBG) ligand with a remarkably high affinity for SHBG. 2-Iodoestradiol exhibits competition for the same binding site as dihydrotestosterone in binding to human SHBG. The binding affinity constant of 2-Iodoestradiol at physiological pH and 37 degrees Celsius is 2.4 x 10(9) M-1, exceeding that for SHBG. 2-Iodoestradiol has been shown to bind to serum albumin, but with lower affinity. The radioisotope 125I-derivative of 2-Iodoestradiol has been used to study the binding properties of human SHBG, demonstrating its potential application in biological research .
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- HY-120874
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PF-06372865; CVL-865
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GABA Receptor
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Neurological Disease
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Darigabat (PF-06372865) is an orally active, α2/α3/α5 subtype-selective GABAA positive allosteric modulator (PAM). Darigabat is a high affinity ligand at GABAA receptors containing α1/α2/α3/α5 subunits (Kis of 2.9 nM, 21 nM, 134 nM for α2, α1 PAM, α2 PAM, respectively), with low affinity for α4/α6 subunits. Darigabat can across the blood-brain barrier (BBB). Darigabat has anxiolytic activity and has the potential for epilepsy .
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| Cat. No. |
Product Name |
Type |
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- HY-D1027
-
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Monodansyl cadaverine
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Fluorescent Dyes/Probes
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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 .
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- HY-D2413
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BODIPY FL PEG4-VH032
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Fluorescent Dyes/Probes
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BODIPY FL VH032 is a high-affinity VHL fluorescent probe with a Kd value of 3.01 nM. BODIPY FL VH032 consists of von Hippel-Lindau (VHL) ligand VH032 (HY-120217) and BODIPY FL (HY-43520). BODIPY FL VH032 can be used for time-resolved fluorescence resonance energy transfer (TR-FRET) detection for high-throughput identification and characterization of VHL ligands with maximum excitation emission wavelength: 504/520 nm .
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| Cat. No. |
Product Name |
Target |
Research Area |
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- HY-P1840
-
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Neuropeptide Y Receptor
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Neurological Disease
Endocrinology
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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 .
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- HY-P5964A
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- HY-P2112
-
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DOTA-Nal3-octreotide
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Radionuclide-Drug Conjugates (RDCs)
Somatostatin Receptor
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Others
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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 can be used for the synthesis/research of Radionuclide-Drug Conjugates (RDCs).
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- HY-P2288A
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Peptides
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Cancer
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WL47 TFA, a high-affinity cavolin-1 (CAV1) ligand (Kd=23 nM), is a potent disrupter of CAV1 oligomers. WL47 TFA shows selectivity for CAV1 over BSA, casein and HEWL. WL47 TFA is 80% smaller in length than the original T20 (HY-P0052) parent sequence and can be used for the study of caveolin-1 function .
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- HY-P1464
-
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Amylin (rat)
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Amylin Receptor
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Metabolic Disease
|
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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.
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- HY-P1840A
-
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Neuropeptide Y Receptor
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Neurological Disease
Endocrinology
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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 .
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- HY-P5964
-
-
- HY-P5054
-
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- HY-P1887
-
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HSP
|
Infection
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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 .
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- HY-P2288
-
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Peptides
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Cancer
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WL47, a high-affinity cavolin-1 (CAV1) ligand (Kd=23 nM), is a potent disrupter of CAV1 oligomers. WL47 shows selectivity for CAV1 over BSA, casein and HEWL. WL47 is 80% smaller in length than the original T20 (HY-P0052) parent sequence and can be used for the study of caveolin-1 function .
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- HY-P1530
-
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Peptides
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Neurological Disease
|
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Prolactin Releasing Peptide (12-31), human is a fragment of the prolactin releasing peptide (PrRP). Prolactin Releasing Peptide (1-31), human is a high affinity GPR10 ligand that cause the release of the prolactin.
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- HY-P10332
-
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Peptides
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Others
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WL 47 dimer (ligand 1) is a caveolin-1 (CAV-1) ligand with high affinity, selectivity and oligomer dissociation activity. WL 47 dimer simultaneously occupies two binding sites of CAV-1, inducing the dissociation of oligomers. WL 47 dimer has 7500-fold improved affinity compared to its T20 parent ligand and an 80% decrease in sequence length. WL 47 dimer can be used to permit targeted study of CAV-1 function .
