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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- Fòrmula: C24H29N3O2
- Peso molecular:391.51
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
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.
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Cell Line:SH-SY5Y cells
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Concentration:0.03, 0.1, 0.3, 1, 3 and 10 μM
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Incubation Time:6 and 24 h
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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).
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57BL/6J mice (8-10 weeks) subjected to 1 h of ischemia followed by 3 h of reperfusion[1]
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Dosage:0.3, 1 and 3 mg/kg
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Administration:i.v., single dose at 3 h post-reperfusion
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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).
Chemical Information
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Peso molecular 391.51
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Fòrmula C24H29N3O2
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SMILES
O=C(N1CCCC1)C2=CC3=CC=CN3C(C(NC4(C[C@H]5C6)C[C@H]6C[C@H](C5)C4)=O)=C2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
TRPM2-IN-2 Related Classifications
HY-178393 Related Classifications
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