A positive allosteric modulator of mGluR8
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AZ 12216052

Item No. 29460

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[[(4-bromophenyl)methyl]thio]-N-[4-(1-methylpropyl)phenyl]-acetamide
CAS Number
1290628-31-7
Molecular Formula
C19H22BrNOS
Formula Weight
392.4
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: soluble
λmax
230, 248 nm
SMILES
BrC1=CC=C(CSCC(NC2=CC=C(C(C)CC)C=C2)=O)C=C1
InChi Code
InChI=1S/C19H22BrNOS/c1-3-14(2)16-6-10-18(11-7-16)21-19(22)13-23-12-15-4-8-17(20)9-5-15/h4-11,14H,3,12-13H2,1-2H3,(H,21,22)
InChi Key
QKUYZJOTWYRWNF-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $42

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    5 mg

    $115

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    10 mg

    $203

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    25 mg

    $454

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    Product Description

    AZ 12216052 is a positive allosteric modulator of metabotropic glutamate receptor 8 (mGluR8).1 It potentiates glutamate-induced [35S]GTPγS binding in GHEK cells expressing human mGluR8b (EC50 = 1 μM). In a cell-based model of Parkinson’s disease, AZ 12216052 inhibits MPP+-induced decreases in the viability of undifferentiated SH-SY5Y cells when used at concentrations ranging from 0.001 to 1 μM and in retinoic acid-differentiated SH-SY5Y cells at 0.1 and 1 μM.2 AZ 12216052 (10 mg/kg) increases the time spent in the open areas of the elevated zero maze and reduces the acoustic startle response in mice, indicating anxiolytic-like activity in response to avoidable and unavoidable anxiogenic stimuli, respectively.1

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Duvoisin, R.M., Pfankuch, T., Wilson, J.M., et al. Acute pharmacological modulation of mGluR8 reduces measures of anxiety. Behav. Brain Res. 212(2), 168-173 (2010).

    2. Jantas, D., Greda, A., Golda, S., et al. Neuroprotective effects of metabotropic glutamate receptor group II and III activators against MPP(+)-induced cell death in human neuroblastoma SH-SY5Y cells: The impact of cell differentiation state. Neuropharmacology 83, 36-53 (2014).