Opioid Receptor Inhibitor

Opioid Receptor Inhibitors (23):

Cat. No.	Product Name	Effect	Purity

HY-15997

(-)-U-50488 hydrochloride	Inhibitor	99.71%
(-)-U-50488 hydrochloride ((-)-Trans-(1S,2S)-U-50488 hydrochloride) is a selective kappa-opioid receptor (KOR) agonist (b>K_d=2.2 nM) over μ-opioid receptor (MOR) (b>K_d=430 nM). (-)-U-50488 hydrochloride is a more active enantiomer than (+)?trans-(1R,2R) U-50488 (HY-15997A)?or the (±)?trans-racemic mixture U-50488 (HY-15997B). (-)-U-50488 hydrochloride has a potent and sustained anti-HIV effect in fected blood monocyte-derived macrophages (MDM).

HY-B0557

Bisacodyl	Inhibitor	99.59%
Bisacodyl is a stimulant laxative agent that works directly on the colon to produce a bowel movement. Bisacodyl increases the secretion of PGE₂ by direct activation of colon macrophages. PGE₂ acts as a paracrine factor and decreases the expression of AQP3 in the colon, which inhibits water transfer from the luminal to the vascular side and leads to a laxative effect.

HY-124754

Navacaprant	Inhibitor	99.97%
Navacaprant (BTRX-335140) is a selective and orally active κ opioid receptor (KOR) antagonist, has antagonist activity for κOR, μOR and δOR with IC₅₀ values of 0.8 nM, 110 nM, and 6500 nM, respectively. Navacaprant endows with favorable in vitro ADMET and in vivo pharmacokinetic profiles and medication-like duration of action in rats. Navacaprant distributes well into the CNS and can be used for the research of neuropathy.

HY-18618A

SB-612111 hydrochloride	Inhibitor	99.26%
SB-612111 hydrochloride hydrochloride is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (K_i=0.33 nM). SB-612111 hydrochloride exhibits selectivity for μ-,?κ- and?δ-receptors with K_i values of?57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.

HY-101392

Harmane	Inhibitor	99.91%
Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀ = 30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

HY-Y0790

Cuminaldehyde	Inhibitor	99.03%
Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC₅₀= 0.00085 mg/mL), α-glucosidase (IC₅₀=0.5 mg/mL) and lipoxygenase (IC₅₀=1370 μM). Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases.

HY-139690

CCG258747	Inhibitor	99.17%
CCG258747 is a selective GRK2 inhibitor (IC₅₀=18 nM) with high selectivity over GRK1, GRK5, PKA, and ROCK1 (518, 83, >5500, and >550–fold, respectively).CCG258747 also blocks the internalization of the µ-opioid receptor. G protein-coupled receptor (GPCR) kinases (GRKs) are attractive targets for the research of heart failure.

HY-N0398

Sec-O-Glucosylhamaudol	Inhibitor	99.81%
Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.

HY-P1596

Gluten Exorphin C	Inhibitor	98.97%
Gluten exorphin C is an opioid peptide derived from wheat gluten. Its IC₅₀ values are 40 μM and 13.5 μM for μ opioid and δ opioid activities in the GPI and MVD assays, respectively.

HY-Y0790R

Cuminaldehyde (Standard)	Inhibitor
Cuminaldehyde (Standard) is the analytical standard of Cuminaldehyde. This product is intended for research and analytical applications. Cuminaldehyde is the main component of Cuminum cyminum and has multiple biological activities, including anti-inflammatory, anti-cancer, anti-diabetic, anti-injury, anti-neuropathy and antibacterial effects. Cuminaldehyde is an inhibitor of aldose reductase (IC₅₀= 0.00085 mg/mL) and α-glucosidase (IC₅₀=0.5 mg/mL). Cuminaldehyde can modulate α-synuclein fibrils. Cuminaldehyde can induce apoptosis in colon adenocarcinoma cells by targeting topoisomerase I and II. In addition, Cuminaldehyde also exerts anti-inflammatory activity by inhibiting lipoxygenase. Cuminaldehyde has a strong inhibitory effect on the growth of Aspergillus flavus and the biosynthesis of aflatoxin B1 (AFB1). Cuminaldehyde can exert anti-injury and anti-neuropathy effects by participating in opioid receptors, L-arginine/NO/cGMP pathways and anti-inflammatory effects. Cuminaldehyde has potential application value in the research of neurodegenerative diseases, cancer, diabetes and neuropathic pain diseases.

