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GRN-529

Cat. No. M8086

All AbMole products are for research use only, cannot be used for human consumption.

GRN-529 Structure

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Biological Activity

GRN-529 is a brain penetrant, potent and selective negative allosteric modulator of the mGluR5 receptor (metabotropic glutamate receptor subtype 5) with an IC50 of 3.1 nM and >1000-fold selectivity vs mGluR1. GRN-529 was shown to alleviate multiple diagnostic behavioral symptoms of autism in BTBR and C58 mice models.

Chemical Information
Molecular Weight 391.37
Formula C22H15F2N3O2
CAS Number 1253291-12-1
Solubility (25°C) DMSO: 5 mg/mL (warmed)
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
References

[1] B D Harvey, et al. Neurophysiological signals as potential translatable biomarkers for modulation of metabotropic glutamate 5 receptors

[2] Lindsay Borthwick. Adulthood: Life lessons

[3] Z A Hughes, et al. Negative allosteric modulation of metabotropic glutamate receptor 5 results in broad spectrum activity relevant to treatment resistant depression

[4] Jill L Silverman, et al. Negative allosteric modulation of the mGluR5 receptor reduces repetitive behaviors and rescues social deficits in mouse models of autism

[5] Vasee S Moorthy, et al. Immunological mechanisms underlying protection mediated by RTS,S: a review of the available data

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Keywords: GRN-529 supplier, inhibitors, activators

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