Overview
Alternative Name SR48527
Lyophilized Powder yes
Source Synthetic
MW: 549
Purity: >95%
Effective concentration 1 nM – 1 µM.
Structure
Chemical name (2S)-2-[[1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)pyrazole-3-carbonyl]amino]-2-cyclohexylacetic acid.
Molecular formula C29H29ClN4O5.
CAS No.: 156579-04-3
PubChem CID 9915499
Activity SR 48527, an analog of SR 48692, is a potent and selective antagonist of NTS1 receptors, shown to inhibit neurotensin-stimulated IP production with Ki of 24 nM1,2.
References-Activity
- Labbe-Jullie, C. et al. (1994) J. Pharmacol. Exp. Ther. 271, 267.
- Labbe-Jullie, C. et al. (1998) J. Biol. Chem. 273, 16351.
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).
Storage of solutions Store at -20°C. It is recommended to aliquot stock solutions to prevent repeated thawing and freezing.
Our bioassay
Alomone Labs SR 48527 inhibits human NTS1 receptors expressed in CHO-K1 cells.Dose-response curve of hNTSR1 normalized inhibition by SR 48527 (#S-225). Cells were loaded with Fluo-8 dye, incubated with increasing concentrations of SR 48527, and stimulated with 3 nM neurotensin. Changes in intracellular Ca2+ following agonist application were detected as changes in maximum relative fluorescence (RLU) using FLIPRTETRA™. IC50 was calculated at 0.72 µM.
Scientific background
SR 48527 is a potent and selective antagonist of neurotensin receptor 1 (NTR1/NTS1). It is an analog of SR 48692 and inhibits neurotensin-stimulated IP production with a Ki value of 24 nM1,2.
The two neurotensin receptors, NTR1 and NTR2, belong to the family of G-protein-coupled receptors1,2. The receptors are expressed in the brain and gastrointestinal tract where they play a role in pain transmission and intestinal motility.
Target Neurotensin Receptor 1
Lyophilized Powder
For research purposes only, not for human use
Last Update: 07/05/2024
Specifications
Citations
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