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high binding affinity and selectivity

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Click Chemistry

Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-P0186A

    Opioid Receptor Neurological Disease
    Endomorphin 2 TFA, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM .
    Endomorphin 2 TFA
  • HY-100155

    Sigma Receptor Cancer
    4-IBP is a selective σ1 agonist, binding to σ1 receptors with high affinity (Ki = 1.7 nM) and with slightly weaker affinity to σ2 receptors (Ki = 25.2 nM).
    4-IBP
  • HY-107568

    Histamine Receptor Inflammation/Immunology
    Iodophenpropit dihydrobromide is a potent and selective histamine H3 receptor antagonist. The binding of [ 125I]Iodophenpropit is selective, saturable, readily reversible, and of high affinity (KD 0.32 nM) .
    Iodophenpropit dihydrobromide
  • HY-160066

    Others Cancer
    SYL3C aptamer sodium is a DNA aptamer that targets the epithelial cell adhesion molecule (EpCAM) on the surface of cancer cells. SYL3C aptamer sodium targets multiple human cancer cell lines including MDA-MB-231, Kato III, HT-29, T47D and SW480. The Kd of SYL3C aptamer sodium against breast cancer cell line MDA-MB-231 and gastric cancer cell line Kato III is 38 nM and 67 nM, respectively. SYL3C aptamer sodium provides stability, high binding affinity, and selectivity for targeted cancer therapy, cancer cell imaging, and circulating tumor cell detection .
    SYL3C aptamer sodium
  • HY-P0186

    Opioid Receptor Neurological Disease
    Endomorphin 2, a high affinity, highly selective agonist of the μ-opioid receptor, displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM.
    Endomorphin 2
  • HY-136280

    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-P0185
    Endomorphin 1
    1 Publications Verification

    Opioid Receptor Neurological Disease
    Endomorphin 1, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 has antinociceptive properties .
    Endomorphin 1
  • HY-P0185A
    Endomorphin 1 acetate
    1 Publications Verification

    Opioid Receptor Neurological Disease
    Endomorphin 1 acetate, a high affinity, highly selective agonist of the μ-opioid receptor (Ki: 1.11 nM), displays reasonable affinities for kappa3 binding sites, with Ki value between 20 and 30 nM. Endomorphin 1 acetate has antinociceptive properties .
    Endomorphin 1 acetate
  • HY-117149

    Ras Cancer
    MLS000532223 is a high affinity, selective inhibitor of Rho family GTPases, with EC50 values ranging from 16 μM to 120 μM. MLS000532223 prevents GTP binding to several GTPases .
    MLS000532223
  • HY-12738

    Mineralocorticoid Receptor Progesterone Receptor Cardiovascular Disease Metabolic Disease
    PF-3882845 is a remarkably high affinity selective and orally efficacious mineralocorticoid receptor (MR binding IC50=2.7 nM) antagonist for hypertension and nephropathy. PF-3882845 also binds to progesterone receptor (PR) with the binding IC50 of 310 nM .
    PF-3882845
  • HY-101310

    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-13956S

    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-13956C

    (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-144397

    Glucocorticoid Receptor Inflammation/Immunology
    LEO 134310 is a selective, non-steroidal glucocorticoid receptor (GR) agonist optimized for topical research., LEO 134310 showed high affinity (EC50 of 14 nM) in a GR binding assay. LEO 134310 can be used for skin diseases .
    LEO 134310
  • HY-163317

    Somatostatin Receptor Cancer
    MMC(TMZ)-TOC has high binding affinity and selectivity for somatostatin receptor subtype-2 (SSTR2). MMC(TMZ)-TOC targets delivery of TMZ to SSTR2-positive tumor cells .
    MMC(TMZ)-TOC
  • HY-18628
    UMI-77
    1 Publications Verification

    Bcl-2 Family Cancer
    UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
    UMI-77
  • HY-149966

    HDAC Inflammation/Immunology
    PB131 is a selective and brain-permeable HDAC6 inhibitor with high binding affinity (IC50: 1.8 nM). PB131 has potent anti-inflammatory activity. PB131 can be used for research of inflammation, especially neuroinflammation .
    PB131
  • HY-15419
    RS-127445 hydrochloride
    2 Publications Verification

