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endogenous antagonist

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54

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15

Peptides

14

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5

Isotope-Labeled Compounds

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Cat. No. Product Name Target Research Areas Chemical Structure
  • HY-13677
    6-Mercaptopurine
    5+ Cited Publications

    Mercaptopurine; 6-MP

    Nucleoside Antimetabolite/Analog Autophagy Endogenous Metabolite Cancer
    6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.
    6-Mercaptopurine
  • HY-135103
    Tauro-β-muricholic acid sodium
    1 Publications Verification

    T-βMCA sodium

    FXR Cancer
    Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM .
    Tauro-β-muricholic acid sodium
  • HY-13677A
    6-Mercaptopurine hydrate
    5+ Cited Publications

    Mercaptopurine hydrate; 6-MP hydrate

    Nucleoside Antimetabolite/Analog Cancer
    6-Mercaptopurine hydrate (Mercaptopurine hydrate; 6-MP hydrate) is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent.
    6-Mercaptopurine hydrate
  • HY-10858A

    sFRP-1 Cancer
    WAY 316606 hydrochloride is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM .
    WAY 316606 hydrochloride
  • HY-120767

    KLH-2109 choline; OBE-2109 choline

    GnRH Receptor Inflammation/Immunology Cancer
    Linzagolix choline (KLH-2109 choline) is a non-peptide gonadotropin-releasing hormone (GnRH) antagonist with oral activity. Linzagolix choline inhibits the release of endogenous gonadotropins such as luteinizing hormone LH and follicle-stimulating hormone FSH by binding to the GnRH receptor within the pituitary gland. This inhibition results in a reduction in the production of sex hormones such as estrogen and progesterone, which in turn affects the course of sex hormone-dependent diseases. Linzagolix choline can be used in the study of sex hormone-dependent diseases such as endometriosis and uterine fibroids .
    Linzagolix choline
  • HY-120189

    iGluR Neurological Disease
    LY 233536 is a competitive NMDA receptor antagonist .
    LY 233536
  • HY-112874

    CCR Neurological Disease Inflammation/Immunology Cancer
    BMS-681 is an orthosteric antagonist of CC chemokine receptor 2 (CCR2). BMS-681 restricts the movement of the extracellular end of TM6 by stabilizing TM7. TM7 and TM6 are the main components of the orthosteric binding site. BMS-681 can be used to study inflammatory neurodegenerative diseases and cancer .
    BMS-681
  • HY-144204

    Estrogen Receptor/ERR Endocrinology Cancer
    Estrogen receptor antagonist 5 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 5 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 165) .
    Estrogen receptor antagonist 5
  • HY-144206

    Estrogen Receptor/ERR Endocrinology
    Estrogen receptor antagonist 6 is a potent antagonist of Estrogen receptor. The estrogen receptor is a ligand-activated transcriptional regulatory protein that mediates induction of a variety of biological effects through its interaction with endogenous estrogens. Estrogen receptor antagonist 6 has the potential for the research of metastatic disease (extracted from patent WO2017174757A1, compound 166) .
    Estrogen receptor antagonist 6
  • HY-P1628

    GnRH Receptor Metabolic Disease
    Ganirelix is a competitive and selective gonadotropin releasing hormone (GnRH) antagonist. Ganirelix prevents endogenous GnRH from inducing luteinising hormone (LH) and follicle stimulating hormone relea .
    Ganirelix
  • HY-P3066

    d(CH2)5Tyr(Et)VAVP

    Vasopressin Receptor Metabolic Disease
    SKF 100398 (d(CH2)5Tyr(Et)VAVP), an arginine vasopressin (AVP) analogue, is a specific antagonist of the antidiuretic effect of exogenous and endogenous AVP .
    SKF 100398
  • HY-107512
    Kynurenic acid sodium
    3 Publications Verification

    iGluR Apoptosis Endogenous Metabolite CXCR GPR35 Neurological Disease Inflammation/Immunology Endocrinology
    Kynurenic acid sodium, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid sodium is also an agonist of GPR35/CXCR8.
    Kynurenic acid sodium
  • HY-100806
    Kynurenic acid
    3 Publications Verification

