Search Result
Results for "
endogenous antagonist
" in MedChemExpress (MCE) Product Catalog:
5
Isotope-Labeled Compounds
Cat. No. |
Product Name |
Target |
Research Areas |
Chemical Structure |
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- HY-13677
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- HY-135103
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T-βMCA sodium
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FXR
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Cancer
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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 .
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- HY-13677A
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Mercaptopurine hydrate; 6-MP hydrate
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Nucleoside Antimetabolite/Analog
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Cancer
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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.
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- HY-10858A
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sFRP-1
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Cancer
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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 .
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- HY-120767
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KLH-2109 choline; OBE-2109 choline
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GnRH Receptor
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Inflammation/Immunology
Cancer
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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 .
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- HY-120189
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-
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- HY-112874
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CCR
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Neurological Disease
Inflammation/Immunology
Cancer
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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 .
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- HY-144204
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Estrogen Receptor/ERR
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Endocrinology
Cancer
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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) .
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- HY-144206
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Estrogen Receptor/ERR
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Endocrinology
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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) .
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- HY-P1628
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GnRH Receptor
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Metabolic Disease
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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 .
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- HY-P3066
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d(CH2)5Tyr(Et)VAVP
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Vasopressin Receptor
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Metabolic Disease
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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 .
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- HY-107512
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-
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- HY-100806
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-
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- HY-P0009
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SB-75
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GnRH Receptor
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Endocrinology
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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 .
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- HY-133890A
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T-α-MCA sodium
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Endogenous Metabolite
FXR
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Others
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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 .
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- HY-14752
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SB 751689
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CaSR
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Metabolic Disease
Endocrinology
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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 .
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- HY-15104
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SB 751689A
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CaSR
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Metabolic Disease
Endocrinology
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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 .
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- HY-10858
-
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sFRP-1
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Cancer
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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 .
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- HY-109532
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Ganirest
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GnRH Receptor
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Metabolic Disease
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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) .
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- HY-13677S
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- HY-P1271
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Catestatin (cattle)
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nAChR
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Cardiovascular Disease
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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 .
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- HY-13677R
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Nucleoside Antimetabolite/Analog
Autophagy
Endogenous Metabolite
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Cancer
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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.
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- HY-135103S
-
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FXR
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Cancer
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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].
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- HY-139576
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DUR-928
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Endogenous Metabolite
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Metabolic Disease
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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 .
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- HY-139576A
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DUR-928 sodium
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Endogenous Metabolite
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Metabolic Disease
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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 .
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- HY-117541
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Glycyl-L-glutamine
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Others
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Neurological Disease
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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) .
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- HY-P1271A
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nAChR
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Cardiovascular Disease
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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 .
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- HY-13677S1
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Mercaptopurine-13C2,15N; 6-MP-13C2,15N
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Nucleoside Antimetabolite/Analog
Autophagy
Endogenous Metabolite
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Cancer
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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.
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- HY-100806S
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- HY-100806R
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-
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- HY-13677AR
-
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Nucleoside Antimetabolite/Analog
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Cancer
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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.
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- HY-139576B
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DUR-928 (trimethylamine)
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LXR
Endogenous Metabolite
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Metabolic Disease
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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 .
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- HY-N6776
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Potassium Channel
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Neurological Disease
Cancer
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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 .
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- HY-110098
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EPPTB
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Trace Amine-associated Receptor (TAAR)
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Neurological Disease
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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 .
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- HY-P3839
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-W650803
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A-57219
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Adrenergic Receptor
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Cardiovascular Disease
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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 .
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- HY-W654353
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T-α-MCA-d4-1 sodium
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Isotope-Labeled Compounds
FXR
Endogenous Metabolite
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Others
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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 .
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- HY-P0264
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Avexitide
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GLP Receptor
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Metabolic Disease
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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) .
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- HY-P0264A
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Avexitide acetate
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GLP Receptor
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Metabolic Disease
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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 .
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- HY-W050122
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Others
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Neurological Disease
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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 .
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- HY-N2908
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Methyl atrarate
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Androgen Receptor
NO Synthase
p38 MAPK
NF-κB
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Inflammation/Immunology
Cancer
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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 .
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- HY-129668
-
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Adrenergic Receptor
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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 .
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- HY-W010820
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-
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- HY-108425
-
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Sodium Channel
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Neurological Disease
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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 .
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- HY-P1318
-
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-P1318A
-
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Opioid Receptor
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Neurological Disease
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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 .
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- HY-124626
-
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Histamine Receptor
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Inflammation/Immunology
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(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 .
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- HY-118056
-
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Cannabinoid Receptor
|
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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 .
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- HY-129207
-
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GHSR
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Endocrinology
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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.
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- HY-165125
-
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Neuropeptide Y Receptor
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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 .
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- HY-P1320
-
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Opioid Receptor
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Inflammation/Immunology
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
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- HY-P1320A
-
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Opioid Receptor
|
Inflammation/Immunology
|
[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
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- HY-30004
-
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Endogenous Metabolite
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Cardiovascular Disease
Metabolic Disease
|
1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
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- HY-30004R
-
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Endogenous Metabolite
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Cardiovascular Disease
Metabolic Disease
|
1-Aminocyclopropane-1-carboxylic acid (Standard) is the analytical standard of 1-Aminocyclopropane-1-carboxylic acid. This product is intended for research and analytical applications. 1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
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Cat. No. |
Product Name |
Target |
Research Area |
-
- 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 .