HY-100845

Salvinorin A	Inhibitor	≥98.0%
Salvinorin A is a potent, unique and short-acting high efficacy kappa-opioid receptor (KOPr) agonist with K_i value of 4.3 nm. Salvinorin A is a non-nitrogenous neoclerodane isolated from Salvia divinorum.

HY-W777360

Harman-¹³C₂,¹⁵N	Inhibitor
Harman-¹³C₂,¹⁵N is ¹³C and ¹⁵N labeled Harmane. Harmane is a benzodiazepine receptor inhibitor (IC₅₀=7 μM), with IC₅₀ values for mACh, Opioid Receptor, MAO-A/B, and α2-adrenergic receptor of 24 μM, 2.8 μM, 0.5 μM, 5 μM, and 18 μM, respectively. Harmane also inhibits haloperidol and serotonin, with IC₅₀ values of 163 μM and 101 μM, respectively. Harmane inhibits the I1 imidazoline receptor (IC₅₀=30 nM) to reduce blood pressure and has antidepressant, anti-anxiety, anticonvulsant, and analgesic effects. Harmane inhibits dopamine biosynthesis by decreasing tyrosine hydroxylase (TH) activity and enhancing L-DOPA-induced cytotoxicity in PC12 cells. Additionally, Harmane can increase the mutagenic effect induced by 2-acetylaminofluorene (AAF).

HY-18618

SB-612111	Inhibitor
SB-612111 is a novel and potent opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (K_i=0.33 nM). SB-612111 exhibits selectivity for μ-, κ- and δ-receptors with K_i values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. SB-612111 effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.

HY-P1246

Neuropeptide AF (human)	Inhibitor
Neuropeptide AF (human) is an endogenous antiopioid peptide.

HY-18617

rel-SB-612111 hydrochloride	Inhibitor
rel-SB-612111 hydrochloride is a novel and potent human opiate receptor-like orphan receptor (ORL-1) antagonist with a high affinity for hORL-1 (K_i=0.33 nM). rel-SB-612111 hydrochloride exhibits selectivity for μ-, κ- and δ-receptors with K_i values of 57.6 nM, 160.5 nM and 2109 nM, respecticely. rel-SB-612111 hydrochloride effectively antagonizes the pronociceptive action of Nociceptin (HY-P0183) in an acute pain model.

HY-N7437

Akuammidine	Inhibitor
Akuammidine, isolated from the seeds of Picralima nitida, shows a preference for μ-opioid binding sites with K_i values of 0.6, 2.4 and 8.6 μM at μ-, σ- and κ-opioid binding sites, respectively. Akuammidine possesses anti-inflammatory and anti-asthmatic properties.

HY-N0398R

Sec-O-Glucosylhamaudol (Standard)	Inhibitor
Sec-O-Glucosylhamaudol (Standard) is the analytical standard of Sec-O-Glucosylhamaudol. This product is intended for research and analytical applications. Sec-O-Glucosylhamaudol is a natural compound extracted from Peucedanum japonicum Thunb, decreases levels of μ-opioid receptor, with analgesic effect.

HY-141468

β-Chlornaltrexamine dihydrochloride	Inhibitor
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-P5061

Dynorphin A (1-13) amide	Inhibitor
Dynorphin A (1-13) amide is an endogenous opioid peptide that antagonizes morphine-induced analgesia.

HY-120846

CHIR 4531	Inhibitor
CHIR 4531, a trimer peptide, is a opiate ligand that binds to the mu-opiate receptor with a K_i of 6 nM.

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