TTA-Q6
目录号 : GC30950
TTA-Q6是T型Ca2+通道的选择性拮抗剂，可用于神经学研究。
Cas No.:910484-28-5
Sample solution is provided at 25 µL, 10mM.
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TTA-Q6 is a selective antagonist of T-type Ca2+ channel and can be used in neurological research[1].
TTA-Q6 displayed good overall profiles and were examined in several in vivo assays responsive to T-type calcium channel antagonists. It showed robust inhibition of seizures in the WAG/Rij epilepsy model after oral dosing at 3 mg/kg. A 10 mg/kg dose of TTA-Q6 to rats right before their sleep period produced a further suppression of active wake for 0.5-2 h after dosing[2]. TTA-Q6 dose-dependently reduced amphetamine-induced psychomotor activity[3].
References:
[1]: Schlegel KA, Yang ZQ, et,al.Discovery and expanded SAR of 4,4-disubstituted quinazolin-2-ones as potent T-type calcium channel antagonists. Bioorg Med Chem Lett. 2010 Sep 1;20(17):5147-52. doi: 10.1016/j.bmcl.2010.07.010. Epub 2010 Jul 8. PMID: 20673719.
[2]: Barrow JC, Rittle KE, et,al. Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists. ACS Med Chem Lett. 2010 Feb 1;1(2):75-9. doi: 10.1021/ml100004r. PMID: 24900180; PMCID: PMC4007971.
[3]: Uslaner JM, Smith SM, et,al. T-type calcium channel antagonism produces antipsychotic-like effects and reduces stimulant-induced glutamate release in the nucleus accumbens of rats. Neuropharmacology. 2012 Mar;62(3):1413-21. doi: 10.1016/j.neuropharm.2010.11.015. Epub 2010 Nov 24. PMID: 21110986.
TTA-Q6是T型Ca2+通道的选择性拮抗剂，可用于神经学研究[1]。
TTA-Q6 显示出良好的整体特征，并在几种对 T 型钙通道拮抗剂有反应的体内试验中进行了检查。在 WAG/Rij 癫痫模型中，口服给药 3 mg/kg 后，它显示出对癫痫发作的强烈抑制作用。在大鼠睡眠期前给予 10 mg/kg 剂量的 TTA-Q6 会在给药后 0.5-2 小时进一步抑制主动觉醒[2]。 TTA-Q6 剂量依赖性地降低苯丙胺诱导的精神运动活动[3]。
| Animal experiment [1]: | |
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Animal models |
WAG/Rij epilepsy model SD rat |
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Preparation Method |
To evaluate the effects of T-type antagonists on sleep and wake, telemetric recordings of electrocorticogram (ECoG) and electromyogram (EMG) signals were measured in rats. In a 7 day crossover design, vehicle or TTA-Q6 was dosed orally every day, 30 min before the inactive phase. The ECoG and EMG signals were collected and scored for the amount of time awake or each phase of sleep. |
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Dosage form |
10 mg/kg TTA-Q6 orally every day for 7 days |
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Applications |
A 10 mg/kg dose of TTA-Q6 to rats right before their sleep period produced a further suppression of active wake for 0.5~2 h after dosing. |
|
References: [1]. Barrow JC, Rittle KE, et,al. Discovery of 4,4-Disubstituted Quinazolin-2-ones as T-Type Calcium Channel Antagonists. ACS Med Chem Lett. 2010 Feb 1;1(2):75-9. doi: 10.1021/ml100004r. PMID: 24900180; PMCID: PMC4007971. |
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| Cas No. | 910484-28-5 | SDF | |
| Canonical SMILES | N#CC1=CC=C([C@]2(C3CC3)N(CC(F)(F)F)C(NC4=C2C=C(Cl)C=C4)=O)C=C1 | ||
| 分子式 | C20H15ClF3N3O | 分子量 | 405.8 |
| 溶解度 | DMSO : 125 mg/mL (308.03 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.4643 mL | 12.3213 mL | 24.6427 mL |
| 5 mM | 0.4929 mL | 2.4643 mL | 4.9285 mL |
| 10 mM | 0.2464 mL | 1.2321 mL | 2.4643 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet