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BMS-984923

Chemical Structure : BMS-984923

CAS No.: 1375755-46-6

BMS-984923 (BMS984923;BMS 984923)

Catalog No.: PC-35962Not For Human Use, Lab Use Only.

BMS-984923 (BMS-984923) is a potent silent allosteric modulator (SAM) of mGluR5 with competitive antagonism of MPEPy binding with Ki of 0.6 nM, but has no detectable agonist and antagonist activity at mGluR5 signaling.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

BMS-984923 (BMS-984923) is a potent silent allosteric modulator (SAM) of mGluR5 with competitive antagonism of MPEPy binding with Ki of 0.6 nM, but has no detectable agonist and antagonist activity at mGluR5 signaling; does not affect glutamate/DHPG ((S)-3,5-Dihydroxyphenylglycine)-induced Ca2+ signaling in mGluR5-overexpressing HEK293T cells and cultured nureons; reduces the interaction of PrPC with mGluR5 in membrane fractions, prevents Aβo-induced signal transduction in brain slices, and rescues memory deficits and synaptic depletion in the APPswe/PS1ΔE9 transgenic mouse brain.

Physicochemical Properties

M.Wt 374.824
Formula C22H15ClN2O2
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

(4R,5R)-rel-5-(2-chlorophenyl)-4-(5-(phenylethynyl)pyridin-3-yl)oxazolidin-2-one

References

1. Huang H, et al. Bioorg Med Chem Lett. 2016 Sep 1;26(17):4165-9.

2. Haas LT, et al. Cell Rep. 2017 Jul 5;20(1):76-88.

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