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GRN-529

Chemical Structure : GRN-529

CAS No.: 1253291-12-1

GRN-529 (GRN 529;GRN529)

Catalog No.: PC-61060Not For Human Use, Lab Use Only.

A highly potent, selective, orally active mGluR5 negative allosteric modulator with Ki of 5.4 nM, IC50 of 3.1 nM.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

A highly potent, selective, orally active mGluR5 negative allosteric modulator with Ki of 5.4 nM, IC50 of 3.1 nM; displays >1,000-fold selective vs mGluR1; reduces repetitive behaviors and rescues social deficits in mouse models of autism, demonstrates dose-dependent efficacy across a therapeutically relevant battery of animal models, comprising depression, anxiety and pain, with no effect on rat sexual behavior or motor co-ordination.

Physicochemical Properties

M.Wt 391.378
Formula C22H15F2N3O2
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

(4-(difluoromethoxy)-3-(pyridin-2-ylethynyl)phenyl)(5,7-dihydro-6H-pyrrolo[3,4-b]pyridin-6-yl)methanone

References

1. Silverman JL, et al. Sci Transl Med. 2012 Apr 25;4(131):131ra51.

2. Hughes ZA, et al. Neuropharmacology. 2013 Mar;66:202-14.

3. Harvey BD, et al. Neuropharmacology. 2013 Dec;75:19-30.

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