1355243-24-1
Chemical Structure
ML138
- CAS No.: 1355243-24-1
- Formula:C19H14Cl2N4OS
- Molecular Weight:417.31
IUPAC Name: 2-(5-((3,4-dichlorobenzyl)thio)-4-(furan-2-ylmethyl)-4H-1,2,4-triazol-3-yl)pyridine
InChIKey: QDXGAJIGONMOCL-UHFFFAOYSA-N
SMILES: ClC1=CC=C(CSC2=NN=C(C3=NC=CC=C3)N2CC4=CC=CO4)C=C1Cl
Biological Activity: 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[1][2].
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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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References
- [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]