    Quinurenic acid

    iGluR Endogenous Metabolite Apoptosis CXCR GPR35 Neurological Disease Inflammation/Immunology Endocrinology
    Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
    Kynurenic acid
  • HY-P0009

    SB-75

    GnRH Receptor Endocrinology
    Cetrorelix is a potent gonadotrophin-releasing hormone (GnRH) antagonist. Cetrorelix inhibits the endogenous luteinizing hormone surge during ovarian stimulation. Cetrorelix reduces cyclophosphamide induced ovarian follicular destruction in mice .
    Cetrorelix
  • HY-133890A
    Tauro-α-muricholic acid sodium
    1 Publications Verification

    T-α-MCA sodium

    Endogenous Metabolite FXR Others
    Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
    Tauro-α-muricholic acid sodium
  • HY-14752

    SB 751689

    CaSR Metabolic Disease Endocrinology
    Ronacaleret (SB 751689) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret (SB 751689) is used for the study of postmenopausal osteoporosis .
    Ronacaleret
  • HY-15104

    SB 751689A

    CaSR Metabolic Disease Endocrinology
    Ronacaleret hydrochloride (SB 751689A) is an orally active, potent, and selective calcium-sensing receptor (CaSR) antagonist that stimulates endogenous parathyroid hormone release from the parathyroid glands. Ronacaleret hydrochloride (SB 751689A) is used for the study of postmenopausal osteoporosis .
    Ronacaleret hydrochloride
  • HY-10858
    WAY 316606
    4 Publications Verification

    sFRP-1 Cancer
    WAY 316606 is an inhibitor of the secreted protein sFRP-1, an endogenous antagonist of the secreted glycoprotein Wnt. The affinity of WAY-316606 for sFRP-1 is determined using the FP binding assay with IC50 of 0.5 μM .
    WAY 316606
  • HY-109532

    Ganirest

    GnRH Receptor Metabolic Disease
    Ganirelix acetate (Ganirest) is an injectable competitive gonadotropin-releasing hormone (GnRH) antagonist. Ganirelix acetate directly competes against the endogenous molecule for receptor binding, and causes a rapid reduction in estradiol levels. Ganirelix acetate can be used for researching ovarian hyperstimulation syndrome (OHSS) .
    Ganirelix acetate
  • HY-13677S

    Mercaptopurine-d2; 6-MP-d2

    Isotope-Labeled Compounds Nucleoside Antimetabolite/Analog Autophagy Endogenous Metabolite Cancer
    6-Mercaptopurine-d2 is the deuterium labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent[1][2].
    6-Mercaptopurine-d2
  • HY-P1271

    Catestatin (cattle)

    nAChR Cardiovascular Disease
    Catestatin is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
    Catestatin
  • HY-13677R

    Nucleoside Antimetabolite/Analog Autophagy Endogenous Metabolite Cancer
    6-Mercaptopurine (Standard) is the analytical standard of 6-Mercaptopurine. This product is intended for research and analytical applications. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.
    6-Mercaptopurine (Standard)
  • HY-135103S

    FXR Cancer
    Tauro-β-muricholic acid-d4 (sodium) is the deuterium labeled Tauro-β-muricholic acid sodium. Tauro-β-muricholic Acid sodium (T-βMCA sodium), a endogenous metabolite, is a competitive and reversible farnesoid X receptor (FXR) antagonist, with an IC50 of 40 μM[1][2][3].
    Tauro-β-muricholic acid-d4 sodium
  • HY-139576

    DUR-928

    Endogenous Metabolite Metabolic Disease
    Larsucosterol (DUR-928), a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol as a potent endogenous regulator decreases lipogenesis. Larsucosterol inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1 .
    Larsucosterol
  • HY-139576A

