Opioid Receptor Antagonist

Opioid Receptor Antagonists (111):

Cat. No.	Product Name	Effect	Purity

HY-17417

Naloxone hydrochloride	Antagonist	99.96%
Naloxone hydrochloride is an antagonist of Opioid receptor. Naloxone hydrochloride alleviates opioid-overdose-induced respiratory depression. Naloxone hydrochloride may cause pulmonary edema and cardiac arrhythmias.

HY-107750

Cyprodime	Antagonist
Cyprodime is a selective μ opioid receptor (MOR) antagonist with K_is of 5.4, 244.6, and 2187 nM for μ, δ, and κ, respectively.

HY-101718

Aticaprant	Antagonist	99.87%
Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a K_i of 0.807 nM.

HY-100903

Norbinaltorphimine dihydrochloride	Antagonist	98.91%
Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.

HY-13274

JTC-801	Antagonist	98.91%
JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist, binding to ORL1 receptor with a K_i value of 8.2 nM.

HY-10487

JDTic dihydrochloride	Antagonist	98.03%
JDTic (dihydrochloride) is a potent antagonist of kappa-opioid receptors (KOR), blocking the κ-agonist U50, 488-induced antinociception.

HY-101302

Naltriben mesylate	Antagonist	99.65%
Naltriben mesylate is a potent δ2-opioid receptor antagonist and a TRPM7 activator. Naltriben mesylate shows K_i values of 0.013 nM, 19 nM and 152 nM for δ, μ and κ receptors, respectively. Naltriben mesylate enhances glioblastoma cell migration and invasion. Naltriben mesylate can be used in research into neurological diseases and cancer.

HY-114452

LY2940094	Antagonist	99.91%
LY2940094 (BTRX-246040) is a potent, selective and orally available nociceptin receptor (NOP receptor) antagonist with high affinity (K_i=0.105 nM) and antagonist potency (K_b=0.166 nM). LY2940094 reduces ethanol self-administration in animal models.

HY-76657A

Alvimopan dihydrate	Antagonist	98.66%
Alvimopan dihydrate (ADL 8-2698 dihydrate) is a potent, selective, orally active and reversible μ-opioid receptor antagonist, with an IC₅₀ of 1.7 nM. Alvimopan dihydrate has selectivity for μ-opioid receptor (K_i=0.47 nM) over κ- and δ-opioid receptors (K_is=100, 12 nM, respectively). Alvimopan dihydrate can be used for the research of postoperative ileus.

HY-P1335A

CTAP TFA	Antagonist	99.60%
CTAP TFA is a potent, highly selective, and BBB penetrant μ opioid receptor antagonist, with an IC₅₀ of 3.5 nM. CTAP TFA displays over 1200-fold selectivity over δ opioid (IC₅₀=4500 nM) and somatostatin receptors. CTAP TFA can be used for the study of L-DOPA-induced dyskinesia (LID) and opiate overdose or addiction.

HY-19627A

Naldemedine tosylate	Antagonist
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-76711

Naltrexone	Antagonist	99.94%
Naltrexone is an antagonist of Opioid receptor. Naltrexone inhibits cell proliferation in vivo. Naltrexone reduces tumor growth by interfering with cell signalling and modifying the immune system.

HY-17417A

Naloxone	Antagonist	99.71%
Naloxone is an antagonist of Opioid receptor. Naloxone alleviates opioid-overdose-induced respiratory depression. Naloxone may cause pulmonary edema and cardiac arrhythmias.

HY-137279

Naloxone methiodide	Antagonist	99.7%
Naloxone methiodide is a peripherally restricted, nonselective, and competitive opioid receptor antagonist. Naloxone methiodide does not penetrate the blood-brain barrier.

HY-A0118A

Naloxegol oxalate	Antagonist	99.91%
Naloxegol oxalate (NKTR-118 oxalate; AZ-13337019 oxalate) is a μ-opioid-receptor antagonist. Naloxegol oxalate inhibits opioid binding in μ-opioid receptors in the gastrointestinal tract and effective for alleviating opioid-induced constipation.

HY-117040

nor-Binaltorphimine	Antagonist	98.70%
nor-Binaltorphimine is a selective antagonist of kappa-opioid receptor. nor-Binaltorphimine has a long-lasting effect in vivo.

HY-13222

BAN ORL 24	Antagonist	99.68%
BAN ORL 24 is a nociceptin/orphanin FQ (N/OFQ) peptide receptor (NOP) antagonist. BAN ORL 24 has antagonistic effect for nociceptin (NOP) receptor with K_I value of 0.24 nM in CHO cell. BAN ORL 24 can be used for the research of cancer and analgesic.

HY-136208

TAN-452	Antagonist	99.44%
TAN-452 is an orally active, selective peripherally acting δ-opioid receptor (DOR) antagonist with a K_i of 0.47 nM and a K_b of 0.21 nM. TAN-452 is an antagonist for μ-opioid receptor (MOR; K_i=36.56 nM and K_b=9.43 nM) and κ-opioid receptor (KOR; K_i=5.31 nM and K_b=7.18 nM). TAN-452, a derivative of Naltrindole, demonstrates low brain penetrability and attenuates morphine-induced side effects without affecting pain control.

HY-P1329A

CTOP TFA	Antagonist	99.84%
CTOP TFA is a potent and highly selective μ-opioid receptor antagonist. CTOP TFA antagonizes the acute analgesic effect and hypermotility. CTOP TFA enhances extracellular dopamine levels in the nucleus accumbens. CTOP TFA dose-dependently enhances locomotor activity.

HY-107721

(±)-J-113397	Antagonist	98.59%
(±)-J-113397 is a potent and selective non-peptidyl ORL1 receptor antagonist with a K_i of 1.8 nM for cloned human ORL1. J-113397 inhibited nociceptin/orphanin FQ-stimulated GTPγS binding to CHO cells expressing ORL1 with an IC₅₀ value of 5.3 nM. J-113397 can be used for researching the physiological roles of nociceptin/orphanin FQ.

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