A GAT2 and GAT3 inhibitor
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SNAP 5114

Item No. 44097

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[2-[tris(4-methoxyphenyl)methoxy]ethyl]-3S-piperidinecarboxylic acid
CAS Number
157604-55-2
Molecular Formula
C30H35NO6
Formula Weight
505.6
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Acetonitrile: Slightly Soluble: 0.1-1 mg/mlDMSO: Sparingly Soluble: 1-10 mg/ml
SMILES
COC1=CC=C(C(C2=CC=C(OC)C=C2)(OCCN3CCC[C@@H](C3)C(O)=O)C4=CC=C(OC)C=C4)C=C1
InChi Code
InChI=1S/C30H35NO6/c1-34-26-12-6-23(7-13-26)30(24-8-14-27(35-2)15-9-24,25-10-16-28(36-3)17-11-25)37-20-19-31-18-4-5-22(21-31)29(32)33/h6-17,22H,4-5,18-21H2,1-3H3,(H,32,33)/t22-/m0/s1
InChi Key
VDLDUZLDZBVOAS-QFIPXVFZSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $125

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    10 mg

    $238

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    50 mg

    $625

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    100 mg

    $1,000

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    Product Description

    SNAP 5114 is an inhibitor of GABA transporter 2 (GAT2) and GAT3 (IC50s = 21 and 5 µM, respectively).1 It is selective for GAT2 and GAT3 over GAT1 and Betaine/GABA transporter 1 (BGT1) in a GABA transport assay (IC50s = >200 and 140 µM, respectively). SNAP 5114 decreases sound-induced seizures in a mouse model of audiogenic seizures (ED50 = 26 mg/kg).2 It reduces immobility time in the forced swim test in mice when administered at a dose of 30 mg/kg.3 SNAP 5114 decreases the nocifensive response in the acetic acid-induced writhing test in mice (ED50 = 8.6 mg/kg).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Dhar, T.G., Borden, L.A., Tyagarajan, S., et al. Design, synthesis and evaluation of substituted triarylnipecotic acid derivatives as GABA uptake inhibitors: Identification of a ligand with moderate affinity and selectivity for the cloned human GABA transporter GAT-3. J. Med. Chem. 37, 2334-2342 (1994).

    2. Madsen, K.K., Clausen, R.P., Larsson, O.M., et al. Synaptic and extrasynaptic GABA transporters as targets for anti-epileptic drugs. J. Neurochem. 109 (Suppl. 1), 139-144 (2009).

    3. Sałat, K., Kulig, K., Gajda, J., et al. Evaluation of anxiolytic-like, anticonvulsant, antidepressant-like and antinociceptive properties of new 2-substituted 4-hydroxybutanamides with affinity for GABA transporters in mice. Pharmacol. Biochem. Behav. 110, 145-153 (2013).