CI-966

CI-966 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 shows more than 200-fold selectivity over GAT-2, GAT-3, and BGT-3. CI-966 exhibits anticonvulsant and neuroprotective activities .


Cat. No.: EX-A10891	Purity: >98%

	Chemical structure of CI-966

For research only, Do not use for Human!

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CAS No.	110283-79-9
Purity	>98%
Formula	C23H21F6NO3
Mol Weight	473.4082
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Shipping	Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Reference:	[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. [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. [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. [4]. D M Grech, et al. Discriminative stimulus effects of presynaptic GABA agonists in pentobarbital-trained rats. Pharmacol Biochem Behav.1994 Jan;47(1):5-11. [5]. U Ebert, et al. 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. 1990 Sep;68(9):1194-9. [6]. L L Radulovic, et al. Pharmacokinetics, mass balance, and induction potential of a novel GABA uptake inhibitor, CI-966 HCl, in laboratory animals. Pharm Res. 1993 Oct;10(10):1442-5.
CoA	CoA of CI-966

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


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