CI 966 hydrochloride

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Cat.No. 1296 - CI 966 hydrochloride | C23H21F6NO3.HCl | CAS No. 110283-66-4
Description: Selective inhibitor of GAT-1
Chemical Name: 1-[2-[bis[4-(Trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride
Purity: ≥98% (HPLC)

Biological Activity

Selective inhibitor of the GABA transporter GAT-1 (IC50 values are 0.26 and 1.2 μM at cloned human and rat GAT-1 respectively). Displays over 200-fold selectivity over GAT-2 and GAT-3. Centrally active upon systemic administration in vivo. Anticonvulsive and neuroprotective.

Compound Libraries

CI 966 hydrochloride is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt 509.87
Formula C23H21F6NO3.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 110283-66-4
PubChem ID 198692
Smiles Cl.OC(=O)C1=CCCN(CCOC(C2=CC=C(C=C2)C(F)(F)F)C2=CC=C(C=C2)C(F)(F)F)C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

SolubilitySoluble to 10 mM in ethanol and to 100 mM in DMSO

Preparing Stock Solutions

The following data is based on the product molecular weight 509.87. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.96 mL 9.81 mL 19.61 mL
5 mM 0.39 mL 1.96 mL 3.92 mL
10 mM 0.2 mL 0.98 mL 1.96 mL
50 mM 0.04 mL 0.2 mL 0.39 mL

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Product Datasheets

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References are publications that support the products' biological activity.

Borden et al (1994) Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur.J.Pharmacol. 269 219 PMID: 7851497

Ebert et al (1990) Systemic CI-966, a new gamma-aminobutyric acid uptake blocker, enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ. Can.J.Physiol.Pharmacol. 68 1194 PMID: 2276082

Radulovic et al (1993) Pharmacokinetics, mass balance, and induction potential of novel GABA uptake inhibitor, CI-966 HCl, in laboratory animals. Pharm.Res. 10 1442 PMID: 8272405

If you know of a relevant reference for CI 966 hydrochloride, please let us know.

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