TTA-Q6 |
| カタログ番号GC30950 |
TTA-Q6は、T型カルシウムチャネルの選択的アンタゴニストであり、神経研究に使用される。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 910484-28-5
Sample solution is provided at 25 µL, 10mM.
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TTA-Q6は、T型カルシウムチャネルの選択的アンタゴニストであり、神経研究に使用される。
TTA-Q6は優れた全体的なプロファイルを示し、T型カルシウムチャネルアンタゴニストに応答する複数のin vivoアッセイで検討された。経口投与で3 mg/kgの用量でWAG/Rijてんかんモデルの発作を強力に抑制した。ラットの睡眠期直前に10 mg/kgの用量を投与すると、投与後0.5〜2時間の間に活発な覚醒のさらなる抑制が観察された。また、TTA-Q6はアンフェタミン誘発性の精神運動活動を用量依存的に低減した。
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.
| 動物実験 [1]: | |
動物モデル | WAG/Rij てんかんモデル SD ラット |
準備方法 | T 型拮抗薬の睡眠と覚醒に対する効果を評価するために、ラットの皮質電気図 (ECoG) と筋電図 (EMG) 信号の遠隔記録を測定しました。7 日間のクロスオーバー設計で、賦形剤または TTA-Q6 を毎日、非活動期の 30 分前に経口投与しました。ECoG 信号と EMG 信号を収集し、覚醒時間または睡眠の各段階についてスコアを付けました。 |
投与形態 | 10 mg/kg TTA-Q6 を 7 日間毎日経口投与 |
アプリケーション | ラットの睡眠期間の直前に 10 mg/kg の TTA-Q6 を投与すると、投与後 0.5～2 時間、活動覚醒がさらに抑制されました。 |
参考文献: [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. | |
| 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 | ||
| Formula | C20H15ClF3N3O | M.Wt | 405.8 |
| 溶解度 | DMSO : 125 mg/mL (308.03 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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 |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 34 reference(s) in Google Scholar.)
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