A GAT-1 inhibitor
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NNC-711 (hydrochloride)

Item No. 29687

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[2-[[(diphenylmethylene)amino]oxy]ethyl]-1,2,5,6-tetrahydro-3-pyridinecarboxylic acid, monohydrochloride
CAS Number
145645-62-1
Synonyms
  • NNC 05-711
  • NO-711
Molecular Formula
C21H22N2O3 • HCl
Formula Weight
386.9
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: solubleWater: 10 mM
λmax
258 nm
SMILES
OC(C1=CCCN(CCO/N=C(C2=CC=CC=C2)/C3=CC=CC=C3)C1)=O.Cl
InChi Code
InChI=1S/C21H22N2O3.ClH/c24-21(25)19-12-7-13-23(16-19)14-15-26-22-20(17-8-3-1-4-9-17)18-10-5-2-6-11-18;/h1-6,8-12H,7,13-16H2,(H,24,25);1H
InChi Key
YZYRTEYMUTWJPL-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $153

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    10 mg

    $253

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    25 mg

    $378

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    Product Description

    NNC-711 is an inhibitor of GABA transporter 1 (GAT-1; IC50 = 0.04 µM for the human transporter).1 It is selective for GAT-1 over human GAT-3 and BGT-3 (IC50s = 1,700 and 622 µM, respectively), rat GAT-2 (IC50 = 171 µM), and a panel of 21 receptors and ion channels (IC50s = >50 µM for all) in radioligand binding assays.1,2 NNC-711 inhibits GABA uptake in rat synaptosome preparations, neurons, and glia (IC50s = 47, 1,238, and 636 nM, respectively).2 In vivo, NNC-711 inhibits clonic seizures induced by pentylenetetrazole (PTZ; Item No. 18682) or DMCM in mice (ED50s = 1.2 and 3 mg/kg, respectively), as well as audiogenic tonic seizures in mice (ED50 = 0.23 mg/kg) and PTZ-induced tonic seizures in rats (ED50 = 1.7 mg/kg). Intrathecal administration of NNC-711 (100 or 200 µg/animal) decreases mechanical allodynia and thermal hyperalgesia in a rat model of neuropathic pain induced by chronic constriction injury (CCI).3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Borden, L.A., Murali Dhar, T.G., Smith, K.E., et al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur. J. Pharmacol. 269(2), 219-224 (1994).

    2. Suzdak, P.D., Frederiksen, K., Andersen, K.A., et al. NNC-711, a novel potent and selective γ-aminobutyric acid uptake inhibitor: Pharmacological characterization. Eur. J. Pharmacol. 224(2-3), 189-198 (1992).

    3. Li, Y., Li, Y., Gu, P., et al. Analgesic effect of intrathecally γ-aminobutyric acid transporter-1 inhibitor NO-711 administrating on neuropathic pain in rats. Neurosci. Lett. 494(1), 6-9 (2011).