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human κ-opioid receptor

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By Targets:	Aminopeptidase (1) Androgen Receptor (1) Apoptosis (3) Autophagy (3) CXCR (1) Cytochrome P450 (1) Endogenous Metabolite (1) Enteropeptidase (1) ERK (1) Ferroptosis (3) Isotope-Labeled Compounds (1) Mitophagy (3) mTOR (1) Opioid Receptor (15) PINK1/Parkin (3) Reference Standards (1) Sodium Channel (1) Urotensin Receptor (1)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Inflammation/Immunology (4) Metabolic Disease (2) Neurological Disease (10)

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Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-N0164

Matrine 15+ Cited Publications Matridin-15-one; Vegard; α-Matrine	PINK1/Parkin Opioid Receptor Autophagy Mitophagy Ferroptosis Apoptosis	Inflammation/Immunology Cancer
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a **kappa opioid receptor and u-receptor** agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

HY-19627A

Naldemedine tosylate 1 Publications Verification S-297995 tosylate	Opioid Receptor	Neurological Disease Metabolic Disease
Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine tosylate shows potent binding affinities (K_i=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC₅₀=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine tosylate is predicted to bind to 3CL ^pro encoded by SARS-CoV2 genome .

HY-P2159

Dynorphin A (1-8)	Opioid Receptor Endogenous Metabolite	Neurological Disease
Dynorphin A (1-8) is a ligand with preference for the **κ-opioid receptor, and its IC₅₀** value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .

HY-107748

5'-Guanidinonaltrindole hydrochloride 5'-GNTI hydrochloride	Opioid Receptor	Neurological Disease
5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent **κ-opioid receptor antagonist with a K_i** of 0.18 nM for human κ-opioid receptor .

HY-19627

Naldemedine S-297995	Opioid Receptor	Neurological Disease Metabolic Disease
Naldemedine (S-297995) is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine shows potent binding affinities (Ki=0.34, 0.43, 0.94 nM, respectively) and antagonist activities (IC₅₀=25.57, 7.09, 16.1 nM, respectively) for recombinant human μ-, δ-, and κ- opioid receptors . Naldemedine can be used in opioid-induced constipation (OIC) research . Naldemedine is predicted to bind to 3CL ^pro encoded by SARS-CoV2 genome .

HY-W019787

BAM-12P	Opioid Receptor CXCR	Neurological Disease
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC₅₀ of 101 nM and a pEC₅₀ of 6.99. BAM-12P is a ligand for CXCR7 with an EC₅₀ of 175 nM .

HY-170973

KOR agonist 4	Opioid Receptor
KOR agonist 4 (compound 39) is an agonist of **Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC₅₀ of 14 nM and with an E_max** of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .

HY-122189

Akuammine (-)-Akuammine; Vincamajoridine	Others	Neurological Disease
Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioid receptors over the δ-opioid receptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioid receptors (IC₅₀s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.

HY-108043

AZD-2327	Opioid Receptor	Neurological Disease
AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (K_i of 0.49 and 0.75 nM and EC₅₀ of 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease .

HY-W654256

Matrine-d3 Matridin-15-one-d₃; Vegard-d₃; α-Matrine-d₃	Isotope-Labeled Compounds PINK1/Parkin Opioid Receptor Autophagy Mitophagy Ferroptosis Apoptosis	Inflammation/Immunology Cancer
Matrine-d₃ (Matridin-d₃) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

HY-P11642A

Sialorphin TFA	Enteropeptidase Aminopeptidase Opioid Receptor ERK mTOR Androgen Receptor	Inflammation/Immunology
Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .

HY-P10006

Leumorphin, human	Opioid Receptor	Neurological Disease
Leumorphin, human is a potent **kappa opioid receptor (κ opioid receptor)** agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .

HY-P5892

β-Endorphin (1-27) (human)	Opioid Receptor	Neurological Disease
β-Endorphin (1-27) (human) is an *opioid* antagonist that binds μ-, δ-, and κ-opioid receptors with K_is of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .

HY-10672

Urotensin-II receptor antagonist-1	Urotensin Receptor Cytochrome P450 Sodium Channel Opioid Receptor	Cardiovascular Disease
Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, K_i=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC₅₀=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC₅₀=3.2 μM), targets cardiac sodium channels (K_i=2.5 μM) .

HY-N0164R

Matrine (Standard) Matridin-15-one (Standard); Vegard (Standard); α-Matrine (Standard)	PINK1/Parkin Reference Standards Opioid Receptor Autophagy Mitophagy Ferroptosis Apoptosis	Inflammation/Immunology Cancer
Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

HY-181515

KOR agonist 8	Opioid Receptor	Neurological Disease
KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a K_i value of 5.3 nM for human KOR, and EC₅₀ values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research .

