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κ-opioid receptor affinity

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By Targets:	Interleukin Related (1) Isotope-Labeled Compounds (2) Opioid Receptor (14) Reference Standards (1) Sigma Receptor (1) Sodium Channel (1) TNF Receptor (1)
By Research Areas:	Cardiovascular Disease (1) Inflammation/Immunology (1) Metabolic Disease (3) Neurological Disease (12)

Inhibitors & Agonists

Isotope-Labeled Compounds

Targets Recommended: MARK

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

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-145404

Mitragynine pseudoindoxyl 1 Publications Verification	Opioid Receptor	Metabolic Disease
Mitragynine pseudoindoxyl is a potent orally active agonist of the μ-opioid receptor (MOR-1, K_i=0.8 nM) and an antagonist of the δ-opioid receptor (DOR-1, K_i=3.0 nM). Mitragynine pseudoindoxyl has moderate affinity for the κ-opioid receptor (KOR-1, K_i=24 nM) and does not recruit β-arrestin-2, acting through G protein-mediated signaling pathways without β-arrestin-2-related activation. Mitragynine pseudoindoxyl produces potent analgesic activity through a mixed μ-agonist/δ-antagonist mechanism, with low side effects such as physical dependence, respiratory depression, and constipation, and no rewarding or aversive behaviors. Mitragynine pseudoindoxyl reduces hyperactivity, inhibits GI transit, and enhances characteristics, making it a potential analgesic .

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. Samidorphan can improve the behavior of depressed animals .

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-135230

LY2444296 FP3FBZ	Opioid Receptor	Neurological Disease
LY2444296 is an orally bioavailable, high-affinity and selective short-acting kappa opioid receptor (KOPR) antagonist, with a K_i value of ～1 nM. LY2444296 exhibits anti-anxiety like effects .

HY-101223

DIPPA hydrochloride	Opioid Receptor	Neurological Disease
DIPPA hydrochloride is an irreversible, long-lasting, selective and high affinity **κ-opioid receptor** antagonist. DIPPA hydrochloride can be used for the research of anxiety and antidepressant .

HY-178945

KOR agonist 7	Opioid Receptor Interleukin Related TNF Receptor Sigma Receptor	Neurological Disease Inflammation/Immunology
KOR agonist 7 (Compound 29) is a highly selective **κ-opioid receptor (KOR) agonist with a K_i** of 138 nM. KOR agonist 7 shows no activity at μ- and δ-opioid receptors or σ1 receptor, and exhibits extremely low affinity for σ2 receptor (K_i = 2.8 μM). KOR agonist 7 significantly reduces the secretion of pro-inflammatory cytokines such as IL-6, TNF-α, and IFN-γ, while increasing the production of the anti-inflammatory cytokine IL-10. KOR agonist 7 downregulates the expression of the pro-inflammatory M1 macrophage marker CD80 and upregulates the anti-inflammatory M2 macrophage marker CD163. KOR agonist 7 holds potential for applications in analgesia and immune modulation .

HY-123689S1

Samidorphan-d5 ALKS-33-d₅; RDC-0313-d₅	Isotope-Labeled Compounds Opioid Receptor	Neurological Disease
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound 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-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. Samidorphan can improve the behavior of depressed animals .

HY-123689S

Samidorphan-d4 ALKS-33-d₄; RDC-0313-d₄	Isotope-Labeled Compounds Opioid Receptor	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-123689R

Samidorphan (Standard) ALKS-33 (Standard); RDC-0313 (Standard)	Opioid Receptor Reference Standards	Neurological Disease
Samidorphan (Standard) is the analytical standard of Samidorphan. This product is intended for research and analytical applications. 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. Samidorphan can improve the behavior of depressed animals.

HY-119733

BU09059	Opioid Receptor	Neurological Disease
BU09059 is a potent and selective **Kappa-opioid receptor** antagonist with a pA₂ of 8.62. BU09059 has nanomolar affinity for the κ-receptor, with 15-fold and 616-fold selectivity over μ- and δ-receptors, respectively. BU09059 significantly blocks U50488 (HY-15997B)-induced antinociception .

HY-106131

RSD-921 PD-123497	Sodium Channel Opioid Receptor	Cardiovascular Disease
RSD-921 (PD-123497) is a potent Na ⁺ channel blocker with anti-arrhythmic activity. RSD-921 displays a low affinity for **κ-opioid receptors** and behaves as a weak κ-agonist in vitro. RSD 921 displays state-, time- and voltage-dependent block of the open state of cardiac, skeletal muscle and neuronal Na ⁺ channels expressed in Xenopus oocytes. RSD-921 can be used for cardiac arrhythmias research .

HY-125790

Cyclazocine	Opioid Receptor	Neurological Disease
Cyclazocine is a μ, δ, and κ opioid *receptor* modulator with K_i values of 0.32, 1.1, and 0.18 nM, respectively. Cyclazocine exhibits "mixed" pharmacological activities, acting as a μ-partial antagonist, κ-agonist, and low-affinity δ ligand. Cyclazocine shows antinociceptive activity in mice. Cyclazocine can be used in studies on psychoactive substance addiction .

Cat. No.	Product Name	Chemical Structure

HY-123689S1

Samidorphan-d5
Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound 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 .

Samidorphan-d5

Samidorphan-d5 (ALKS-33-d5) is is a deuterated compound 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-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 .

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 .

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BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature. Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred to a PVDF membrane and blocked with 5% non-fat milk in TBST for 2 hour at room temperature. The primary antibody (1/1000) and Loading control antibody (Beta Actin, HY-P80438, 1/10000) was used in 5% non-fat milk in TBST at 4°C overnight. Goat Anti-Mouse/Rabbit IgG-HRP Secondary Antibody (1/10000) was used for 1 hour at room temperature.

BODIPY 493/503 purchased from MedChemExpress. Usage Cited in: Nat Commun. 2025 Feb 1;16(1):1241. [Abstract]

MedchemExpress Validation 01

MedchemExpress Validation 03

Western blot analysis of extracts from THP-1(lane 2(20μg), Jurkat (lane 3(20μg) and NIH3T3(lane 4(20μg) using FOXO1A (HY-P80132) Rabbit mAb. Proteins were transferred

MedchemExpress Validation 04

MedchemExpress Validation

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