2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. TRP Channel
  4. TRPM2-IN-2

TRPM2-IN-2 is a potent and selective TRPM2 inhibitor (IC50 = 0.66 μM) with minimal activity against TRPM8 and TRPV1 (IC50 >10 μM). TRPM2-IN-2 exhibits robust neuroprotective effects in both in vitro oxygen-glucose deprivation/reperfusion (OGD/R) model and in vivo transient middle cerebral artery occlusion (tMCAO) mouse model. TRPM2-IN-2 can be used for ischemic stroke research.

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TRPM2-IN-2

TRPM2-IN-2 Chemical Structure

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TRPM2-IN-2 Related Antibodies

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Description

TRPM2-IN-2 is a potent and selective TRPM2 inhibitor (IC50 = 0.66 μM) with minimal activity against TRPM8 and TRPV1 (IC50 >10 μM). TRPM2-IN-2 exhibits robust neuroprotective effects in both in vitro oxygen-glucose deprivation/reperfusion (OGD/R) model and in vivo transient middle cerebral artery occlusion (tMCAO) mouse model. TRPM2-IN-2 can be used for ischemic stroke research[1].

IC50 & Target[1]

TRPM2

0.66 μM (IC50)

In Vitro

TRPM2-IN-2 (LC4) (0.03-10 μM, 6-24 h) shows protective effects of adamantane derivatives on an OGD/R cell model, with low cytotoxicity in SH-SY5Y cells[1].
TRPM2-IN-2 (10 μM) exhibits minimal inhibition activity against TRPV1 and TRPM8 with inhibition rates of 20.5% and 23.2%[1].
TRPM2-IN-2 inhibits hERG channel with an IC50 of 21.61 μM in CHO cells[1].

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

TRPM2-IN-2 Related Antibodies

Cell Viability Assay[1]

Cell Line: SH-SY5Y cells
Concentration: 0.03, 0.1, 0.3, 1, 3 and 10 μM
Incubation Time: 6 and 24 h
Result: Showed low cytotoxicity in SH-SY5Y cells at 10 μM.
Showed no significant cytotoxicity in SH-SY5Y cells up to 1 μM.
Exhibited significant protective effects against OGD/R-induced injury at 0.1 μM and notably maintaining protection even at 0.03 μM.
Did not exhibit significant cytotoxicity at its effective concentration (0.03-0.3 μM).
In Vivo

TRPM2-IN-2 (0.3, 1 and 3 mg/kg, i.v., single dose at 3 h post-reperfusion) shows significant neuroprotective effects in the tMCAO mouse model[1].

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

Animal Model: Male C57BL/6J mice (8-10 weeks) subjected to 1 h of ischemia followed by 3 h of reperfusion[1]
Dosage: 0.3, 1 and 3 mg/kg
Administration: i.v., single dose at 3 h post-reperfusion
Result: Significantly reduced infarct volume (35.7 %) compared with the vehicle group (60.9 %) at 3 mg/kg.
Exhibited comparable efficacy to 3 mg/kg of Edaravone (HY-B0099) at 1 mg/kg.
Did not show significant protection at 0.3 mg/kg.
Had significantly better outcomes than the vehicle at 3 mg/kg.
Showed no significant improvement compared with vehicle at 0.3 and 1 mg/kg.
significantly lowered levels of MDA (6.8 μM/mgprot) and LDH (0.18 U/mgprot).
Molecular Weight

391.51

Formula

C24H29N3O2
SMILES

O=C(N1CCCC1)C2=CC3=CC=CN3C(C(NC4(C[C@H]5C6)C[C@H]6C[C@H](C5)C4)=O)=C2
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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TRPM2-IN-2 Related Classifications

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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:

TRPM2-IN-2TRP ChannelTransient receptor potential channelsTRPM2neuroprotectiveOGD/RtMCAOischemic strokeInhibitorinhibitorinhibit

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