Cat. No.	Product Name	Target	Research Area

HY-P2159

Dynorphin A (1-8)	Opioid Receptor Endogenous Metabolite	Neurological Disease
Dynorphin A (1-8) is a ligand with preference for the **κ-opioid receptor, and its IC₅₀** value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .

HY-W019787

BAM-12P	Opioid Receptor CXCR	Neurological Disease
BAM-12P, an endogenous opioid peptide, is a novel pro-Met-enkephalin. BAM-12P can activate human κ-opioid receptor (hKOR) with an EC₅₀ of 101 nM and a pEC₅₀ of 6.99. BAM-12P is a ligand for CXCR7 with an EC₅₀ of 175 nM .

HY-P11642A

Sialorphin TFA	Enteropeptidase Aminopeptidase Opioid Receptor ERK mTOR Androgen Receptor	Inflammation/Immunology
Sialorphin TFA is a neutral endopeptidase (NEP) and aminopeptidase N (APN) inhibitor that responds to androgen signals. Sialorphin TFA blocks the degradation of endogenous opioid peptides and interacts with μ-, δ-, κ-opioid receptors. Sialorphin TFA regulates the ERK/mTOR signaling pathway by inducing cell cycle arrest, enhancing ERK1/2 activity, and reducing the phosphorylation levels of mTOR, 4E-BP1, p70S6K; accordingly, Sialorphin TFA exhibits antiproliferative activity against colorectal cancer, glioma and prostate cancer cells without cytotoxicity. In addition, Sialorphin TFA also produces antinociceptive responses, regulates sexual behavior, relaxes corpus cavernosum smooth muscle, and alleviates experimental colitis. Sialorphin TFA is also a copper (II) ion-binding ligand. Sialorphin TFA has been used in mechanistic studies related to cancer, pain management and inflammatory bowel disease .

HY-P10006

Leumorphin, human	Opioid Receptor	Neurological Disease
Leumorphin, human is a potent **kappa opioid receptor (κ opioid receptor)** agonist. Leumorphin, human inhibits the contraction of the myenteric plexus-longitudinal muscle preparation of the guinea pig ileum .

HY-P5892

β-Endorphin (1-27) (human)	Opioid Receptor	Neurological Disease
β-Endorphin (1-27) (human) is an *opioid* antagonist that binds μ-, δ-, and κ-opioid receptors with K_is of 5.31, 6.17, and 39.82 nM, respectively. β-Endorphin (1-27) (human) inhibits β-Endorphin (HY-P1502)-induced and etorphine-induced analgesia .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0164

Matrine 15+ Cited Publications Matridin-15-one; Vegard; α-Matrine	Alkaloids Piperidine Alkaloids Classification of Application Fields Leguminosae Sophora flavescens Aiton Plants Inflammation/Immunology Disease Research Fields Biological Pesticide Research Source Classification Cancer Agricultural Research	PINK1/Parkin Opioid Receptor Autophagy Mitophagy Ferroptosis Apoptosis
Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a **kappa opioid receptor and u-receptor** agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

HY-P2159

Dynorphin A (1-8)	Structural Classification Natural Products Neurological Disease Classification of Application Fields Endogenous metabolite Disease Research Fields Source Classification	Opioid Receptor Endogenous Metabolite
Dynorphin A (1-8) is a ligand with preference for the **κ-opioid receptor, and its IC₅₀** value against human placental κ-opioid receptor is 330 nM. Dynorphin A (1-8) mediates neuroprotective effects by inhibiting oxidative stress, suppressing apoptosis, and competitively displacing the binding of κ partial agonists. Dynorphin A (1-8) is the dominant opioid peptide in human placental villi and tissue extracts; it undergoes rapid hydrolysis and can enter the central nervous system via intranasal administration. Dynorphin A (1-8) can be used in studies related to ischemic stroke .

HY-N0164R

Matrine (Standard) Matridin-15-one (Standard); Vegard (Standard); α-Matrine (Standard)	Alkaloids Piperidine Alkaloids Structural Classification Leguminosae Sophora flavescens Aiton Plants Source Classification	PINK1/Parkin Reference Standards Opioid Receptor Autophagy Mitophagy Ferroptosis Apoptosis
Matrine (Standard) is the analytical standard of Matrine. This product is intended for research and analytical applications. Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

Cat. No.	Product Name	Chemical Structure

HY-W654256

Matrine-d3
Matrine-d₃ (Matridin-d₃) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

Matrine-d3

Matrine-d₃ (Matridin-d₃) is a deuterium labeled Matrine (HY-N0164). Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus that can act as a kappa opioid receptor and u-receptor agonist. Matrine has a variety of pharmacological effects, including anti-cancer, anti-oxidative stress, anti-inflammation and anti-apoptosis effects. Matrine is potential in the research of disease like human non-small cell lung cancer, hepatoma, papillary thyroid cancer and acute kidney injury (AKI) .

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human κ-opioid receptor

Inhibitors & Agonists

Peptides

NaturalProducts

Isotope-Labeled Compounds

Natural
Products