1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. CI-966

CI-966 是一种有效,选择性,具有口服活性和可透过血脑屏障的 GABA 转运蛋白 GAT-1 抑制剂,抑制 hGAT-1rGAT-1IC50 分别为 0.26 μM 和 1.2 μM。CI-966 对 GAT-1 的选择性比 GAT-2,GAT-3 和 BGT-3 高 200 倍以上。CI-966 具有抗惊厥和神经保护活性。

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CI-966 Chemical Structure

CI-966 Chemical Structure

CAS No. : 110283-79-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1][2][3].

IC50 & Target

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]

体外研究
(In Vitro)

CI-966 functions by selectively inhibiting GABA reuptake in neurons and glial cells[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

CI-966 produces intermediate levels of Pentylenetetrazol (PTZ)-lever responding when administered to PTZ-trained rats[4].
CI-966 enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ. CI-966 is administered systemically by i.p. injection (5 mg/kg) in Sprague-Dawley rats under urethane anaesthesia. Twenty to thirty minutes after injection there is a highly variable, but overall significant, enhancement of the inhibition of hippocampal population spikes by GABA applied by microiontophoresis in the CA1 region[5].
CI-966 exhibits anticonvulsant properties in various animal models. Oral absorption of CI-966 in dogs given 1.39 mg/kg is rapid with a tmax of 0.7 hr. In rats given 5 mg/kg oral, a mean tmax of 4.0 hr is observed. Following i.v. administration of the same respective doses, elimination t1/2 in dogs and rats averages 1.2 and 4.5 hr. Absolute oral bioavailability of CI-966 is 100% in both species[6].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Eight male Sprague-Dawley rats[4]
Dosage: 0.3-30 mg/kg
Administration: Injection IP in a volume of 1 mL/kg
Result: Dose dependent decreases in rates of responding occurred following CI-966 administration.
分子量

473.41

Formula

C23H21F6NO3

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

纯度 & 产品资料
参考文献
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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