ML138
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.
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- CAS No.: 1355243-24-1
- Formule: C19H14Cl2N4OS
- Masse moléculaire:417.31
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Stockage:
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
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human κ-opioid receptor (hKOR) 0.87 μM (EC50) |
human κ-opioid receptor (hKOR) 2.4 nM (Ki) |
ERK1 |
ERK2 |
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Cell Line
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Type | Value | Description | References |
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| U2OS | EC50 |
0.87 μM
Compound: 31
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Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by luminescence assay
Agonist activity at human kappa opioid receptor expressed in human U2OS cells co-transfected with EFC and beta-arrestin-2 assessed as increase in beta-arrestin-2 recruitment after 90 mins by luminescence assay
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[PMID: 29939744] |
ML138 acts as a κ-opioid receptor agonist in the KOR DiscoveRx β-arrestin PathHunter cell assay, with an EC50 of 0.87 μM[1].
ML138 acts as a κ-opioid receptor (KOR) agonist in cellular assays based on high-content imaging of β-arrestin translocation mediated by κ-opioid receptors, with an EC50 of 0.35 μM, and exhibits over 100-fold selectivity over MOR and DOR[1].
ML138 binds to the κ-opioid receptor with high affinity (Ki = 2.4 nM), exhibits over 792-fold selectivity for MOR and over 2000-fold selectivity for DOR, and shows weak binding to 11 non-opioid targets[1].
ML138 (10 µM; 1.5 h) inhibits κ-opioid receptor activity in OPRK1 β-arrestin cells, with an IC50 of 870 nM[2].
ML138 activates cells expressing KOR, with an EC50 of 350 nM in the HCS-Transfluor assay[2].
ML138 binds potently and selectively to the κ-opioid receptor with a Ki value of 0.23 nM, exhibiting over 2100-fold selectivity over μ and δ-opioid receptors, and over 5000-fold selectivity over weakly bound off-target GPCRs[2].
ML138 stimulates the coupling of G proteins to κ-opioid receptors, with an EC50 of 55.2 nM[2].
ML138 stimulates ERK1/2 phosphorylation in cells expressing κ-opioid receptors[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1355243-24-1
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Masse moléculaire 417.31
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Formule C19H14Cl2N4OS
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SMILES
ClC1=CC=C(CSC2=NN=C(C3=NC=CC=C3)N2CC4=CC=CO4)C=C1Cl
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Frankowski KJ, et al. Discovery of Small Molecule Kappa Opioid Receptor Agonist and Antagonist Chemotypes through a HTS and Hit Refinement Strategy. ACS chemical neuroscience. 2012 Mar 21;3(3):221-236. [Content Brief]
[2]. Hedrick MP, et al. Selective KOP Receptor Agonists: Probe 1 & Probe 2. 2010 Feb 28 [updated 2010 Oct 4]. In: Probe Reports from the NIH Molecular Libraries Program [Internet]. Bethesda (MD): National Center for Biotechnology Information (US); 2010-. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ML138 Related Classifications
HY-121800 Related Classifications
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