    DUR-928 sodium

    Endogenous Metabolite Metabolic Disease
    Larsucosterol (DUR-928) sodium, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol sodium as a potent endogenous regulator decreases lipogenesis. Larsucosterol sodium inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1 .
    Larsucosterol sodium
  • HY-117541

    Glycyl-L-glutamine

    Others Neurological Disease
    Glycyl-glutamine (Glycyl-L-glutamine), as a enzymatic cleavage product of β-endorphin, is apparently an endogenous antagonist of beta-endorphin(1-31) in several systems . Glycyl-glutamine (Glycyl-L-glutamine) is an activate and stable glutamine-containing neuropeptide over glutamine (Gln) .
    Glycyl-glutamine
  • HY-P1271A

    nAChR Cardiovascular Disease
    Catestatin TFA is a 21-amino acid residue, cationic and hydrophobic peptide. Catestatin TFA is an endogenous peptide that regulates cardiac function and blood pressure . Catestatin TFA is a non-competitive nicotinic antagonist acting through nicotinic acetylcholine receptors (nAChRs) to inhibit catecholamine release .
    Catestatin TFA
  • HY-13677S1

    Mercaptopurine-13C2,15N; 6-MP-13C2,15N

    Nucleoside Antimetabolite/Analog Autophagy Endogenous Metabolite Cancer
    6-Mercaptopurine- 13C2, 15N is the 13C- and 15N-labeled 6-Mercaptopurine. 6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent.
    6-Mercaptopurine-13C2,15N
  • HY-100806S

    Quinurenic acid-d5

    Isotope-Labeled Compounds iGluR Endogenous Metabolite Apoptosis CXCR GPR35 Neurological Disease Inflammation/Immunology Endocrinology
    Kynurenic acid-d5 is the deuterium labeled Kynurenic acid. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8 .
    Kynurenic acid-d5
  • HY-100806R
    Kynurenic acid (Standard)
    3 Publications Verification

    Quinurenic acid (Standard)

    iGluR Endogenous Metabolite Apoptosis CXCR GPR35 Neurological Disease Inflammation/Immunology Endocrinology
    Kynurenic acid (Standard) is the analytical standard of Kynurenic acid. This product is intended for research and analytical applications. Kynurenic acid, an endogenous tryptophan metabolite, is a broad-spectrum antagonist targeting NMDA, glutamate, α7 nicotinic acetylcholine receptor. Kynurenic acid is also an agonist of GPR35/CXCR8.
    Kynurenic acid (Standard)
  • HY-13677AR

    Nucleoside Antimetabolite/Analog Cancer
    6-Mercaptopurine hydrate (Standard) is the analytical standard of 6-Mercaptopurine hydrate. This product is intended for research and analytical applications. 6-Mercaptopurine hydrate (Mercaptopurine hydrate; 6-MP hydrate) is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive agent.
    6-Mercaptopurine hydrate (Standard)
  • HY-139576B

    DUR-928 (trimethylamine)

    LXR Endogenous Metabolite Metabolic Disease
    Larsucosterol (DUR-928) trimethylamine, a cholesterol metabolite, is a potent liver X receptor (LXR) antagonist. Larsucosterol trimethylamine as a potent endogenous regulator decreases lipogenesis. Larsucosterol trimethylamine inhibits the cholesterol biosynthesis via decreasing mRNA levels and inhibiting the activation of SREBP-1 .
    Larsucosterol (trimethylamine)
  • HY-N6776

    Potassium Channel Neurological Disease Cancer
    Penitrem A is an indole diterpene neurotoxic alkaloid produced by Penicillium, acts as a selective BK channel antagonist with antiproliferative and anti-invasive activities against multiple malignancies. Penitrem A increases the spontaneous release of endogenous glutamate, gamma-aminobutyric acid (GABA) and aspartate from cerebrocortical synaptosomes, and induces tremorgenic syndromes in animals .
    Penitrem A
  • HY-110098