    5-HT Receptor Neurological Disease
    RS-127445 hydrochloride is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 hydrochloride shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
    RS-127445 hydrochloride
  • HY-15419A
    RS-127445
    2 Publications Verification

    5-HT Receptor Neurological Disease
    RS-127445 is a selective, high affinity, orally bioavailable 5-HT2B receptor antagonist with a pKi of 9.5. RS-127445 shows 1000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites .
    RS-127445
  • HY-13956
    Pioglitazone
    Maximum Cited Publications
    25 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

    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-100514
    GSK484 hydrochloride
    15+ Cited Publications

    Protein Arginine Deiminase Cardiovascular Disease Inflammation/Immunology Cancer
    GSK484 hydrochloride is a selective and reversible peptidylarginine deiminase 4 (PAD4) inhibitor. GSK484 hydrochloride demonstrates high affinity binding to PAD4 with IC50s of 50 nM in the absence of Calcium. In the presence of 2 mM Calcium, notably lower potency (250 nM) is observed.
    GSK484 hydrochloride
  • HY-127105A
    Iptacopan hydrochloride
    3 Publications Verification

    LNP023 hydrochloride

    Complement System Metabolic Disease Inflammation/Immunology
    LNP023 hydrochloride is an orally bioavailable, highly potent and highly selective factor B inhibitor. LNP023 shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. LNP023 inhibits factor B with an IC50 value of 10 nM .
    Iptacopan hydrochloride
  • HY-13956S1

    Isotope-Labeled Compounds PPAR Ferroptosis Metabolic Disease Cancer
    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[1][2].
    Pioglitazone-d4 (alkyl)
  • HY-100027A

    Monoamine Oxidase Neurological Disease
    Ro 41-1049 hydrochloride is a reversible and selective inhibitor of monoamine oxidase-A (MAO-A). An homogeneous population of high affinity binding sites for [ 3H]Ro 41-1049 is found in membrane preparations from human frontal cortex and placenta (Kd values of 16.5 and 64.4 nM, respectively) .
    Ro 41-1049 hydrochloride
  • HY-150654

    Histone Methyltransferase Cancer
    WDR5-IN-5 is an orally active and selective inhibitor of WIN site of WD repeat domain 5 (WDR5). WDR5-IN-5 exhibits anti-proliferative activity towards cancer cells and good pharmacokinetics profile in mice. WDR5-IN-5 shows high affinity to WDR5 and the binding affinity Ki value <0.02 nM .
    WDR5-IN-5
  • HY-18628S

    Isotope-Labeled Compounds Bcl-2 Family Cancer
    UMI-77-d4 is the deuterium labeled UMI-77. UMI-77 is a selective Mcl-1 inhibitor, which shows high binding affinity to Mcl-1 (IC50=0.31 μM). UMI-77 binds to the BH3 binding groove of Mcl-1 with Ki of 490 nM, showing selectivity over other members of anti-apoptotic Bcl-2 members.
    UMI-77-d4
  • HY-109012A
    Seltorexant hydrochloride
    1 Publications Verification

    JNJ-42847922 hydrochloride

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Seltorexant hydrochloride (JNJ-42847922 hydrochloride) is an orally active, high-affinity, and selective OX2R antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant hydrochloride crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
    Seltorexant hydrochloride
  • HY-13956R

    PPAR Ferroptosis Metabolic Disease Cancer
    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 .
    Pioglitazone (Standard)
  • HY-127105
    Iptacopan
    3 Publications Verification

    LNP023

    Complement System Metabolic Disease Inflammation/Immunology
    Iptacopan (LNP023) is a first-in-class, orally bioavailable, highly potent and highly selective factor B inhibitor with an IC50 value of 10 nM. Iptacopan shows direct, reversible, and high-affinity binding to human factor B with a KD of 7.9 nM. Iptacopan targets the underlying cause of complement 3 glomerulopathy (C3G) .
    Iptacopan
  • HY-107322

    Mepirodipine hydrochloride; YM-09730-5

    Calcium Channel Cardiovascular Disease
    Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
    Barnidipine hydrochloride
  • HY-107322A

    Mepirodipine; YM-09730-5 Free base

    Calcium Channel Cardiovascular Disease
    Barnidipine (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
    Barnidipine
  • HY-10835
    DG-041
    2 Publications Verification

