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Results for "

endogenous antagonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Endogenous Metabolite (12) Androgen Receptor (1) Apoptosis (4) Autophagy (3) CaSR (2) CXCR (4) DNA/RNA Synthesis (1) Estrogen Receptor/ERR (2) FXR (3) GnRH Receptor (3) GPR35 (4) iGluR (5) Isotope-Labeled Compounds (2) LXR (1) nAChR (2) NF-κB (1) NO Synthase (1) Nucleoside Antimetabolite/Analog (4) 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 (12) Cardiovascular Disease (2) Endocrinology (9) Inflammation/Immunology (8) Metabolic Disease (9) Neurological Disease (12)

By Targets:

Endogenous Metabolite (12)

Androgen Receptor (1)

Apoptosis (4)

Autophagy (3)

CaSR (2)

CXCR (4)

DNA/RNA Synthesis (1)

Estrogen Receptor/ERR (2)

FXR (3)

GnRH Receptor (3)

GPR35 (4)

iGluR (5)

Isotope-Labeled Compounds (2)

LXR (1)

nAChR (2)

NF-κB (1)

NO Synthase (1)

Nucleoside Antimetabolite/Analog (4)

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 (12)

Cardiovascular Disease (2)

Endocrinology (9)

Inflammation/Immunology (8)

Metabolic Disease (9)

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-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-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-120189

LY 233536

iGluR Neurological Disease

LY 233536 is a competitive NMDA receptor antagonist .

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-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-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-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