2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Calcium Channel
  4. TTA-P2

TTA-P2  (Synonyms: T-Type calcium channel inhibitor)

Cat. No.: HY-10035 Purity: 99.58% ee.: 100.00%
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TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy< sup>[4].

For research use only. We do not sell to patients.

TTA-P2 Chemical Structure

TTA-P2 Chemical Structure

CAS No. : 1072018-68-8

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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Based on 3 publication(s) in Google Scholar

Other Forms of TTA-P2:

TTA-P2 Related Antibodies

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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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Description

TTA-P2 (T-Type calcium channel inhibitor) is a selective, orally active, and BBB-penetrant T-type calcium channel blocker (IC50 = 22 nM). TTA-P2 reduces mechanical hypersensitivity and alleviates acute as well as chronic pain. TTA-P2 significantly reduces firing rates in temporal lobe epilepsy (TLE) neurons to control levels and suppresses synaptically evoked burst firing. TTA-P2 can be studied in research for neurological diseases such as tremor and absence epilepsy[1][2][3]< sup>[4][5].

IC50 & Target

T-type calcium channel

 

Cav3.2

 

In Vitro

TTA-P2 (1-10 μM) inhibits most of the T current recorded at the holding potentials of -90 mV, and the inhibitory effect has a fast onset but was slowly and partially reversible in dorsal root ganglion (DRG) cells[2].
TTA-P2 (3 μM, 10 min) has maximal effect within 3-4 min after application[3].
TTA-P2 (1 μM, 70 min) fully recovers the window component of the T-type Ca2+ current (IT) after 50 min of wash out in ventrobasal nucleus (VB) thalamocortical (TC) neurons[3].
TTA-P2 (1 nM-1 μM) blocks IT dose-dependently with an IC50 of 22 nM in VB TC neurons [3].
TTA-P2 (1 μM, 20 min) induces a maximal reduction of IT even in the absence of channel activation, indicating the absence of a use-dependent block in VB TC neurons [3].
TTA-P2 (25 nM, 20 min) induces a clear decrease in current amplitude with no apparent shift in the voltage dependence of channel activation and steady-state inactivation in VB TC neurons [3].
TTA-P2 (1 μM) decreases the amplitude of IT recorded in rat nucleus reticularis thalami (NRT) neurons, whereas the high-voltage-activated (HVA) Ca2+ current in the same neurons is not affected[3].

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

TTA-P2 Related Antibodies
In Vivo

TTA-P2 (0.3-10 mg/kg, i.p., single dose) has no effects on the mechanical threshold at 0.3 mg/kg, while increases the mechanical threshold to 17 g at 1 mg/kg, to 19 g at 3 mg/kg, and to 26 g at 10 mg/kg in rat models using Von Frey testing starting at 4 g[1].
TTA-P2 (5-7.5 mg/kg, i.p., single dose) significantly reduces licking and biting of the affected paws injected with formalin at 7.5 mg/kg in CaV3.2 knockout mice[2].
TTA-P2 (5-10 mg/kg, i.p., single dose) allows complete reversal of neuropathic hyperalgesia at 10 mg/kg in diabetic Streptozocin (HY-13753)-treated rats[2].
TTA-P2 (1-10 mg/kg, p.o., single dose) exhibits a dose- and exposure-dependent decrease in the total seizure time during the 4 h period following oral dosing, demonstrating robust CNS efficacy at 10 mg/kg with a plasma level of 1 μM in WAG/Rij rat model of absence epilepsy and significantly reduces tremor activity in a dose-dependent manner in rat harmaline model[5].
TTA-P2 (1.29-4.30 (mg/kg)/60 min, i.v. infusion) has no significant impact in mean arterial blood pressure, heart rate or ECG intervals in dog models[5].

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

Animal Model: Sprague Dawley rats (males and females, 300–350 g) with spinal cord injury[1]
Dosage: 0.3, 1, 3, 10 mg/kg, one single dose
Administration: Intraperitoneal injection (i.p.), single dose
Result: Had no effects on the mechanical threshold both at 30 min and 1-hour post-injection.
Reduced the mechanical hypersensitivity that developed following spinal cord injury in male rats.
Induced a robust conditioned place preference (CPP) with an increase in the difference score in the TTA-P2-paired chamber of 62 s and a decrease in the vehicle-paired chamber of -39 s.
Showed that the spontaneous ongoing pain following SCI is sensitive to TTA-P2 in male rats.
Increased the mechanical threshold to 16 g at 30 min post-injection and to 18 g at 1-hour post-injection in female rats with 10 mg/kg dose.
Were effective in reducing the mechanical hypersensitivity that developed following spinal cord injury in both male and female rats.
Had small effects with an increase in the difference score in the TTA-P2-paired chamber of 36 s and a decrease in the vehicle-paired chamber of -25 s.
Showed that the spontaneous ongoing pain following SCI has little or no sensitivity to TTA-P2 in female rats.
Molecular Weight

431.37

Formula

C21H29Cl2FN2O2
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

CC(C)(OCC1)C[C@H]1CN2CCC(F)(CC2)CNC(C3=CC(Cl)=CC(Cl)=C3)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 25 mg/mL (57.95 mM; ultrasonic and warming and heat to 60°C; 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 2.3182 mL 11.5910 mL 23.1820 mL
5 mM 0.4636 mL 2.3182 mL 4.6364 mL
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* 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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Purity & Documentation
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 2.3182 mL 11.5910 mL 23.1820 mL 57.9549 mL
5 mM 0.4636 mL 2.3182 mL 4.6364 mL 11.5910 mL
10 mM 0.2318 mL 1.1591 mL 2.3182 mL 5.7955 mL
15 mM 0.1545 mL 0.7727 mL 1.5455 mL 3.8637 mL
20 mM 0.1159 mL 0.5795 mL 1.1591 mL 2.8977 mL
25 mM 0.0927 mL 0.4636 mL 0.9273 mL 2.3182 mL
30 mM 0.0773 mL 0.3864 mL 0.7727 mL 1.9318 mL
40 mM 0.0580 mL 0.2898 mL 0.5795 mL 1.4489 mL
50 mM 0.0464 mL 0.2318 mL 0.4636 mL 1.1591 mL
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TTA-P2 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-P21072018-68-8T-Type calcium channel inhibitorCalcium ChannelCa2+ channelsCa channelsT-Type calcium channelCNST-type currentscerebellar nuclear neuronsneurologicalneuronsmechanical hypersensitivitypainInhibitorinhibitorinhibit

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