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VU0424238

Chemical Structure : VU0424238

CAS No.: 1396337-04-4

VU0424238 (VU 0424238;Auglurant)

Catalog No.: PC-63197Not For Human Use, Lab Use Only.

VU0424238 (Auglurant) is a potent, selective, orally active mGlu5 negative allosteric modulator with Ki of 4.4 nM, displays >900-fold selectivity for mGlu5 versus the other mGlu receptors.

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Purity & Documentation Purity: >98% (HPLC)

Biological Activity

VU0424238 (Auglurant) is a potent, selective, orally active mGlu5 negative allosteric modulator with Ki of 4.4 nM, displays >900-fold selectivity for mGlu5 versus the other mGlu receptors; demonstrates 50% receptor occupancy at an oral dose of 0.8 mg/kg in rats and an intravenous dose of 0.06 mg/kg in baboons.

Physicochemical Properties

M.Wt 325.303
Formula C16H12FN5O2
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

N-(5-Fluoropyridin-2-yl)-6-methyl-4-(pyrimidin-5-yloxy)picolinamide

References

1. Felts AS, et al. J Med Chem. 2017 Jun 22;60(12):5072-5085.

2. Crouch RD, et al. Drug Metab Dispos. 2017 Dec;45(12):1245-1259.

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