WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H524733
CAS#: 110283-79-9
Description: CI-966 is a central nervous system depressant acting as a GABA reuptake inhibitor, specifically a highly potent and selective blocker of the GABA transporter 1 (GAT-1) (IC50 = 0.26 µM). It has potential as an anticonvulsant, anxiolytic, and neuroprotective therapeutic agent. In a phase I human clinical trial it was developed for the treatment of epilepsy.
Hodoodo Cat#: H524733
Name: CI-966
CAS#: 110283-79-9
Chemical Formula: C23H22ClF6NO3
Exact Mass: 0.00
Molecular Weight: 509.870
Elemental Analysis: C, 54.18; H, 4.35; Cl, 6.95; F, 22.36; N, 2.75; O, 9.41
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Synonym: CI-966; CI 966; CI966; CHEMBL77287; CHEMBL542207.
IUPAC/Chemical Name: 1-(2-(Bis(4-(trifluoromethyl)phenyl)methoxy)ethyl)-1,2,5,6-tetrahydro-3-pyridinecarboxylic acid hydrochloride
InChi Key: NUQWSOWKRTZJTO-UHFFFAOYSA-N
InChi Code: InChI=1S/C23H21F6NO3.ClH/c24-22(25,26)18-7-3-15(4-8-18)20(16-5-9-19(10-6-16)23(27,28)29)33-13-12-30-11-1-2-17(14-30)21(31)32;/h2-10,20H,1,11-14H2,(H,31,32);1H
SMILES Code: C1C(=CCC[N@@]1CCOC(c1ccc(cc1)C(F)(F)F)c1ccc(cc1)C(F)(F)F)C(=O)O.Cl
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO, not in water
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
More Info:
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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.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
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1: Phillis JW. CI-966, a GABA uptake inhibitor, antagonizes ischemia-induced neuronal degeneration in the gerbil. Gen Pharmacol. 1995 Sep;26(5):1061-4. PubMed PMID: 7557251.
2: Green AR, Hainsworth AH, Jackson DM. GABA potentiation: a logical pharmacological approach for the treatment of acute ischaemic stroke. Neuropharmacology. 2000 Jul 10;39(9):1483-94. Review. PubMed PMID: 10854894.
3: Dhar TG, Borden LA, Tyagarajan S, Smith KE, Branchek TA, Weinshank RL, Gluchowski C. 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. 1994 Jul 22;37(15):2334-42. PubMed PMID: 8057281.
4: Borden LA, Dhar TG, Smith KE, Branchek TA, Gluchowski C, Weinshank RL. Cloning of the human homologue of the GABA transporter GAT-3 and identification of a novel inhibitor with selectivity for this site. Receptors Channels. 1994;2(3):207-13. PubMed PMID: 7874447.
5: Radulovic LL, Bockbrader HN, Chang T. 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. PubMed PMID: 8272405.
6: Ebert U, Krnjević K. 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. PubMed PMID: 2276082.
