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Opioid Receptor Opioid Receptor

Inhibitors

Cat.No.  Name Information
M4808 TRV130 hydrochloride TRV130 hydrochloride (Oliceridine) is a novel μ-opioid receptor (MOR) G protein-biased ligand.
M21375 BMS-986187 BMS-986187 is a δ-opioid receptor selective orthosteric modulator (PAM) with an EC50 of 0.03 μM and a pKB of 6.02 (~1 μM). bms-986187 has no observable PAM activity at the μ receptor (EC50=3 μM).
M21363 TRV-130 TRV 130 is a novel μ-opioid receptor (MOR) G protein-biased ligand; elicits robust G protein signaling(pEC50=8.1), with potency and efficacy similar to morphine, but with far less β-arrestin recruitment and receptor internalization.
M21325 β-Casomorphin, human β-Casomorphin, human is an opioid-like peptide that is an opioid receptor agonist. Sequence: Tyr-Pro-Phe-Val-Glu-Pro-Ile.
M21324 β-Casomorphin, bovine β-casomorphin, bovine (β-Casomorphin-7 (bovine)) is an opioid-active peptide with an IC50 value of 14 μM for binding to opioid receptors.Sequence:Tyr-Pro-Phe-Pro-Gly-Pro-Ile.
M21317 EST73502 EST73502 is a selective, orally active, μ-opioid receptor (μ-opioid receptor/MOR) agonist and σ1 receptor (σ1R) antagonist that crosses the blood-brain barrier with Ki values of 64 nM and 118 nM for MOR and σ1R effects, respectively. EST73502 can be used in pain relief studies.
M20425 (-)-Menthol (-)-Menthol is a levo isomer of menthol and used as a cooling agent that strongly activates TRPM8.
M14033 Ro 64-6198 Ro 64-6198 is a potent, selective, nonpeptide, high-affinity, high cellular permeability and brain penetration N/OFQ receptor (NOP) agonist with an EC50 value of 25.6 nM.
M14032 Norbinaltorphimine dihydrochloride Norbinaltorphimine dihydrochloride is a potent and selective κ opioid receptor antagonist.
M14031 Methylnaltrexone Bromide Methylnaltrexone Bromide, a quaternary derivative of Naltrexone, is an orally active and selective mu-opioid receptor antagonist, functions as a peripherally acting receptor antagonist in tissues of the gastrointestinal tract.
M14030 Matrine Matrine (Matridin-15-one) is an alkaloid found in plants from the Sophora genus. It has a variety of pharmacological effects, including anti-cancer effects, and action as a kappa opioid receptor and u-receptor agonist.
M14029 Aticaprant Aticaprant (CERC-501) is a potent and centrally-penetrant kappa opioid receptor antagonist with a Ki of 0.807 nM.
M14028 Deltorphin 2 TFA Deltorphin 2 TFA is a selective peptide agonist for the δ opioid receptor.
M11311 BMS-986122 Bms-986122 is a selective and effective positive allosteric regulator of μ -opioid receptor (µ-OR). Bms-986122 showed enhancement of β -inhibitory protein recruitment, adenylate cyclase inhibition and G-protein activation mediated by normal agonists. Bms-986122 enhances damGO-mediated [35S]GTPγS binding in mouse meninges.
M11163 Dermorphin Dermorphin is a natural heptapeptide μ-opioid receptor (MOR) agonist found in amphibian skin. Dermorphin can be used to suppress neuralgia.
M10584 SR17018 SR17018 is an mu-opioid-receptor (MOR) agonist, EC50 is 97 nM for binding with GTPγS.
M10570 Adrenorphin (Metorphamide) Adrenorphin (Metorphamide) is a opioid octapeptide, acting as a potent agonist of μ-opioid receptor, with Ki of 12 nM.
M10564 CYT-1010 CYT-1010 is a mu-opioid receptor agonist with EC50s of 13.1 nM and 0.0053 nM on beta-arrestin recruitment and inhibition of cAMP production, respectively.
M10563 Dynorphin A (1-8) Dynorphin A (1-8) is the most likely natural ligand of the kappa receptor. Dynorphin A (1-8) inhibited 3H-Bremazocine binding to the purified kappa receptor with IC50 of 303 nM.
M10510 LY2940094 LY-2940094 is a potent, selective and orally available antagonist of nociceptin receptor (NOP receptor) with Ki of 0.105 nM and Kb of 0.166 nM.
M10484 Nalfurafine hydrochloride Nalfurafine hydrochloride (TRK-820 hydrochloride) is a potent selective and orally active kappa opioid receptor (KOR) agonist.



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