CI 966 hydrochloride

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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)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for CI 966 hydrochloride

CI 966 hydrochloride is a 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 for CI 966 hydrochloride

CI 966 hydrochloride is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for CI 966 hydrochloride

M. Wt 509.87
Formula C23H21F6NO3.HCl
Storage Desiccate at RT
Purity ≥98% (HPLC)
CAS Number 110283-66-4
PubChem ID 198692
InChI Key NUQWSOWKRTZJTO-UHFFFAOYSA-N
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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for CI 966 hydrochloride

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 100
ethanol 10

Preparing Stock Solutions for CI 966 hydrochloride

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

Select a batch to recalculate based on the batch molecular weight:
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 for CI 966 hydrochloride

References for CI 966 hydrochloride

References are publications that support the biological activity of the product.

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


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Citations for CI 966 hydrochloride

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

*Please note that Tocris will only send literature to established scientific business / institute addresses.


GABA Receptors Scientific Review

GABA Receptors Scientific Review

Written by Ian Martin, Norman Bowery and Susan Dunn, this review provides a history of the GABA receptor, as well as discussing the structure and function of the various subtypes and the clinical potential of receptor modulators; compounds available from Tocris are listed.

Addiction Poster

Addiction Poster

The key feature of drug addiction is the inability to stop using a drug despite clear evidence of harm. This poster describes the brain circuits associated with addiction, and provides an overview of the main classes of addictive drugs and the neurotransmitter systems that they target.