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- HY-P1520
-
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|
GnRH Receptor
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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 .
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- HY-P1520A
-
|
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GnRH Receptor
|
Neurological Disease
|
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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 .
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-
- HY-P10762
-
|
LDC 10B
|
Peptide-Drug Conjugates (PDCs)
Folate Receptor (FR)
TRP Channel
|
Cancer
|
|
CBP-1008 is a dual-ligand peptide-drug conjugate (PDC) conjugated to MMAE (HY-15162), targeting Folate receptor α (FRα) and TRPV6. CBP-1008 binds to FRα with high affinity and TRPV6 with low affinity. CBP-1008 has antitumor activity, and can be used in advanced solid tumor research (eg: colorectal cancer, breast cancer, non-small cell lung cancer, ovarian cancer, adrenocortical carcinoma and follicular dendritic cell sarcoma) .
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| Cat. No. |
Product Name |
Target |
Research Area |
-
- HY-P99188
-
|
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 .
|
-
- HY-P99307
-
|
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 .
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-
- HY-P99036
-
-
- HY-P99763
-
|
BGB-A1217
|
Inhibitory Antibodies
|
Cancer
|
|
Ociperlimab is a humanized IgG1 anti-TIGIT antibody. Ociperlimab binds to the extracellular domain of human TIGIT with high affinity (KD = 0.135 nM). Ociperlimab blocks the interaction between TIGIT and its ligands PVR or PVR-L2. Ociperlimab can be used in research of cancer .
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-
- HY-P99257
-
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ASKP 1240
|
TNF Receptor
|
Inflammation/Immunology
|
|
Bleselumab (ASKP 1240) is a human anti-CD40 monoclonal antibody (mAb). Bleselumab binds to human CD40 with high affinity (Kd: 0.24 nM). Bleselumab inhibits immune responses by blocking the interaction of CD40 with its ligand CD40L. Bleselumab prevents organ transplant rejection .
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-
- HY-P99345
-
|
TSR-042
|
PD-1/PD-L1
|
Cancer
|
|
Dostarlimab (TSR-042) is a humanized anti-PD-1 monoclonal antibody. Dostarlimab binds with high affinity to human PD-1 and competitively inhibits its interaction with its ligands, PD-L1 and PD-L2, with IC50s of 1.8 and 1.5 nM, respectively .
|
-
- HY-P99189
-
|
IMC-A12; NSC742460
|
IGF-1R
|
Cancer
|
|
Cixutumumab (IMC-A12) is a human anti-IGF-1R monoclonal antibody with high affinity that inhibits ligand-dependent receptor activation and downstream signaling. Cixutumumab also mediates the internalization and degradation of IGF-IR. Cixutumumab shows broad-spectrum anti-tumour activity and can be used in studies of cancers such as lung cancer, malignancies, leukaemia, non-small cell lung cancer and prostate cancer .
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| Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
| Cat. No. |
Product Name |
Chemical Structure |
-
- HY-13956S
-
|
|
|
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 .
|
-
-
- HY-13956S1
-
|
|
|
Pioglitazone-d4 (alkyl) (U 72107-d4 (alkyl)) is the 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 .
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-
| Cat. No. |
Product Name |
|
Classification |
-
- HY-176502
-
|
|
|
Alkynes
|
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FKBP12 ligand-3 (compound dj) is a high-affinity ligand targeting FKBP12. FKBP12 ligand-3 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-3 can be used for selective cancer research based on differences in intracellular presenter protein levels .
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-
- HY-176501
-
|
|
|
Alkynes
|
|
FKBP12 ligand-2 (compound d) is a high affinity ligand targeting FKBP12. FKBP12 ligand-2 can be used to selectively enhance the binding of heterobifunctional molecules to BRD4, enriching the drug intracellularly through the "CellTrap" effect to form a ternary complex of FKBP12-ligand-BRD4. This ternary complex has inhibitory activity against BRD4, thereby inhibiting the expression of BRD4 target genes (such as MYC) and inducing tumor cell death. FKBP12 ligand-2 can be used for selective cancer research based on differences in intracellular presenter protein levels .
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