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- HY-P1271
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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 .
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- HY-P1271A
-
|
nAChR
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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 .
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- HY-P0264
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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) .
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- HY-P1628
-
|
GnRH Receptor
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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 .
|
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- HY-P0009
-
SB-75
|
GnRH Receptor
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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 .
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- HY-P3598
-
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Peptides
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Cancer
|
Substance P(1-4) is a potent neurokinin receptors (NK-R) antagonist. Substance P(1-4) has regulation of normal hematopoiesis and inhibits endogenous erythroid colony (EEC) formation .
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- HY-P3839
-
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Opioid Receptor
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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 .
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- HY-103294
-
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Peptides
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Others
|
R892 is a selective and efficient bradyKinin B1 receptor antagonist with significant antagonistic activity. The pA2 values of R892 in human and rabbit B1 receptors are 8.8 and 8.6 respectively, indicating its strong anti-activity at these receptors. R892 exhibits selectivity with ID50 values of 2.8 nM and >600 nM for B1 and B2 receptors, respectively, and has no endogenous agonist activity. R892 is resistant to aminopeptidase and kininase II (ACE) degradation and exhibits metabolic stability .
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- HY-P0264A
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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 .
|
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- 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 .
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- HY-P1318A
-
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Opioid Receptor
|
Neurological Disease
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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 .
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- HY-P2025
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Peptides
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Neurological Disease
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JMV 236 is a cholecystokinin antagonist with appetite-suppressing activity. JMV 236 affects the regulation of food intake through the interaction of the intestinal endogenous peptide PrRP and the CCK1 receptor. The administration of JMV 236 activates PrRP neurons located in the NTS, thereby enhancing its appetite-suppressing effect. JMV 236 has significant effects on areas of the central nervous system associated with food intake, especially during states of starvation .
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- HY-P1320
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Opioid Receptor
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Inflammation/Immunology
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[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2 binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
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- HY-P1320A
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Opioid Receptor
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Inflammation/Immunology
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[Nphe1]Nociceptin(1-13)NH2, a novel nociceptin/orphanin FQ (NC) endogenous ligand, is a selective and competitive ociceptin receptor antagonist without any residual agonist activity. [Nphe1]nociceptin(1-13)NH2?binds selectively to recombinant nociceptin receptors (pKi=8.4) and antagonizes the inhibitory effects of nociceptin on cyclic AMP accumulation in CHO cells (pA2=6.0). [Nphe1]Nociceptin(1-13)NH2 has the potential to act as an analgesic agent .
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Cat. No. |
Product Name |
Category |
Target |
Chemical Structure |
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- HY-13677
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- HY-107512
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- HY-100806
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- HY-133890A
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- HY-100806R
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- HY-139576B
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- HY-N6776
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Structural Classification
Microorganisms
Terpenoids
Source classification
Diterpenoids
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Potassium Channel
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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 .
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- HY-13677R
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- HY-139576
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- HY-139576A
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- HY-N2908
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- HY-W010820
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- HY-30004
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Structural Classification
Microorganisms
Classification of Application Fields
Ketones, Aldehydes, Acids
Source classification
Metabolic Disease
Endogenous metabolite
Disease Research Fields
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Endogenous Metabolite
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1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
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- HY-30004R
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Structural Classification
Microorganisms
Ketones, Aldehydes, Acids
Source classification
Endogenous metabolite
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Endogenous Metabolite
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1-Aminocyclopropane-1-carboxylic acid (Standard) is the analytical standard of 1-Aminocyclopropane-1-carboxylic acid. This product is intended for research and analytical applications. 1-Aminocyclopropane-1-carboxylic acid is an endogenous metabolite. In the presence of low concentrations (1 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a small molecule agonist of NMDA receptors with an EC50 of 0.7-0.9 μM. At high concentrations (10 μM) of glutamate, 1-Aminocyclopropane-1-carboxylic acid acts as a competitive antagonist of NMDA receptors with an EC50 of 81.6 nM. 1-Aminocyclopropane-1-carboxylic acid exerts neuroprotective activity by moderately activating NMDA receptors to prevent neuronal cell death in ischemic animal models. Additionally, 1-Aminocyclopropane-1-carboxylic acid is an antagonist of NMDA receptors, inducing blood pressure reduction and antioxidant effects in stroke-prone hypertensive rats. 1-Aminocyclopropane-1-carboxylic acid enhances object recognition memory and cognitive flexibility dependent on the prefrontal cortex, but does not affect impulsivity nor exhibit an antipsychotic-like profile. 1-Aminocyclopropane-1-carboxylic acid shows promise for research in the field of neurotoxicity. .
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Cat. No. |
Product Name |
Chemical Structure |
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- HY-13677S1
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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.
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- HY-100806S
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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 .
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- HY-13677S
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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].
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- HY-135103S
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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].
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- HY-W654353
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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 .
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