| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| Targets |
IC50: 0.26 μM (hGAT-1); 1.2 μM (rGAT-1); 297 μM (rGAT-2); 333 μM (hGAT-3); 1140 μM (rGAT-3); 300 μM (hBGT-3)[1]
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| ln Vitro |
The mechanism of action of CI-966 hydrochloride is to specifically block GABA reuptake in neurons and glial cells[4].
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| ln Vivo |
When given to PTZ-trained rats, CI-966 hydrochloride causes intermediate levels of Pentylenetetrazol (PTZ)-lever responding[4]. Gamma-aminobutyric acid activity in the CA1 pyramidal layer is enhanced in situ by CI-966 hydrochloride. Under urethane anesthesia, CI-966 hydrochloride is given systemically to Sprague-Dawley rats via intraperitoneal injection (5 mg/kg). A very varied but often considerable augmentation of the suppression of hippocampal population spikes by GABA administered by microiontophoresis in the CA1 region occurs twenty to thirty minutes after injection[5]. In a number of animal models, CI-966 hydrochloride demonstrates anticonvulsant characteristics. When fed 1.39 mg/kg, dogs absorb CI-966 hydrochloride orally with a tmax of 0.7 hours. Rats administered oral 5 mg/kg exhibit a mean tmax of 4.0 hours. After intravenous administration of identical dosages, the average elimination t1/2 for rats and dogs is 4.5 hours and 1.2 hours, respectively. In both species, CI-966 hydrochloride has 100% oral bioavailability[6].
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| Animal Protocol |
Animal/Disease Models: Eight male SD (Sprague-Dawley) rats[4]
Doses: 0.3-30 mg/kg Route of Administration: Injection IP in a volume of 1 mL/kg Experimental Results: Dose dependent decreases in rates of responding occurred following CI-966 administration. |
| 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.
[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. [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. |
| Molecular Formula |
C23H22CLF6NO3
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|---|---|
| Molecular Weight |
509.87
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| CAS # |
110283-66-4
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| Related CAS # |
CI-966;110283-79-9
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| SMILES |
FC(F)(F)C1C=CC(C(C2C=CC(C(F)(F)F)=CC=2)OCCN2CCC=C(C(O)=O)C2)=CC=1
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50 mg/mL (98.06 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.90 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9613 mL | 9.8064 mL | 19.6128 mL | |
| 5 mM | 0.3923 mL | 1.9613 mL | 3.9226 mL | |
| 10 mM | 0.1961 mL | 0.9806 mL | 1.9613 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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