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Results for "

endogenous antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Endogenous Metabolite (14) Androgen Receptor (1) Apoptosis (4) Autophagy (4) CaSR (2) CXCR (4) DNA/RNA Synthesis (1) Estrogen Receptor/ERR (2) FXR (3) GHSR (1) GnRH Receptor (4) GPR35 (4) iGluR (5) Isotope-Labeled Compounds (2) LXR (1) nAChR (2) NF-κB (1) NO Synthase (1) Nucleoside Antimetabolite/Analog (5) Opioid Receptor (5) P2Y Receptor (1) p38 MAPK (1) Potassium Channel (1) sFRP-1 (2) Sodium Channel (1) Trace Amine-associated Receptor (TAAR) (1) Vasopressin Receptor (1)
By Research Areas:	Cancer (14) Cardiovascular Disease (2) Endocrinology (10) Inflammation/Immunology (9) Metabolic Disease (10) Neurological Disease (12)

By Targets:

Endogenous Metabolite (14)

Androgen Receptor (1)

Apoptosis (4)

Autophagy (4)

CaSR (2)

CXCR (4)

DNA/RNA Synthesis (1)

Estrogen Receptor/ERR (2)

FXR (3)

GHSR (1)

GnRH Receptor (4)

GPR35 (4)

iGluR (5)

Isotope-Labeled Compounds (2)

LXR (1)

nAChR (2)

NF-κB (1)

NO Synthase (1)

Nucleoside Antimetabolite/Analog (5)

Opioid Receptor (5)

P2Y Receptor (1)

p38 MAPK (1)

Potassium Channel (1)

sFRP-1 (2)

Sodium Channel (1)

Trace Amine-associated Receptor (TAAR) (1)

Vasopressin Receptor (1)

By Research Areas:

Cancer (14)

Cardiovascular Disease (2)

Endocrinology (10)

Inflammation/Immunology (9)

Metabolic Disease (10)

Neurological Disease (12)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Endogenous Metabolite

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-10858A

WAY 316606 hydrochloride	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 .

HY-120767

Linzagolix choline 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 .

HY-120189

LY 233536	iGluR	Neurological Disease
LY 233536 is a competitive NMDA receptor antagonist .

HY-144204

Estrogen receptor antagonist 5	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) .

HY-144206

Estrogen receptor antagonist 6	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) .

HY-13677

6-Mercaptopurine Maximum Cited Publications 6 Publications Verification 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.

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 .

HY-13677A

6-Mercaptopurine hydrate Maximum Cited Publications 6 Publications Verification 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.

HY-P1628

Ganirelix	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 .

HY-P3066

SKF 100398 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 .

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.

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.

HY-P0009

Cetrorelix 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 .

HY-133890A

Tauro-α-muricholic acid sodium 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 .

HY-14752

Ronacaleret 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 .

HY-15104

Ronacaleret hydrochloride 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 .

HY-10858

WAY 316606 3 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 .

HY-109532

Ganirelix acetate 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) .

HY-13677S

6-Mercaptopurine-d2 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].

HY-P1271

Catestatin	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 .

HY-13677R

6-Mercaptopurine (Standard)	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.

HY-135103S

Tauro-β-muricholic acid-d4 sodium	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].

HY-139576

Larsucosterol 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 .

HY-139576A

Larsucosterol sodium 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 .

HY-117541

Glycyl-glutamine 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) .

HY-P1271A

Catestatin TFA	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 .

HY-13677S1

6-Mercaptopurine-13C2,15N 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.

HY-100806S

Kynurenic acid-d5 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[1][2].**

HY-100806R

Kynurenic acid (Standard) 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.

HY-139576B

Larsucosterol (trimethylamine) 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 .

HY-N6776

Penitrem A	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 .

HY-110098

Ro 5212773 EPPTB	Trace Amine-associated Receptor (TAAR)	Neurological Disease
Ro 5212773 (EPPTB) is a potent and selective trace amine-associated receptor 1 (TAAR1) antagonist (K_i=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 .

HY-P3839

Nocistatin	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 G_i/o proteinmediated pathway. Nocistatin blocks Nociceptin (Nociceptin)-induced allodynia and hyperalgesia .

HY-N2908

Atraric acid 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 .

HY-W010820

Uridine 5'-diphosphate sodium salt	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 .

HY-108425

AMG8379	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 .

HY-P1318

Ac-RYYRIK-NH2	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=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 .

HY-P1318A

Ac-RYYRIK-NH2 TFA	Opioid Receptor	Neurological Disease
Ac-RYYRIK-NH2 TFA is a potent and partial agonist on ORL1 transfected in CHO cells (K_d=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 .

HY-129207

JMV 3002	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.

HY-30004

1-Aminocyclopropane-1-carboxylic acid	Endogenous Metabolite	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. .

HY-P1320

[Nphe1]Nociceptin(1-13)NH2	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 (pK_i=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 .

HY-P1320A

[Nphe1]Nociceptin(1-13)NH2 TFA	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 (pK_i=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 .

Cat. No.	Product Name	Target	Research Area