    Prostaglandin Receptor Cardiovascular Disease
    DG-041 is a potent, high affinity and selective EP3 receptor antagonist with IC50s of 4.6 nM and 8.1 nM in the binding and FLIPR assay, respectively. DG-041 inhibits PGE2 facilitation of platelet aggregation. DG-041 crosses the blood-brain barrier .
    DG-041
  • HY-105215

    Neurokinin Receptor Inflammation/Immunology
    FK888 is a potent, selective, and high affinity dipeptide NK1 receptor antagonist. FK888 displaces [3H]-SP binding with a Ki value of 0.69 nM and 0.45 microM. FK888 also inhibits SP-induced airway oedema in guinea-pig after both intravenous and oral administration .
    FK888
  • HY-B0601
    Tafluprost acid
    1 Publications Verification

    AFP-172

    Prostaglandin Receptor Drug Metabolite Cardiovascular Disease Neurological Disease Endocrinology
    Tafluprost acid (AFP-172), an active metabolic form of Tafluprost, is a selective prostanoid FP receptor agonist. Tafluprost acid shows a high affinity for human prostanoid FP receptor with Ki and EC50 values of 0.4 nM and 0.53 nM, respectively. Tafluprost acid has 126 times weaker binding affinity for prostanoid EP3 receptor (IC50=67 nM) than for the prostanoid FP receptor. Tafluprost acid can be used in the research of glaucoma .
    Tafluprost acid
  • HY-138879B

    (1S,5R)-CP-601927

    nAChR Neurological Disease
    CP-601932 ((1S,5R)-CP-601927) is a high-affinity partial agonist at α3β4 nAChR (Ki=21 nM; EC50=~ 3 μM). CP-601932 has the same high-binding affinity at α4β2 nAChR (Ki=21 nM) and an order of magnitude lower affinity for α6 and α7 nAChR subtypes. CP-601932 selectively decreases ethanol but not sucrose consumption and operant self-administration following long-term exposure. CP-601932 can penetrate the CNS .
    CP-601932
  • HY-136214

    Integrin Inflammation/Immunology Cancer
    R-BC154 acetate is a selective fluorescent α9β1 integrin antagonist. R-BC154 acetate acts as a useful high affinity, activation dependent integrin probe, which can be used to investigate α9β1 and α4β1 integrin binding activity .
    R-BC154 acetate
  • HY-109012
    Seltorexant
    1 Publications Verification

    JNJ-42847922

    Orexin Receptor (OX Receptor) Neurological Disease Endocrinology
    Seltorexant (JNJ-42847922) is an orally active, high-affinity, and selective orexin-2 receptor (OX2R) antagonist (pKi values of 8.0 and 8.1 for human and rat OX2R). Seltorexant (JNJ-42847922) crosses the blood-brain barrier and quickly occupies OX2R binding sites in the rat brain .
    Seltorexant
  • HY-14495

    EX-1314

    GHSR Metabolic Disease
    BMS-604992 (EX-1314) is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 demonstrates high-affinity binding (Ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 can stimulate food intake in rodents .
    BMS-604992
  • HY-14495B

    EX-1314 dihydrochloride

    GHSR Metabolic Disease
    BMS-604992 (EX-1314) dihydrochloride is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 dihydrochloride demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 dihydrochloride can stimulate food intake in rodents .
    BMS-604992 dihydrochloride
  • HY-14604

    SR57746A; SR57746 hydrochloride

    5-HT Receptor Dopamine Receptor Neurological Disease
    Xaliproden hydrochloride (SR57746A) is a potent, selective and orally active agonist of 5-HT1A receptor, shows a high affinity for 5-HT1A specific binding sites in the rat hippocampus (IC50=3 nM). Xaliproden hydrochloride is also a selective antagonist of dopamine D2 receptor, has moderate affinity (IC50=0.1-1 μM). Xaliproden hydrochloride exhibits anti-depression and anti-anxiety effects, and it may possess therapeutic potential for the research of neurodegenerative diseases .
    Xaliproden hydrochloride
  • HY-117930
    Danicopan
    3 Publications Verification

