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NMDAR/TRPM4-IN-2

SKU: orb1744757

Description

NMDAR/TRPM4-IN-2 is a potent, small-molecule interfacial inhibitor that disrupts the NMDAR/TRPM4 complex. It demonstrates significant neuroprotective efficacy in models of ischemic stroke (MCAO) and excitotoxicity, protecting against brain damage, retinal ganglion cell loss, and hippocampal neuronal cell death and mitochondrial dysfunction in vitro with an IC50 of 2.1 µM.

Research Area

Neuroscience, Pharmacology & Drug Discovery, Signal Transduction

Images & Validation

Key Properties

CAS Number2243506-33-2
MW330.092
Purity99.75%
FormulaC11H19BrCl2N2
SMILESCl.Cl.CCN(CCN)Cc1cccc(Br)c1
TargetTRP/TRPV Channel,NMDAR,ERK,iGluR
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:4 mg/mL (12.12 mM);DMSO:112.5 mg/mL (340.81 mM);H2O:90 mg/mL (272.65 mM)

Bioactivity

In Vitro
NMDAR/TRPM4-IN-2, also referred to as compound 8 within the concentration range of 0-10 μM, interrupts the interactions between GluN2A and GluN2B with TRPM4 in a dose-dependent fashion. Through its action, it abolishes the CREB shutdown pathway, concurrently reactivating the ERK1/2 pathway and stimulating IEG induction, while preserving the NMDARs' inherent ability to drive synaptic activity-led transcription enhancement.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

ERK, iGluR, NMDA receptor, TRPVChannel, TRPV Channel, TRPChannel, TRPM4, TRP Channel
Quality Guarantee

Quality Guarantee

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Key Properties

No computed properties available.

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Protocol Information

NMDAR/TRPM4-IN-2 (orb1744757)

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Available Sizes

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5 mg
¥ 1,040.00
1 ml x 10 mM (in DMSO)
¥ 1,170.00
10 mg
¥ 1,300.00
25 mg
¥ 1,820.00
50 mg
¥ 2,470.00
100 mg
¥ 3,380.00
DispatchUsually dispatched within 3-5 working days
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