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Key Documents

SML3168

Sigma-Aldrich

VU0469650 hydrochloride

≥98% (HPLC)

Synonym(s):

VU0469650 hydrochloride, 3-[(3R)-3-Methyl-4-(tricyclo[3.3.1.13,7]dec-1-ylcarbonyl)-1-piperazinyl]-2-pyridinecarbonitrile, hydrochloride salt, VU 0469650 HCl, VU-0469650 HCl

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About This Item

Empirical Formula (Hill Notation):
C22H28N4O · HCl
Molecular Weight:
400.94
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

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

Biochem/physiol Actions

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.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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