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SR 48692

Chemical Structure : SR 48692

CAS No.: 146362-70-1

SR 48692 (Meclinertant;SR48692;SR-48692)

Catalog No.: PC-60947Not For Human Use, Lab Use Only.

A potent, selective and orally active nonpeptide antagonist of the neurotensin receptor with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A potent, selective and orally active nonpeptide antagonist of the neurotensin receptor with IC50 of 0.99 nM (guinea pig), without any intrinsic agonist activity; blocks K(+)-evoked release of [3H]dopamine stimulated by neurotensin in guinea pig striatal slices with IC50 of 0.46 nM, competitively antagonizes neurotensin-induced intracellular Ca2+ mobilization with pA2 of 8.13 in H29 cells; reverses the turning behavior induced by intrastriatal injection of neurotensin in mice.

Lung Cancer

Phase 2 Clinical

Physicochemical Properties

M.Wt 587.073
Formula C32H31ClN4O5
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(1r,3r,5r,7r)-2-(1-(7-chloroquinolin-4-yl)-5-(2,6-dimethoxyphenyl)-1H-pyrazole-3-carboxamido)adamantane-2-carboxylic acid

References

1. Dubuc I, et al. Br J Pharmacol. 1994 Jun;112(2):352-4.

2. Steinberg R, et al. Neuroscience. 1994 Apr;59(4):921-9.

3. Brouard A, et al. Eur J Pharmacol. 1994 Mar 3;253(3):289-91.

4. Gully D, et al. Proc Natl Acad Sci U S A. 1993 Jan 1;90(1):65-9.

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