1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel iGluR Calcium Channel
  3. TAT-EE3

TAT-EE3 is a neuroprotective peptide which can uncouple TRPM2-NMDARs interaction. TAT-EE3 inhibits TRPM2-induced enhancement of NMDAR surface expression and current amplitude.TAT-EE3 protects neurons against ischemic injury in vitro and in vivo. TAT-EE3can be used for the study of ischemic stroke.

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TAT-EE3

TAT-EE3 Chemical Structure

CAS No. : 2899218-49-4

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Based on 1 publication(s) in Google Scholar

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Description

TAT-EE3 is a neuroprotective peptide which can uncouple TRPM2-NMDARs interaction. TAT-EE3 inhibits TRPM2-induced enhancement of NMDAR surface expression and current amplitude.TAT-EE3 protects neurons against ischemic injury in vitro and in vivo. TAT-EE3can be used for the study of ischemic stroke[1].

In Vitro

TAT-EE3 (10 μM, overnight) disrupts the interaction between TRPM2 and GluN2a/GluN2b in HEK293T cells and neurons, inhibits TRPM2-induced enhancement of NMDAR surface expression and current amplitude[1].
TAT-EE3 (10 μM, overnight) reduces OGD-induced intracellular Ca2+ overload, neuronal death, and mitochondrial depolarization in wild-type neurons, but has no effect on gM2KO neurons[1].
TAT-EE3 (10 μM, 30-90 min) eliminates PMA-induced NMDAR current potentiation in wild-type neurons, without additional inhibition in gM2KO neurons[1].

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

In Vivo

AT-EE3 (0.33 mg/kg (100 nmol/kg), i.p., 15 min before middle cerebral artery occlusion (MCAO) or post-MCAO with reinjection every 12 h, 7 days) reduces infarct volume and improves neurological deficit score in wild-type mice, but shows no further protective effect in neuron-specific TRPM2 knockout (nM2KO) mice[1].

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

Animal Model: Focal cerebral ischemia models were constructed by performing right middle cerebral artery occlusion (MCAO) on 8-9 week-old male mice, with 120 minutes of occlusion followed by 24 hours of reperfusion, or 60 minutes of occlusion followed by 7 days of reperfusion[1]
Dosage: 0.33 mg/kg (100 nmol/kg)
Administration: i.p. repeated every 12 h after MCAO for 7 days
Result: Reduced infarct volume.
Inhibited MCAO-induced increase in NMDAR surface expression in wild-type mice, but did not exert further Protective effects in neuron-specific TRPM2 knockout (nM2KO) mice.
Improved long-term neurological deficit scores and rotarod test performance in mice.
Maintained the phosphorylation levels of ERK1/2 and CREB in the brain.
Molecular Weight

3339.61

Formula

C135H228N48O49S

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Glu-Glu-Asp-Thr-Asp-Ser-Ser-Glu-Glu-Met-Leu-Ala-Leu-Ala-Glu-Glu

Sequence Shortening

YGRKKRRQRRREEDTDSSEEMLALAEE

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Sealed storage, away from moisture

Powder -80°C 2 years
-20°C 1 year

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

H2O : 5.88 mg/mL (1.76 mM; ultrasonic and adjust pH to 9 with NH3·H2O)

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Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2994 mL 1.4972 mL 2.9944 mL
5 mM --- --- ---
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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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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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 (sealed storage, away from moisture). 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
H2O 1 mM 0.2994 mL 1.4972 mL 2.9944 mL 7.4859 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • 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.

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TAT-EE3
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