110283-66-4
Chemical Structure
CI-966 hydrochloride
- CAS No.: 110283-66-4
- Formula:C23H22ClF6NO3
- Molecular Weight:509.87
IUPAC Name: 1-(2-(bis(4-(trifluoromethyl)phenyl)methoxy)ethyl)-1,2,5,6-tetrahydropyridine-3-carboxylic acid hydrochloride
InChIKey: NUQWSOWKRTZJTO-UHFFFAOYSA-N
SMILES: O=C(C1=CCCN(CCOC(C2=CC=C(C(F)(F)F)C=C2)C3=CC=C(C(F)(F)F)C=C3)C1)O.[H]Cl
Biological Activity: CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities[1][2][3].
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CI-966 hydrochloride | 99.60% | CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities. | ||||||||||||||||||||
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CI-966 hydrochloride (Standard) | ≥98% | CI-966 hydrochloride (Standard) is the analytical standard of CI-966 hydrochloride (HY-103534). This product is intended for research and analytical applications. CI-966 hydrochloride is a potent, selective, orally active and brain-penetrant inhibitor of the GABA transporter GAT-1, with IC50s of 0.26 μM and 1.2 μM for hGAT-1, rGAT-1, respectively. CI-966 hydrochloride shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 hydrochloride exhibits anticonvulsant and neuroprotective activities. | ||||||||||||||||||||
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References
- [1]. Borden LA, et, al. Tiagabine, SK&F 89976-A, CI-966, and NNC-711 are selective for the cloned GABA transporter GAT-1. Eur J Pharmacol. 1994 Oct 14;269(2):219-24. [Content Brief]
- [2]. Green AR, et, al. GABA potentiation: a logical pharmacological approach for the treatment of acute ischaemic stroke. Neuropharmacology. 2000 Jul 10;39(9):1483-94. [Content Brief]
- [3]. T G Dhar, 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 (IF: 7.45; Q1). 1994 Jul 22;37(15):2334-42. [Content Brief]