    EPPTB

    Trace Amine-associated Receptor (TAAR) Neurological Disease
    Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (Ki=0.9 nM for mouse TAAR1), with no significant effects on other TAARs. TAAR1 is a G protein-coupled receptor (GPCR) that is nonselectively activated by endogenous metabolites of amino acids .
    Ro 5212773
  • HY-P3839

    Opioid Receptor Neurological Disease
    Nocistatin, a neuropeptide, is an endogenous ligand for the orphan opioid receptor-like receptor. Nocistatin is also a functional antagonist of neuropeptide nociceptin or orphanin FQ (Noc/OFQ). Nocistatin inhibits 5-HT release via a Gi/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .
    Nocistatin
  • HY-W650803

    A-57219

    Adrenergic Receptor Cardiovascular Disease
    Nemazoline (A-57219) is selective α-adrenergic agent with α1-agonist/α2-antagonist activity, which is used as a nasal decongestant. Nemazoline produces decongestion by α1-mediated contraction of capacitance vessels, but not compromises blood flow by virtue of α2-antagonism. Nemazoline also blocks endogenous noradrenaline-mediated α 2-constriction of the resistance vessels .
    Nemazoline
  • HY-W654353

    T-α-MCA-d4-1 sodium

    Isotope-Labeled Compounds FXR Endogenous Metabolite Others
    Tauro-α-muricholic acid-d4-1 (sodium) is deuterium labeled Tauro-α-muricholic acid (sodium). Tauro-α-muricholic acid (T-α-MCA) sodium is a FXR (Farnesoid X receptor) antagonist (IC50=28μM). Tauro-α-muricholic acid sodium is also a endogenous metabolite that can be found in cecal .
    Tauro-α-muricholic acid-d4-1 sodium
  • HY-P0264
    Exendin(9-39) amide
    Maximum Cited Publications
    25 Publications Verification

    Avexitide

    GLP Receptor Metabolic Disease
    Exendin(9-39) amide (Avexitide) is a glucagon-like peptide-1 (GLP-1) antagonist that competes with endogenous GLP-1 for binding to GLP-1 receptors, thereby antagonizing the effects of excess GLP-1 secretion. Exendin(9-39) amide can be used to study postoperative hypoglycemia (PBH) .
    Exendin(9-39) amide
  • HY-P0264A

    Avexitide acetate

    GLP Receptor Metabolic Disease
    Exendin(9-39) amide (Avexitide) acetate is a glucagon-like peptide-1 (GLP-1) antagonist that competes with endogenous GLP-1 for the GLP-1R, counteracting the effects of excessive GLP-1 secretion. Exendin(9-39) amide acetate can be utilized in Postbariatric hypoglycemia (PBH) research .
    Exendin(9-39) amide acetate
  • HY-W050122

    Others Neurological Disease
    S-(+)-GABOB is an endogenous ligand with antiepileptic activity. S-(+)-GABOB is a metabolite of GABA and may function as a neurotransmitter. S-(+)-GABOB behaves as a full agonist when bound to the ρ(1) wild-type receptor. S-(+)-GABOB acts as a competitive antagonist in the ρ(1) T244S mutant receptor .
    S-(+)-GABOB
  • HY-N2908

    Methyl atrarate

    Androgen Receptor NO Synthase p38 MAPK NF-κB Inflammation/Immunology Cancer
    Atraric acid (Methyl atrarate) is a specific androgen receptor (AR) antagonist with anti-inflammatory and anticancer effects. Atraric acid represses the expression of the endogenous prostate specific antigen gene in both LNCaP and C4-2 cells. Atraric acid can also inhibit the synthesis of NO and cytokine, and suppress the MAPK-NFκB signaling pathway. Atraric acid can be used to research prostate diseases and inflammatory diseases .
    Atraric acid
  • HY-129668

