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κ-opioid Receptor Agonist

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Opioid Receptor (46) Adenylate Cyclase (2) Apoptosis (4) Autophagy (2) Caspase (2) Endogenous Metabolite (2) Ferroptosis (2) Isotope-Labeled Compounds (2) Mitophagy (2) PINK1/Parkin (2)
By Research Areas:	Cancer (3) Cardiovascular Disease (1) Endocrinology (1) Infection (1) Inflammation/Immunology (6) Metabolic Disease (1) Neurological Disease (39)

Inhibitors & Agonists

Peptides

Natural
Products

Isotope-Labeled Compounds

Targets Recommended: Opioid Receptor

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-101205

ICI 199441	Opioid Receptor	Cardiovascular Disease
ICI 199441 is a potent and selective *κ-opioid* receptor agonist. ICI 199441 can improve heart resistance to ischemia/reperfusion .

HY-P3609

CR 665 JNJ 38488502; FE 200665	Opioid Receptor	Neurological Disease
CR 665 (JNJ 38488502) is a peripherally selective *κ-opioid* agonist. CR 665 can activate the kappa opioid receptor with EC₅₀ value of 10.9 nM. CR 665 can be used for the research of peripheral pain .

HY-163017

NP-5497-KA	Others	Neurological Disease
NP-5497-KA is a *κ-opioid* receptor agonist. NP-5497-KA has orally activity[1].

HY-19206

R-84760	Opioid Receptor	Neurological Disease
R-84760 is a selective **κ-opioid receptor** agonist. R-84760 has antinociceptive effect .

HY-100963

U-54494A	Opioid Receptor	Neurological Disease
U-54494A is a benzamide derivative related to κ-opioid *receptor* agonists, U-54494A has an anticonvulsant activity .

HY-145128

GR103545	Opioid Receptor	Neurological Disease
GR103545 is a potent and selective agonist of the κ-opioid receptor (κ-OR). ¹¹GR103545 is a radiotracer for imaging κ-OR in vivo ^[1]

HY-123389

MR2034 (R)-UM-1071	Others	Endocrinology
MR2034 ((R)-UM-1071) is a κ-opioid receptor agonist with activity that stimulates the hypothalamic-pituitary-adrenal axis. MR2034 has shown the potential to promote mood and inhibit addictive behaviors in animal models and can be used to study inhibitory approaches related to mood and addictive disorders. MR2034 is selective for κ-opioid receptors and can effectively modulate biological processes related to stress and mood .

HY-P3647

[DPro10] Dynorphin A (1-11), porcine	Opioid Receptor Adenylate Cyclase	Neurological Disease
[DPro10] Dynorphin A (1-11), porcine, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a K_i value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine has analgesic property .

HY-P3647A

[DPro10] Dynorphin A (1-11), porcine hydrochloride	Opioid Receptor Adenylate Cyclase	Neurological Disease
[DPro10] Dynorphin A (1-11), porcine hydrochloride, a N-Alkylated derivative, is a potent κ-opioid receptor agonist with a K_i value of 0.13 nM. [DPro10] Dynorphin A (1-11), porcine hydrochloride has analgesic property .

HY-160761

*K-Opioid* receptor agonist-1**	Opioid Receptor	Inflammation/Immunology
K-Opioid receptor agonist-1 (Compound 5a) is an agonist for κ-Opioid receptor with K_i of 0.25 nM and EC₅₀ of 2 nM. K-Opioid receptor agonist-1 is blood brain barrier (BBB) penetrate (brain/plasma ratios of 0.50 to 0.65). K-Opioid receptor agonist-1 exhibits anti-inflammatory activity in dermatitis models induced by Arachidonic acid (HY-109590) or oxazolidinone .

HY-19231

DPI-3290 Org 41793	Opioid Receptor	Neurological Disease
DPI-3290 (Org 41793) is a potent and specific **opioid receptors** agonist with K_i values of 0.18 nM, 0.46 nM, and 0.62 nM for δ-, μ-, and κ-opioid receptors, respectively。DPI-3290 is one of a series of novel centrally acting agents with potent antinociceptive activity .

