TTA-A2
Based on 1 publication(s) in Google Scholar
TTA-A2 is a potent, selective and orally active t-type voltage gated calcium channel antagonist with reduced pregnane X receptor (PXR) activation. TTA-A2 is equally potent against the Cav3.1 (a1G) and Cav3.2 (a1H) channels with IC50 values of 89 nM and 92 nM, respectively, at -80 and -100 mV holding potentials. TTA-A2 can be used for the research of a variety of human neurological diseases, including sleep disorders and epilepsy.
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- Purity: 99.33%
- CAS No.: 953778-63-7
- 화학식: C20H21F3N2O2
- 분자량:378.39
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보관:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) TTA-A2
MoreAll Calcium Channel Isoforms
More
Biological Activity
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T-type calcium channel |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
>10 μM
Compound: 4, TTA-A2
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Displacement of [3S]MK499 from human ERG in HEK293 cells
Displacement of [3S]MK499 from human ERG in HEK293 cells
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[PMID: 24900239] |
| HEK293 | IC50 |
3.7 nM
Compound: 37, TTA-A2
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Antagonist activity at Cav3.3 alpha1i expressed in HEK293 cells at -100 mV by standard voltage-clamp electrophysiology assay
Antagonist activity at Cav3.3 alpha1i expressed in HEK293 cells at -100 mV by standard voltage-clamp electrophysiology assay
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[PMID: 21316226] |
| HEK293 | IC50 |
98 nM
Compound: 37, TTA-A2
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Antagonist activity at Cav3.3 alpha1i expressed in HEK293 cells at -80 mV by standard voltage-clamp electrophysiology assay
Antagonist activity at Cav3.3 alpha1i expressed in HEK293 cells at -80 mV by standard voltage-clamp electrophysiology assay
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[PMID: 21316226] |
TTA-A2 exhibits a state-dependent inhibition of α1I with potencies of 98 nM and 3.7 μM at membrane holding potentials of -80 and -100 mV, respectively in astandard voltage-clamp electrophysiology assay. It also exhibits excellent selectivity against the Cav1.2 (L-type), Cav2.1 (P/Q-type), Cav2.2 (N-type), and Cav2.3 (R-type) channels which all had IC50 values of >30 μM at 80 mV[1].TTA-A2 exhibits high affinity in the α1I binding assay with a Ki of 1.2 nM and has excellent selectivity over the hERG potassium channel and L-type calcium channel (both IC50>10 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wild-type and double Cav3.1/Cav3.3 knockout C57BL6/Sv129 background mices[2]
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Dosage:10 mg/kg
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Administration:Oral gavage; 10 mg/kg; once daily; 5 days
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Result:Blocked active wake and promotes slow-wave sleep in wild-type mice but not mutant mice.
Chemical Information
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CAS No. 953778-63-7
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Appearance Solid
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분자량 378.39
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화학식 C20H21F3N2O2
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Color White to off-white
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SMILES
O=C(N[C@@H](C1=NC=C(OCC(F)(F)F)C=C1)C)CC2=CC=C(C3CC3)C=C2
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Cell Commun Signal
T-type voltage-gated channels, Na+/Ca2+-exchanger, and calpain-2 promote photoreceptor cell death in inherited retinal degeneration. [Abstract]2024 Feb 1;22(1):92. PMID: 38303059
용액&용해도
DMSO : 100 mg/mL (264.28 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 2.5 mg/mL (6.61 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.6428 mL | 13.2139 mL | 26.4278 mL | 66.0694 mL |
| 5 mM | 0.5286 mL | 2.6428 mL | 5.2856 mL | 13.2139 mL | |
| 10 mM | 0.2643 mL | 1.3214 mL | 2.6428 mL | 6.6069 mL | |
| 15 mM | 0.1762 mL | 0.8809 mL | 1.7619 mL | 4.4046 mL | |
| 20 mM | 0.1321 mL | 0.6607 mL | 1.3214 mL | 3.3035 mL | |
| 25 mM | 0.1057 mL | 0.5286 mL | 1.0571 mL | 2.6428 mL | |
| 30 mM | 0.0881 mL | 0.4405 mL | 0.8809 mL | 2.2023 mL | |
| 40 mM | 0.0661 mL | 0.3303 mL | 0.6607 mL | 1.6517 mL | |
| 50 mM | 0.0529 mL | 0.2643 mL | 0.5286 mL | 1.3214 mL | |
| 60 mM | 0.0440 mL | 0.2202 mL | 0.4405 mL | 1.1012 mL | |
| 80 mM | 0.0330 mL | 0.1652 mL | 0.3303 mL | 0.8259 mL | |
| 100 mM | 0.0264 mL | 0.1321 mL | 0.2643 mL | 0.6607 mL |
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