    Adrenergic Receptor Neurological Disease
    Bremazocine is a potent opioid kappa receptor agonist with analgesic activity. Bremazocine induces peripheral analgesia by releasing endogenous norepinephrine. The analgesic effect of bremazocine is associated with interaction with adenosine receptors. Bremazocine produces a dose-dependent peripheral analgesia after topical application. The effect of bremazocine is affected by nonselective α(2) adrenaline receptor antagonists, suggesting that it acts through a norepinephrine pathway .
    Bremazocine
  • HY-W010820

    P2Y Receptor DNA/RNA Synthesis Endogenous Metabolite Metabolic Disease Inflammation/Immunology
    Uridine 5'-diphosphate sodium salt is a potent, selective P2Y6 receptor native agonist (EC50=300 nM; pEC50=6.52) and a potent P2Y14 antagonist (pEC50=7.28). Uridine 5'-diphosphate sodium salt, an endogenous metabolite, catalyzes the glucuronidation of a wide array of substrates and is used in nucleic acid (RNA) biosynthesis .
    Uridine 5'-diphosphate sodium salt
  • HY-108425

    Sodium Channel Neurological Disease
    AMG8379 is a potent, orally active and selective sulfonamide antagonist of the voltage-gated sodium channel NaV1.7, with IC50s of 8.5 and 18.6 nM for hNaV1.7 and mNaV1.7, respectively. AMG8379 potently and reversibly blocks endogenous Tetrodotoxin (TTX)-sensitive sodium channels in dorsal root ganglia (DRG) neurons with an IC50 of 3.1 nM .
    AMG8379
  • HY-P1318

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
    Ac-RYYRIK-NH2
  • HY-P1318A

    Opioid Receptor Neurological Disease
    Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (Kd=1.5 nM) and behaves as a endogenous ligand of ORL1. Ac-RYYRIK-NH2 is a specific antagonist for the activation of G protein and competitively antagonizes the stimulation of [ 35S]-GTPgS binding to G proteins by nociceptin/orphanin FQ (noc/OFQ) in membranes and sections of rat brain .
    Ac-RYYRIK-NH2 TFA
  • HY-124626

    Histamine Receptor Inflammation/Immunology
    (R)-(+)-Mequitazine is a histamine H1 receptor antagonist that mainly undergoes bio-transformation via human liver microsomes, resulting in hydroxylated and S-oxidized metabolites. (R)-(+)-Mequitazine competitively binds to the H1 receptors in gastrointestinal, vascular, and respiratory effect cells, thus blocking the endogenous activity of histamine. (R)-(+)-Mequitazine has an inhibitory effect on CYP3A-catalyzed midazolam 1’-hydroxylase. (R)-(+)-Mequitazine can be used in the study of various allergic diseases .
    (R)-(+)-Mequitazine
  • HY-118056

    Cannabinoid Receptor
    ABD459 is a CB1 receptor antagonist with significant effects on regulating food intake and sleep-wake cycles. ABD459 completely displaces CB1 agonist CP99540 (Ki = 8.6 nM) and antagonizes CP55940-induced GTPγS binding (KB = 7.7 nM). ABD459 may specifically modulate endogenous cannabinoid release through cholinergic activity and plays a role in attention and arousal regulation. ABD459 is suitable for research in neurological disorders .
    ABD459
  • HY-129207

    GHSR Endocrinology
    Ghrelin is an endogenous ligand for the growth hormone secretagogue receptor that stimulates food intake and transduces signals to hypothalamic regulatory nuclei that control energy homeostasis. JMV3002 is a potent ghrelin receptor antagonist with an IC50 value of 1.1 nM in vitro. 80 μg/kg, JMV3002 inhibits hexarelin-stimulated food intake by as much as 98% in rats. JMV3002 alone does not elicit growth hormone release nor does it inhibit hexarelin-stimulated growth hormone secretion when tested in infant rats at a dose of 160 μg/kg.
    JMV 3002
  • HY-165125

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

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