HY-101079

BRL 52537 hydrochloride	Opioid Receptor	Neurological Disease
BRL 52537 hydrochloride is a highly selective κ-Opioid receptor (KOR) agonist with K_is of 0.24 nM and 1560 nM for κ and μ subtypes, respectively. BRL 52537 hydrochloride decreases ischemia-evoked NO production as a potential mechanism of neuroprotection. BRL 52537 hydrochloride attenuates early stroke damage .

HY-P3376

Riminkefon	Opioid Receptor	Neurological Disease
Riminkefon is a **kappa opioid receptor** agonist .

HY-123689A

Samidorphan hydrochloride ALKS-33 hydrochloride; RDC-0313 hydrochloride	Opioid Receptor	Neurological Disease
Samidorphan hydrochloride is an orally active *opioid* system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan hydrochloride acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan hydrochloride primarily acts as an opioid receptor antagonist in vivo .

HY-110302

6'-GNTI dihydrochloride	Opioid Receptor	Neurological Disease
6'-GNTI dihydrochloride, a κ-opioid receptor (KOR) agonist, displays bias toward the activation of G protein-mediated signaling over β-arrestin2 recruitment. 6'-GNTI 6'-GNTI dihydrochloride only activates the Akt pathway in striatal neurons .

HY-123689

Samidorphan ALKS-33; RDC-0313	Opioid Receptor	Neurological Disease
Samidorphan (ALKS-33) is an orally active *opioid* system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .

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-121800

ML138	Opioid Receptor	Others
ML138, a **κ opioid receptor** agonist, is a MLPCN probe .

HY-P3445

Anrikefon HSK21542	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) is a kappa opioid receptor agonist with analgesic effect .

HY-P3445A

Anrikefon acetate HSK21542 acetate	Opioid Receptor	Neurological Disease
Anrikefon (HSK21542) acetate is a kappa opioid receptor agonist with analgesic effect .

HY-P0088

Porcine dynorphin A(1-13) Dynorphin A Porcine Fragment 1-13	Opioid Receptor	Others
Porcine dynorphin A (1-13) is a potent, endogenous **κ opioid receptor** agonist and is antinociceptive at physiological concentrations.

HY-123689S

Samidorphan-d4 ALKS-33-d₄; RDC-0313-d₄	Isotope-Labeled Compounds	Neurological Disease
Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active *opioid* system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .

HY-123689S1

Samidorphan-d5 ALKS-33-d₅; RDC-0313-d₅	Isotope-Labeled Compounds	Neurological Disease
Samidorphan-d5 (ALKS-33-d5) is a tritiated version of Samidorphan. Samidorphan is an orally active *opioid* system modulator that binds with high affinity to *μ-opioid, κ-opioid, and δ-opioid* receptors. Samidorphan is a *μ-opioid* receptor antagonist and a partial agonist at *k-opioid* and *δ-opioid* receptors. Samidorphan acts primarily as an *opioid* receptor antagonist in vivo .

HY-10487

JDTic dihydrochloride	Opioid Receptor	Neurological Disease
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

HY-15997B

(±)-U-50488 hydrochloride (±)-Trans-(1R,2R)-U-50488 hydrochloride	Opioid Receptor	Neurological Disease
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrochloride is a selective κ opioid receptor (KOR) agonist .

HY-15997C

(±)-U-50488 hydrate hydrochloride (±)-Trans-(1R,2R)-U-50488 hydrate hydrochloride	Opioid Receptor	Neurological Disease
(±)-U-50488 ((±)-Trans-(1R,2R)-U-50488) hydrate hydrochloride is a selective κ opioid receptor (KOR) agonist .

HY-156131

Loperamide ADL 2-1294	Opioid Receptor	Inflammation/Immunology
Loperamide (ADL 2-1294) is a selective μ opioid receptor agonist with K_is of 3, 48 and 1156 nM against μ, δ and κ opioid receptor, respectively. Loperamide can be used as an antidiarrheal agent .

