Overview
Alternative Name ML301
Lyophilized Powder yes
Source Synthetic
MW: 522.99
Purity: >98%
Effective concentration 1 nM – 1 µM.
Structure
Chemical name (2S)-2-[[1-(7-chloroquinolin-4-yl)-2-(2,6-dimethoxyphenyl)imidazole-4-carbonyl]amino]-4-methylpentanoic acid.
Molecular formula C27H27ClN4O5.
PubChem CID 49837912
Activity ML-301 is a selective agonist of NTR1 receptors, shown to stimulate NTR1-mediated calcium mobilization with EC50 of 289 nM1-2.
References-Activity
- Hershberger, P.M. et al. (2014) Bioorg. Med. Chem. Lett. 24, 262.
- Di Fruscia, P. et al. (2014) Bioorg. Med. Chem. Lett. 24, 3974.
Shipping and storage Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
Solubility Soluble in DMSO.
Centrifuge all products before handling (10000 x g 5 min).
Centrifuge all products before handling (10000 x g 5 min).
Storage of solutions Store at -20°C.
It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
Our bioassay
Alomone Labs ML-301 activates human NTR1 receptors expressed in CHO-K1 cells.Dose-response curve of hNTSR1 activation by ML-301 (#M-315), normalized to maximum effect of neurotensin. Cells were loaded with Fluo-8 dye and stimulated with increasing concentrations of ML-301. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence using FLIPRTETRA™.
Scientific background
ML-301 is a fully selective imidazole-based agonist of neurotensin receptor 1 (NTR1). It stimulates NTR1-mediated calcium mobilization with an EC50 value of 289 nM1. The carboxylic acid moiety increases the compound’s solubility1.
To date, four neurotensin receptors have been cloned from human: NTR1, NTR2, NTR3 and NTR4 which belong to the super family of G-protein coupled receptors (GPCRs). NTR1 mediates most of the known neurotensin ligand effects and is a potential therapeutic target2.
Target Neurotensin Receptor 1
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
Citations
