الصفحة الرئيسية>>Signaling Pathways>> Membrane Transporter/Ion Channel>> Calcium Channel>>TTA-Q6

TTA-Q6

رقم الكتالوجGC30950

TTA-Q6 هو مضاد انتقائي لقناة Ca2 + من النوع T ، والذي يمكن استخدامه في البحث عن الأمراض العصبية

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TTA-Q6 التركيب الكيميائي

Cas No.: 910484-28-5

الحجم السعر المخزون الكميّة
10mM (in 1mL DMSO)
168٫00
متوفر
5mg
153٫00
متوفر
10mg
266٫00
متوفر
25mg
510٫00
متوفر
50mg
783٫00
متوفر

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Sample solution is provided at 25 µL, 10mM.

Description of TTA-Q6

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.

Protocol of TTA-Q6

Animal experiment [1]:

Animal models

WAG/Rij epilepsy model SD rat

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.

Dosage form

10 mg/kg TTA-Q6 orally every day for 7 days

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.

Chemical Properties of TTA-Q6

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
الذوبان 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.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table of TTA-Q6

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
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In vivo Formulation Calculator (Clear solution) of TTA-Q6

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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.

Product Documents

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Average Rating: 5 ★★★★★ (Based on Reviews and 34 reference(s) in Google Scholar.)

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