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Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
18 Results for "
human κ-opioid receptor
" in MedChemExpress (MCE) Product Catalog:
Products (18)
18 Results for "human κ-opioid receptor" in MCE Product Catalog:
19
19 Publications Verification
Synonyms: Matridin-15-one; Vegard; α-Matrine
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Naldemedine (S-297995) tosylate is an orally active μ-opioid receptor antagonist (PAMORA) . Naldemedine tosylate 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 tosylate is predicted to bind to 3CL pro encoded by SARS-CoV2 genome .
Cat. No.: HY-P2159
CAS No.: 75790-53-3
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Synonyms: 5'-GNTI hydrochloride
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5'-Guanidinonaltrindole (5'-GNTI) hydrochloride is a highly selective and potent κ-opioid receptor antagonist with a Ki of 0.18 nM for human κ-opioid receptor .
Cat. No.: HY-P3445
CAS No.: 2269511-95-5
Synonyms: HSK21542
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Cat. No.: HY-19627
CAS No.: 916072-89-4
Synonyms: S-297995
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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 .
Cat. No.: HY-121800
CAS No.: 1355243-24-1
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ML138 is a blood-brain barrier-permeable κ-opioid receptor (KOR) agonist, with an EC50 value of 0.87 μM and a human Ki value of 2.4 nM for human receptors; it exhibits high selectivity for KOR over μ, δ and other receptors. ML138 activates β-arrestin (beta-arrestin)-mediated signaling pathways, stimulates G protein coupling, and activates the downstream extracellular regulated protein kinase 1/2 (ERK1/2) mitogen-activated protein kinase (MAP kinase) signaling pathway. ML138 is applicable to research related to addictive behaviors .
Cat. No.: HY-W019787
CAS No.: 75513-71-2
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Cat. No.: HY-170973
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KOR agonist 4 (compound 39) is an agonist of Kappa Opioid Receptor. KOR agonist 4 is an activator of G-protein signaling. KOR agonist 4 binds with GTPγS with an EC50 of 14 nM and with an Emax of 83 %. KOR agonist 4 demonstrates moderate to high intrinsic clearance in human hepatocytes. KOR agonist 4 exhibits 60- and 810-fold selectivities versus the related mu (MOR) and delta (DOR) opioid receptors. KOR agonist 4 is potential for central nervous system (CNS) disorders research .
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Akuammine is an indole alkaloid that has been found in Picralima nitida and has analgesic activity. It selectively binds to the μ- and κ-opioid receptors over the δ-opioid receptor (Kis=0.3, 1.68, and 10.4 μM for the human receptors, respectively). Akuammine inhibits forskolin-induced cAMP production in HEK293 cells expressing human μ- or κ-opioid receptors (IC50s=2.6 and 0.073 μM, respectively). It increases the latency to withdrawal in the tail-flick or hot plate test in mice when administered at a dose of 60 mg/kg.
Cat. No.: HY-108043
CAS No.: 875647-81-7
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AZD-2327 is a potent and selective δ-opioid receptor agonist. AZD-2327 binds to the human opioid receptor (Ki of 0.49 and 0.75 nM and EC50 of 24 and 9.2 nM at the C27 and F27 isoforms, respectively). AZD-2327 shows selectivity of >1000-fold over the human μ- and κ-opioid receptor subtypes as well as >130 other receptors and channels. AZD-2327 exhibits antidepressant and anxiolytic activities and can be used for the research of neurological disease .
Cat. No.: HY-W654256
Synonyms: Matridin-15-one-d3; Vegard-d3; α-Matrine-d3
Cat. No.: HY-P11642A
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Cat. No.: HY-P10006
CAS No.: 88846-98-4
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Cat. No.: HY-P5892
CAS No.: 76622-84-9
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Cat. No.: HY-10672
CAS No.: 1034708-07-0
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Urotensin-II receptor antagonist-1 (compound 1) is a low oral bioavailability (F=0-3%, rat) selective human Urotensin II receptor antagonist, Ki=16 nM (test on HEK293 cells expressing recombinant human UT receptor). Urotensin-II receptor antagonist-1 inhibits cytochrome P450 (IC50=0.75 μM, CYP2D6; 1.4 μM, CYP3A4), inhibits κ-opioid receptor (EC50=3.2 μM), targets cardiac sodium channels (Ki=2.5 μM) .
Synonyms: Matridin-15-one (Standard); Vegard (Standard); α-Matrine (Standard)
Cat. No.: HY-181515
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KOR agonist 8 (Compound 8a) is a κ-opioid receptor (KOR) agonist and an analgesic agent, with a Ki value of 5.3 nM for human KOR, and EC50 values of 43.1 nM and 9236 nM for human KOR. It exhibits subtype selectivity for MOR/KOR and DOR/KOR. KOR agonist 8 is applicable for pain-related research .
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Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
