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Meclinertant Inhibitor

For Research Use Only. Not for use in diagnostic procedures. Catalog #: MBS5755176

Meclinertant is an effective, selective, nonpeptide, and orally active neurotensin receptor 1 (NTS1) antagonist. Meclinertant competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization (pA2 : 8.13), in human colon carcinoma (HT-29) cells.… More details

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Technical Datasheet View PDF
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Product Overview

Online Datasheet in PDF
Product Name
Meclinertant, Inhibitor
Full Product Name
Meclinertant
Product Synonym Names
SR 48692
Form/Format
Solid. Powder
Purity/Purification
98.00%
Preparation and Storage
Store at -20 degree C for 3 years powder
-80 degree C for 2 years in solvent
Molecular Weight
587.07
Solubility
<1mg/ml refers to the product slightly soluble or insoluble
Formula
C32H31ClN4O5
SMILES
O=C(C1=NN(C2=CC=NC3=C2C=CC(Cl)=C3)C(C4=C(C=CC=C4OC)OC)=C1)NC5([C@H]6C[C@H](C7)C[C@@H]5C[C@H]7C6)C(O)=O
CAS Number
146362-70-1
Target & IC50
Neurotensin receptor 1 (NTS1)
In Vitro
Meclinertant displaces 125I-labeled neurotensin from the low-affinity levocabastine-sensitive binding sites but at higher concentrations (34.8nM for adult mouse brain and 82.0nM for adult rat brain). Meclinertant competitively inhibits 125I-labeled neurotensin binding to the high-affinity binding site present in brain tissue from various species with IC50 values of 0.99nM (guinea pig), 4.0nM (rat mesencephalic cells), 7.6nM (COS-7 cells transfected with the cloned high-affinity rat brain receptor), 13.7nM (newborn mouse brain), 17.8nM (newborn human brain), 8.7nM (adult human brain), and 30.3nM (HT-29 cells). Meclinertant blocks K+-evoked release of [3H]dopamine stimulated by neurotensin with a potency (IC50 = 0.46nM) that correlates with its binding affinity, in guinea pig striatal slices[1].

Product References and Citations for Meclinertant, inhibitor

Gully D, et al. Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):65-9.
Gully D, et al. Biochemical and pharmacological profile of a potent and selective nonpeptide antagonist of the neurotensin receptor. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):65-9.
Griebel G, et al. Characterization of the profile of neurokinin-2 and neurotensin receptor antagonists in the mouse defense test battery. Neurosci Biobehav Rev. 2001 Dec;25(7-8):619-26.
Griebel G, et al. Characterization of the profile of neurokinin-2 and neurotensin receptor antagonists in the mouse defense test battery. Neurosci Biobehav Rev. 2001 Dec;25(7-8):619-26.
Felszeghy K, et al. Neurotensin receptor antagonist administered during cocaine withdrawal decreases locomotor sensitization and conditioned place preference. Neuropsychopharmacology. 2007 Dec;32(12):2601-10.
Felszeghy K, et al. Neurotensin receptor antagonist administered during cocaine withdrawal decreases locomotor sensitization and conditioned place preference. Neuropsychopharmacology. 2007 Dec;32(12):2601-10.

Other Notes

Small volumes of Meclinertant, inhibitor vial(s) may occasionally become entrapped in the seal of the product vial during shipment and storage. If necessary, briefly centrifuge the vial on a tabletop centrifuge to dislodge any liquid in the container`s cap. Certain products may require to ship with dry ice and additional dry ice fee may apply.

Searchable Terms for Meclinertant purchase

MBS5755176 is an inhibitor targeting Meclinertant.
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