SR 142948 TFA
Based on 1 publication(s) in Google Scholar
SR 142948 TFA is an orally active and selective non-peptide neurotensin receptor (NT) antagonist with IC50s of 1.19 nM, 0.32 nM, 3.96 nM in h-NTR1-CHO cells, HT-29 cells, and adult rat brain, respectively. SR 142948 TFA antagonizes NT-induced inositol monophosphate formation in HT-29 cells with an IC50 of 3.9 nM. SR 142948 TFA blocks hypothermia, analgesia and steering behavior induced by NT in vivo. SR 142948 TFA shows blood-brain permeability and can be used in study of psychiatric disorders.
For research use only. We do not sell to patients.
- Formula: C41H52F3N5O8
- Molecular Weight:799.88
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) SR 142948 TFA
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Biological Activity
Description
In Vitro
SR 142948 (1 µM; 90 min) TFA inhibits expression of c-fos and krox24 in CHO-hNT1-R cells[1].
SR 142948 (0-1 µM; 1 h) TFA exhibits good antagonistic activity by inhibiting [125I-Tyr3]NT binds to h-NTR1-CHO and HT 29 cell membranes, with IC50s of 1.19 and 0.32 nM, respectively[2].
SR 142948 (0-1 µM; 30 min) TFA antagonizes production of IP1 stimulated by NT both in h-NTR1-CHO and HT 29 cells, in a concentration-dependent manner[2].
SR 142948 (1, 10 nM; 60-80 s) TFA antagonizes intracellular calcium mobilization stimulated by NT in h-NTR1-CHO cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
SR 142948 (0.01, 0.03, 0.3 mg/kg; i.p.; single) TFA prevents the enhancement of ACh release produced by NT (100 nM), in a dose-dependent manner[2].
SR 142948 (0-10 mg/kg; p.o.; single) TFA partially but significantly blocks NT-induced hypothermia (53% at 2 mg/kg in rats and 54% at 4 mg/kg in mice)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Molecular Weight 799.88
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Formula C41H52F3N5O8
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SMILES
O=C(C1=NN(C2=C(C=C(C(N(C)CCCN(C)C)=O)C=C2)C(C)C)C(C3=C(C=CC=C3OC)OC)=C1)NC4([C@H]5C[C@H](C6)C[C@@H]4C[C@H]6C5)C(O)=O.FC(C(O)=O)(F)F
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (1)
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Journal Impact Factor
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Most Recent
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
References
[1]. Portier M, et al. Neurotensin type 1 receptor-mediated activation of krox24, c-fos and Elk-1: preventing effect of the neurotensin antagonists SR 48692 and SR 142948. FEBS Lett. 1998 Jul 31;432(1-2):88-93. [Content Brief]
[2]. Gully D, et al. Biochemical and pharmacological activities of SR 142948A, a new potent neurotensin receptor antagonist. J Pharmacol Exp Ther. 1997 Feb;280(2):802-12. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)