HY-105235

Enadoline CI-977	Opioid Receptor	Neurological Disease
Enadoline (CI-977) is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects .

HY-105235A

Enadoline hydrochloride CI-977 hydrochloride	Opioid Receptor	Neurological Disease
Enadoline (CI-977) hydrochloride is a highly selective, brain-penetrating, and nonpeptide kappa-opioid receptor (KOR) agonist (K_i=1.25 nM). Antinociceptive effects .

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-163917

SalA-VS-08	Opioid Receptor	Neurological Disease
SalA-VS-08 is a full agonist of kappa-opioid receptor (KOR) with selectivity and G-protein bias. SalA-VS-08 can be used in the research of analgesia .

HY-163916

SalA-VS-07	Opioid Receptor	Neurological Disease
SalA-VS-07 is a G protein-biased partial agonist for the Kappa-opioid receptor (KOR). SalA-VS-07 can be used for research of pain and other disorders .

HY-120949

(1R,2R)-U-50488 hydrochloride	Opioid Receptor	Neurological Disease
(1R,2R)-U-50488 hydrochloride is the absolute stereochemistry of (±)-U-50488 hydrochloride. (±)-U-50488 hydrochloride is a selective κ opioid receptor (KOR) agonist .

HY-161812

MOR agonist-4	Opioid Receptor	Others
MOR agonist-4 (2d) is a G protein signaling-biased Kappa opioid receptor (KOR) agonist with an EC₅₀ value of 11 nM. MOR agonist-4 contains an electron withdrawing CF3 group and a bias factor of 38 based on triazole. MOR agonist-4 is used in the research of pruritis and analgesia .

HY-P1333

Dynorphin A	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-159088

KOR agonist 2	Opioid Receptor	Neurological Disease
KOR agonist 2 (Compound 23p) is an agonist for κ opioid receptor (KOR) with K_i of 1.9 nM. KOR agonist 2 exhibits analgesic effect in mouse models with ED₅₀ of 1.30 mg/kg. KOR agonist 2 exhibits high clearance rate (2 mg/kg, i.v.) in mice, high metabolism and clearance in liver microsomes .

HY-17609

Difelikefalin CR-845; FE-202845	Opioid Receptor	Neurological Disease
Difelikefalin (CR-845; FE-202845) is a peripherally restricted and selective agonist of kappa opioid receptor (KOR). Difelikefalin produces anti-inflammatory effects and has the potential in modulating pruritus in conditions such as chronic kidney disease .

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-141468

β-Chlornaltrexamine dihydrochloride β-CNA dihydrochloride	Opioid Receptor	Neurological Disease
β-Chlornaltrexamine dihydrochloride (β-CNA dihydrochloride) is a potent long-term **opioid receptor** blocker. β-Chlornaltrexamine dihydrochloride can effectively block the inhibitory effect of κ opioid receptor agonists on dopamine release. β-Chlornaltrexamine dihydrochloride can be used to study the mechanism of pain perception .

HY-106756

Spiradoline U-62066	Opioid Receptor	Neurological Disease
Spiradoline (U-62066), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a K_i of 8.6 nM in guinea pig. The K_i values of Spiradoline for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .

HY-124959

Spiradoline mesylate U-62066 mesylate	Opioid Receptor	Neurological Disease
Spiradoline mesylate (U-62066 mesylate), an arylacetamide, is a selective kappa opioid receptor (KOR) agonist with a K_i of 8.6 nM in guinea pig. The K_i values of Spiradoline mesylate for μ and δ receptors are 252 nM and 9400 nM, respectively. Spiradoline mesylate has potent diuretic, analgesic, antiarrythmic, antitussive, neuroprotective properties and easily penetrates the blood-brain barrier .

HY-P3634

[DAla2] Dynorphin A (1-13), amide (porcine)	Opioid Receptor	Neurological Disease
[DAla2] Dynorphin A (1-13), amide (porcine) is a petide. [DAla2] Dynorphin A (1-13), amide (porcine) might have the κ opioid receptor agonist effect. [DAla2] Dynorphin A (1-13), amide (porcine) can be used for the research of nervous system .

