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KOR/DOR agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Apoptosis (5) Beta-secretase (1) Caspase (2) Endogenous Metabolite (2) Isotope-Labeled Compounds (1) NF-κB (3) NO Synthase (3) Opioid Receptor (15) p38 MAPK (3) Reactive Oxygen Species (ROS) (3) Toll-like Receptor (TLR) (3)
By Research Areas:	Cardiovascular Disease (3) Inflammation/Immunology (4) Neurological Disease (13)

Inhibitors & Agonists

Peptides

Isotope-Labeled Compounds

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-107744

Nalmefene 1 Publications Verification	Opioid Receptor Apoptosis Reactive Oxygen Species (ROS) NO Synthase Toll-like Receptor (TLR) p38 MAPK NF-κB	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and *DOR, and a partial agonist* of *KOR*. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders .

HY-P1333

Dynorphin A 1 Publications Verification	Opioid Receptor Apoptosis Caspase Endogenous Metabolite	Neurological Disease
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .

HY-162552

KOR/DOR agonist 1	Opioid Receptor	Neurological Disease
KOR/DOR agonist 2 is a *KOR* and DOR opioid receptors agonist with K_i values of 0.14 nM, and 0.93 nM, respectively. KOR/DOR agonist 2 shows significant antinociceptive effects. KOR/DOR agonist 2 penetrates the blood-brain barrier .

HY-161539

*KOR agonist* 1**	Opioid Receptor	Neurological Disease
KOR agonist 1 (Compound 7a) is a selective agonist for opioid receptor, with EC₅₀s of 3.4, 701.2 and 1649 nM, for *KOR, MOR* and *DOR, respectively. KOR* agonist 1 binds KOR, MOR and DOR, with K_is of 3.9, 1053 and 4196 nM, respectively. KOR agonist 1 exhibits antinociceptive effect in ICR mouse model (ED₅₀ in hot plate test is 0.3 mg/kg, in abdominal constriction test is 0.2 mg/kg) .

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-175486

*KOR agonist* 6**	Opioid Receptor	Neurological Disease
KOR agonist 6 is a *KOR* agonist (K_i = 0.25 pM). KOR agonist 6 shows agonistic activity at MOR and *DOR* in CHO cells and inhibits Forskolin (HY-15371)-stimulated cAMP accumulation. KOR agonist 6 stimulates *KOR*-mediated [ ³⁵S]GTPγS binding and inhibits cAMP accumulation in *KOR*-expressing HEK293 cells with potent agonistic activity, while showing lower β-arrestin recruitment potency. KOR agonist 6 demonstrates anti-nociceptive efficacy in mice. KOR agonist 6 can be used for the study of analgesics with reduced central nervous system (CNS) side effects .

HY-B1485

Nalmefene hydrochloride	Opioid Receptor	Neurological Disease
Nalmefene hydrochloride is a long acting opioid (MOR and *DOR* antagonist), and a partial *KOR* agonist. Nalmefene hydrochloride is used for opioid overdose and alcohol dependence .

HY-P10203

*μ/κ/δ opioid receptor agonist* 1**	Opioid Receptor	Inflammation/Immunology
μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .

HY-107744R

Nalmefene (Standard)	Opioid Receptor Apoptosis Reactive Oxygen Species (ROS) NO Synthase Toll-like Receptor (TLR) p38 MAPK NF-κB	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Nalmefene (Standard) is the analytical standard of Nalmefene. This product is intended for research and analytical applications. Nalmefene is a long acting opioid (MOR and DOR antagonist), and a partial KOR agonist. Nalmefene is used for opioid overdose and alcohol dependence .

HY-173030

*Opioid receptor agonist* 1**	Opioid Receptor	Neurological Disease
Opioid receptor agonist 1 (Compound 2638-28) is the orally active agonist for opioid receptor that exhibits good affinity to MOR, *DOR* and *KOR* with K_i of 5, 24 and 212 nM, respectively. Opioid receptor agonist 1 exhibits analgesic activity in mouse warm water tail flick models and acetic acid writhing models .

HY-P1333A

Dynorphin A TFA	Opioid Receptor Apoptosis Caspase Endogenous Metabolite	Neurological Disease
Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .

HY-175661

SRI-22136	Opioid Receptor Beta-secretase	Neurological Disease
SRI-22136 is a Delta Opioid Receptor (DOR) antagonist that can cross blood-brain barrier with a IC₅₀ of 0.42 nM. SRI-22136 does not have agonistic activity but antagonistic activity against DOR, MOR (IC₅₀ = 370 nM), *KOR* (IC₅₀ = 54 nM) and can avoid addiction/aversion effects. SRI-22136 can effectively inhibit the BACE1 activity induced by DADLE (a DOR agonist) (HY-105343) (IC₅₀ = 120 nM). SRI-22136 prevents completely Alzheimer’s-like pathology in mouse model. SRI-22136 can used for the study of Alzheimer’s disease .

HY-W754114

Nalmefene Sulfate-d3	Isotope-Labeled Compounds Opioid Receptor Apoptosis Reactive Oxygen Species (ROS) NO Synthase Toll-like Receptor (TLR) p38 MAPK NF-κB	Cardiovascular Disease Neurological Disease Inflammation/Immunology
Nalmefene Sulfate-d₃ is the deuterium labeled Nalmefene (HY-107744). Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders .

HY-P1625

Daeatal Dynorphin A ethylamide (1-9)	Opioid Receptor	Neurological Disease
Daeatal (Dynorphin A ethylamide (1-9)) is an ethylamine-modified dynorphin fragment that can be used in the study of analgesia, addiction, depression, etc. Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .

HY-135698

Methocinnamox M-CAM	Opioid Receptor	Neurological Disease
Methocinnamox (M-CAM) a selective and long-acting μ-opioid receptor (MOR) antagonist with a K_i of 0.6 nM. Methocinnamox binds to the orthosteric site of the MOR in a pseudo-irreversible, non-covalent manner, resulting in prolonged receptor blockade that persists until new receptors are synthesized. Methocinnamox acts as a reversible antagonist at both the kappa-opioid receptor (KOR) (K_i = 4.9 nM) and delta-opioid receptor (DOR) (K_i = 2.2 nM), and it exhibits no intrinsic agonist activity at these receptors. Methocinnamox can be used to reverse and prevent opioid overdose and addiction .

Cat. No.	Product Name	Target	Research Area

HY-P1333

Dynorphin A 1 Publications Verification	Opioid Receptor Apoptosis Caspase Endogenous Metabolite	Neurological Disease
Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .

HY-P10203

*μ/κ/δ opioid receptor agonist* 1**	Opioid Receptor	Inflammation/Immunology
μ/κ/δ opioid receptor agonist 1 is a μ opioid receptor (MOR), κ opioid receptor (KOR), and δ opioid receptor (DOR) agonist. μ/κ/δ opioid receptor agonist 1 produces a strong and long-lasting analgesic effect through peripheral MOR and KOR in the tail-flick test .

HY-P1333A

Dynorphin A TFA	Opioid Receptor Apoptosis Caspase Endogenous Metabolite	Neurological Disease
Dynorphin A TFA is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A TFA is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A TFA can induce neuronal death, and can be used in the research of neurological disease .

HY-P1625

Daeatal Dynorphin A ethylamide (1-9)	Opioid Receptor	Neurological Disease
Daeatal (Dynorphin A ethylamide (1-9)) is an ethylamine-modified dynorphin fragment that can be used in the study of analgesia, addiction, depression, etc. Dynorphin A is an endogenous opioid peptide involved in inhibitory neurotransmission in the central nervous system (CNS). Dynorphin A is a highy potent kappa opioid receptor (KOR) agonist, and is also an agonist for other opioid receptors, such as mu (MOR) and delta (DOR). Dynorphin A can induce neuronal death, and can be used in the research of neurological disease .

Cat. No.	Product Name	Chemical Structure

HY-W754114

Nalmefene Sulfate-d3
Nalmefene Sulfate-d₃ is the deuterium labeled Nalmefene (HY-107744). Nalmefene is a BBB-penetrable opioid receptor modulator. Nalmefene is an antagonist of MOR and DOR, and a partial agonist of KOR. Nalmefene has anti-inflammatory and neuroprotective activities. Nalmefene can be used in the research of reducing alcohol-dependent disorders .

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