A negative allosteric modulator of mGluR1
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VU0469650 (hydrochloride)

Item No. 32933

Technical Information
Formal Name
3-[(3R)-3-methyl-4-(tricyclo[3.3.1.13,7]dec-1-ylcarbonyl)-1-piperazinyl]-2-pyridinecarbonitrile, monohydrochloride
Molecular Formula
C22H28N4O • HCl
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: 100 mMEthanol: 50 mM
SMILES
O=C(N(CCN(C(C=CC=N1)=C1C#N)C2)[C@@H]2C)C3(C[C@H](C4)C5)C[C@H]5C[C@H]4C3.Cl
InChi Code
InChI=1S/C22H28N4O.ClH/c1-15-14-25(20-3-2-4-24-19(20)13-23)5-6-26(15)21(27)22-10-16-7-17(11-22)9-18(8-16)12-22;/h2-4,15-18H,5-12,14H2,1H3;1H/t15-,16-,17+,18-,22?;/m1./s1
InChi Key
YENVAZRENOYZGQ-CBHDUDCMSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    VU0469650 is a brain-penetrant negative allosteric modulator of metabotropic glutamate receptor 1 (mGluR1).1 It inhibits glutamate-induced calcium flux in cells expressing human mGluR1 (IC50 = 99 nM). VU0469650 is greater than 100-fold selective for mGluR1 over mGluR2-8 at 10 µM.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Lovell, K.M., Felts, A.S., Rodriguez, A.L., et alN-Acyl-N'-arylpiperazines as negative allosteric modulators of mGlu1: Identification of VU0469650, a potent and selective tool compound with CNS exposure in rats. Bioorg. Med. Chem. Lett. 23(13), 3713-3718 (2013).