HY-126910

Mesyl Salvinorin B	Opioid Receptor	Metabolic Disease
Mesyl Salvinorin B is a potent and selective kappa opioid receptor (KOP-r) agonist. Mesyl Salvinorin B prevents the ADE (Alcohol deprivation effect) in mice. Mesyl Salvinorin B dose-dependently reduces alcohol intake and preference in CED (chronic escalation drinking) mice .

HY-P4679

(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) E2078	Opioid Receptor	Neurological Disease
(N-Me-Tyr1,N-Me-Arg7,D-Leu-NHEt8)-Dynorphin A (1-8) (E-2078), a stable Dynorphin A (1–8) (HY-P2159) analog, is a kappa opioid receptor (KOR) agonist .

HY-163277

PIPE-3297	Opioid Receptor	Inflammation/Immunology
PIPE-3297 (compound 25) is a selective kappa opioid receptor (KOR) agonist, which activates the G-protein signaling with EC₅₀ of 1.1 nM and exhibits low β-arrestin-2 recruitment activity (10%). PIPE-3297 induces myelination and reveals an anti-inflammatory activity .

HY-130696

(+)-U-50488 (+)-Trans-(1R,2R)-U-50488	Opioid Receptor	Neurological Disease
(+)-U-50488 ((+)-Trans-(1R,2R)-U-50488) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .

HY-15997A

(+)-U-50488 hydrochloride (+)-Trans-(1R,2R)-U-50488 hydrochloride	Opioid Receptor	Neurological Disease
(+)-U-50488 (hydrochloride) (+)-Trans-(1R,2R)-U-50488 hydrochloride) is a less active κ opioid receptor (KOR) agonist than the enantiomer of (-)-Trans-(1S,2S)-U-50488 (HY-15997) .

HY-N0164

Matrine 10+ 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-N0164R

Matrine (Standard)	PINK1/Parkin 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-120045A

DuP 747 hydrochloride	Others	Neurological Disease
DuP 747 hydrochloride is an analgesic with selective kappa-opioid receptor agonist activity. DuP 747 showed less spiradoline-appropriate selection when administered SC, but showed a partial generalized response to spiradoline when administered IP or PO. The 5-hydroxy-desmethoxy metabolite of DuP 747 induced selection of the saline-appropriate lever only. The effects of DuP 747 suggest that its metabolites may play a major role in the similar responses to spiradoline after IP and PO administration .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N0164

Matrine 10+ Cited Publications Matridin-15-one; Vegard; α-Matrine	Structural Classification Classification of Application Fields Source classification Sophora flavescens Aiton Plants Biological Pesticide Research Agricultural Research Alkaloids Piperidine Alkaloids Leguminosae Inflammation/Immunology Disease Research Fields Cancer	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-N0164R

Matrine (Standard)	Alkaloids Piperidine Alkaloids Structural Classification Leguminosae Source classification Sophora flavescens Aiton Plants	PINK1/Parkin 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-123689S

Samidorphan-d4

Samidorphan-d4 is the deuterium labeled Samidorphan(HY-123689).Samidorphan (ALKS-33) is an orally active opioid system modulator that has a high affinity for binding with μ‐opioid, κ‐opioid, and δ‐opioid receptors. Samidorphan acts as an antagonist at μ‐opioid receptors and acts as a partial agonist at k-opioid and δ‐opioid receptors. Samidorphan primarily acts as an opioid receptor antagonist in vivo .

HY-123689S1

Samidorphan-d5

Samidorphan-d5 (ALKS-33-d5) is a tritiated version of Samidorphan. Samidorphan is an orally active opioid system modulator that binds with high affinity to μ-opioid, κ-opioid, and δ-opioid receptors. Samidorphan is a μ-opioid receptor antagonist and a partial agonist at k-opioid and δ-opioid receptors. Samidorphan acts primarily as an opioid receptor antagonist in vivo .

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