CI-966 hydrochloride|cas:110283-66-4|西域试剂

CI-966 hydrochloride,99.0%

产品编号：Bellancom-103534| CAS NO：110283-66-4| 分子式：C₂₃H₂₂ClF₆NO₃| 分子量：509.87

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货号	价格	库存与货期
Bellancom-103534	￥1300.00	杭州北京（现货）
Bellancom-103534	￥2100.00	杭州北京（现货）
Bellancom-103534	￥6900.00	杭州北京（现货）
Bellancom-103534	￥11000.00	杭州北京（现货）

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CI-966 hydrochloride

产品介绍

CI-966 hydrochloride 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-1 和 rGAT-1 的 IC₅₀ 分别为 0.26 μM 和 1.2 μM。CI-966 hydrochloride 对 GAT-1 的选择性比 GAT-2，GAT-3 和 BGT-3 高 200 倍以上。CI-966 hydrochloride 具有抗惊厥和神经保护活性。

生物活性

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.

体外研究

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

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

体内研究

CI-966 hydrochloride produces intermediate levels of Pentylenetetrazol (PTZ)-lever responding when administered to PTZ-trained rats^[4].
CI-966 hydrochloride enhances gamma-aminobutyric acid action in CA1 pyramidal layer in situ. CI-966 hydrochloride 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 hydrochloride exhibits anticonvulsant properties in various animal models. Oral absorption of CI-966 hydrochloride in dogs given 1.39 mg/kg is rapid with a t_max of 0.7 hr. In rats given 5 mg/kg oral, a mean t_max of 4.0 hr is observed. Following i.v. administration of the same respective doses, elimination t_1/2 in dogs and rats averages 1.2 and 4.5 hr. Absolute oral bioavailability of CI-966 hydrochloride is 100% in both species^[6].

西域 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.

体内研究

西域 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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 50 mg/mL (98.06 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	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

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.90 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.90 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (4.90 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (4.90 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在西域网站选购。

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

参考文献

. 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]

. 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]

. 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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

[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. [Content Brief]

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CI-966 hydrochloride,99.0%

CI-966 hydrochloride

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