    ACH-4471

    Complement System Inflammation/Immunology
    Danicopan (ACH-4471), a selective and orally active small-molecule factor D inhibitor, shows high binding affinity to human Factor D with Kd value of 0.54 nM. Danicopan (ACH-4471) inhibits alternative pathway of complement (APC) activity, has potential to block the alternative pathway of complement in paroxysmal nocturnal hemoglobinuria (PNH) and atypical hemolytic uremic syndrome (aHUS) .
    Danicopan
  • HY-101083

    Bcl-2 Family Cancer
    BDA-366 is a potent Bcl2 antagonist (Ki = 3.3 nM), binding Bcl2-BH4 domain with high affinity and selectivity. BDA-366 induces conformational change in Bcl2 that abrogates its antiapoptotic function, converting it from a survival molecule to a cell death inducer. BDA-366 suppresses growth of lung cancer cells .
    BDA-366
  • HY-14495A

    EX-1314 free base

    GHSR Metabolic Disease
    BMS-604992 (EX-1314) free base is a selective, orally active small-molecule growth hormone secretagogue receptor (GHSR) agonist. BMS-604992 free base demonstrates high-affinity binding (ki=2.3 nM) and potent functional activity (EC50=0.4 nM). BMS-604992 free base can stimulate food intake in rodents .
    BMS-604992 free base
  • HY-107322S

    Mepirodipine-d5 hydrochloride; YM-09730-5-d5 hydrochloride

    Isotope-Labeled Compounds Calcium Channel Cardiovascular Disease
    Barnidipine-d5 (hydrochloride) is the deuterium labeled Barnidipine hydrochloride. Barnidipine hydrochloride (Mepirodipine hydrochloride) is an L-type calcium antagonist (CaA) with high affinity for [3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors[1].Barnidipine hydrochloride (Mepirodipine hydrochloride) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action[2].
    Barnidipine-d5 hydrochloride
  • HY-125821

    Sigma Receptor Neurological Disease
    Sigma‑1 receptor antagonist 1 (compound 137) is a potent and selective sigma-1 receptor (σ1R) antagonist, with a high binding affinity to σ1R receptor (Ki = 1.06 nM). Sigma‑1 receptor antagonist 1 exhibits antineuropathic pain activity and acts as a promising agent for the treatment of neuropathic pain .
    Sigma-1 receptor antagonist 1
  • HY-147336

    Drug Metabolite Infection Cardiovascular Disease Metabolic Disease Inflammation/Immunology
    Desmethylazelastine is a main active metabolite of Azelastine that is oxidatively metabolized by the cytochrome P450 enzyme system with a protein binding rate of 97% and an elimination half-life of 54 hours. Azelastine is an orally active, selective and high-affinity histamine H1-receptor antagonist. Azelastine can be used in studies of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2 .
    Desmethylazelastine
  • HY-147060

    DYRK Neurological Disease
    Dyrk1A-IN-3 (Compound 8b), a highly selective  dual-specificity tyrosine-regulated kinase 1A (DYRK1A) inhibitor, maintains high levels of DYRK1A binding affinity (IC50=76 nM). Dyrk1A-IN-3 can be used for the research of neurodegenerative disorders such as Alzheimer’s Disease, Huntington’s Disease, and Parkinson’s Disease .
    Dyrk1A-IN-3
  • HY-124602

    E1/E2/E3 Enzyme Cancer
    DI-591 is a potent, high-affinity and cell-permeable inhibitor of the DCN1-UBC12 interaction. DI-591 binds to DCN1 and DCN2 with Ki values of 12 nM and 10.4 nM, respectively and has no appreciable binding to DCN3, DCN4, and DCN5 proteins. DI-591 selectively inhibits neddylation of cullin 3 but has no or minimal effect on neddylation of other cullin family members .
    DI-591
  • HY-107322AS1

    Mepirodipine-d5; YM-09730-5-d5 Free base

    Isotope-Labeled Compounds Others
    Barnidipine-d5 is the deuterium-labeled Barnidipine (HY-107322A). Barnidipine-d5 (Mepirodipine) is an L-type calcium antagonist (CaA) with high affinity for [ 3H] initrendipine binding sites (Ki=0.21 nmol/l), has selective action against CaA receptors . Barnidipine-d5 (Mepirodipine) is an antihypertensive agent and acts by the reduction of peripheral vascular resistance secondary to its vasodilatory action .
    Barnidipine-d5

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