2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. TTA-A2

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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TTA-A2 Chemical Structure

TTA-A2 Chemical Structure

CAS No. : 953778-63-7

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

TTA-A2 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE TTA-A2

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N-type calcium channel L-type calcium channel P/Q-type calcium channel T-type calcium channel Calcium Channel

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  • Purity & Documentation

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Description

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[1][2].

IC50 & Target

IC50: 98 nM ( α1I at membrane holding potentials of -80 mV)
IC50: 3.7 μM (α1I at membrane holding potentials of -100 mV)[1]
Cellular Effect
Cell Line Type Value Description References
HEK293 IC50
3.7 nM
Compound: 37, TTA-A2
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
[PMID: 21316226]
HEK293 IC50
98 nM
Compound: 37, TTA-A2
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
[PMID: 21316226]
In Vitro

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.

TTA-A2 Related Antibodies
In Vivo

TTA-A2 (oral gavage; 3 mg/kg; single dose) produces significant changes in sleep architecture in rats. A reduction in active wake soon after dosing with a concurrent increase in delta sleep and decrease in REM sleep. Additionally, these effects persists for up to 4 h post-dose in rats[1].
TTA-A2 (oral gavage; 10 mg/kg; once daily; 5 days) shows selective effect on recurrent thalamocortical network activity, it suppresses active wake and promotes slow-wave sleep in wild-type mice but not in mice lacking both Cav3.1 and Cav3.3[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Wild-type and double Cav3.1/Cav3.3 knockout C57BL6/Sv129 background mices[2]
Dosage: 10 mg/kg
Administration: Oral gavage; 10 mg/kg; once daily; 5 days
Result: Blocked active wake and promotes slow-wave sleep in wild-type mice but not mutant mice.
Molecular Weight

378.39

Formula

C20H21F3N2O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(N[C@@H](C1=NC=C(OCC(F)(F)F)C=C1)C)CC2=CC=C(C3CC3)C=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.6428 mL 13.2139 mL 26.4278 mL
5 mM 0.5286 mL 2.6428 mL 5.2856 mL
View the 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.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.61 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
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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Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
Purity & Documentation

Purity: ≥99.0%

SDS (251 KB)

COA (244 KB)

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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TTA-A2 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

TTA-A2953778-63-7Calcium ChannelCa2+ channelsCa channelsT-type calcium channelPregnane X receptorElectrocorticogramEpilepsyneurological diseasessleep disordersInhibitorinhibitorinhibit

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