assay
≥98% (HPLC)
form
powder
optical activity
[α]/D -41 to -51°, c = 1 in methanol
storage condition
desiccated
color
white to beige
solubility
DMSO: 2 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
Brain-penetrant, potent and selective metabotropic glutamate receptor 1 (mGlu1) negative allosteric modulator (NAM).
VU0469650 is a brain-penetrant, potent and selective metabotropic glutamate receptor 1 (mGlu1) negative allosteric modulator (NAM). VU0469650 selectively inhibits glu-induced Ca2+ influx in human mGluR1-expressing HEK 293A (EC50 = 99 nM with [Glu] = EC20 for 1.9 min, then EC100 for 1.7 min; inactive against cells expressing human mGlu2-8 at 10 μM) with no affinity toward a panel of 68 clinically relevant GPCRs, ion channels, kinases, and transporters. Prior administration of VU0469650 in mice in vivo (60 mg/kg i.p.) modulates the antipsychotic activity of M4 muscarinic receptor PAM VU0467154 and that of the M1/M4 agonist xanomeline.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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