1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. TRP Channel
  3. TAT-M2NX

TAT-M2NX (tatM2NX) is a selective inhibitor targeting human TRPM2 channels and exerts inhibitory effects on ischemic stroke. TAT-M2NX reduces H2O2-induced calcium influx via TRPM2 channels. After traumatic brain injury in mice, TAT-M2NX preserves hippocampal long-term potentiation, improves memory function, and reduces infarct volume after middle cerebral artery occlusion, but it shows no effect on female mice. TAT-M2NX can be used in studies related to traumatic brain injury and ischemic stroke.

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TAT-M2NX

TAT-M2NX Chemical Structure

CAS No. : 2126166-03-6

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Based on 1 publication(s) in Google Scholar

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Description

TAT-M2NX (tatM2NX) is a selective inhibitor targeting human TRPM2 channels and exerts inhibitory effects on ischemic stroke. TAT-M2NX reduces H2O2-induced calcium influx via TRPM2 channels. After traumatic brain injury in mice, TAT-M2NX preserves hippocampal long-term potentiation, improves memory function, and reduces infarct volume after middle cerebral artery occlusion, but it shows no effect on female mice. TAT-M2NX can be used in studies related to traumatic brain injury and ischemic stroke[1][2].

IC50 & Target

TRPM2

 

In Vitro

TAT-M2NX (25-100 μM; 2 h) inhibits human TRPM2 channels in a concentration-dependent manner, as measured by reduced H2O2-induced Ca2+ influx in TRPM2-expressing HEK-293 cells[2].

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

In Vivo

TAT-M2NX (0.2-20 mg/kg; i.v.; single dose at 2 hours after traumatic brain injury (TBI)) prevents TBI-induced memory impairment in male C57Bl/6 mice at doses of 2, 10 or 20 mg/kg, preserves hippocampal LTP in mice at 7 days post-TBI at doses of 2 or 10 mg/kg, and reduces brain lesion volume; the strongest beneficial effects are observed at the dose of 10 mg/kg[1].
TAT-M2NX (20 mg/kg; retro-orbital injection; single administration) exerts cerebral ischemia-specific neuroprotective effects in male mice: when administered prior to middle cerebral artery occlusion (MCAO), it reduces infarct volume[2].

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

Animal Model: C57Bl/6 (adult 2-4 month, male)[1]
Dosage: 0.2 mg/kg; 2 mg/kg; 10 mg/kg; 20 mg/kg
Administration: i.v.; single dose at 2 hours post-TBI
Result: Did not affect hippocampal LTP, with a normalized fEPSP slope of 129.9%, which was not significantly different from control-treated TBI mice.
Preserved hippocampal LTP, with a normalized fEPSP slope of 165.5%, and prevented TBI-induced memory impairment, with freezing behavior of 47.9%.
Preserved hippocampal LTP, with a normalized fEPSP slope of 186.9%, and prevented TBI-induced memory impairment, with freezing behavior of 52.1%.
Prevented TBI-induced memory impairment, with freezing behavior of 62.3%, which was equivalent to the effect of 10 mg/kg.
Animal Model: C57Bl/6 (young adult, 2-3 month old, male, wild-type; TRPM2−/− (young adult, 2-3 month old, male, knockout))[2]
Dosage: 20 mg/kg
Administration: retro-orbital; single dose (20 min prior to MCAO; 3 h after reperfusion)
Result: Reduced mean infarct volume to 29.2% in wild-type mice treated 20 min prior to MCAO. Reduced mean infarct volume to 28.3% (24 h post-reperfusion) and 23.8% (96 h post-reperfusion) in wild-type mice treated 3 h after reperfusion. Showed no further reduction in infarct volume (27.3%) in TRPM2−/− knockout mice compared to untreated TRPM2−/− knockout mice (27.3%).
Molecular Weight

4354.11

Formula

C190H323N71O45S

CAS No.
Appearance

Solid

Color

White to off-white

Sequence

Tyr-Gly-Arg-Lys-Lys-Arg-Arg-Gln-Arg-Arg-Arg-Gly-Ser-Arg-Glu-Pro-Gly-Glu-Met-Leu-Pro-Arg-Lys-Leu-Lys-Arg-Val-Leu-Arg-Gln-Glu-Phe-Trp-Val

Sequence Shortening

YGRKKRRQRRRGSREPGEMLPRKLKRVLRQEFWV

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 : 50 mg/mL (11.48 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 0.2297 mL 1.1483 mL 2.2967 mL
5 mM 0.0459 mL 0.2297 mL 0.4593 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 (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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Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Purity & Documentation

Purity: 99.55%

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 (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 0.2297 mL 1.1483 mL 2.2967 mL 5.7417 mL
5 mM 0.0459 mL 0.2297 mL 0.4593 mL 1.1483 mL
10 mM 0.0230 mL 0.1148 mL 0.2297 mL 0.5742 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-M2NX
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