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Biochem/physiol Actions
Compound 8 (C8) is a small molecule that directly targets TRPM4 TwinF domain and blocks its interaction with GluN2A/GluN2B (NR2A/NR2B) I4 domain. C8 prevents NMDAR/TRPM4 interaction-dependent excitotoxicity (death protection EC50 = 2.1 μM 24 h post 10-min exposure of primary murine hippocampal neurons to 20 μM NMDA) without affecting, and even enhancing, NMDAR-mediated essential functions. C8 protects mice from MCAO-induced brain damage and NMDA-induced retinal ganglion cell (RGC) loss in mice in vivo (40 mg/kg i.p. at -16h, -3h before, 0h, 3h, 24h after MCAO or 20 nmol NMDA/2.0 μL by intravitreal injection).
TRPM4 TwinF domain-targeting NMDAR/TRPM4 interaction blocker that protects against TRPM4-mediated excitotoxicity in vitro and in vivo.
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder or solid |
| storage condition | desiccated |
| color | white to beige |
| solubility | H2O: 2 mg/mL, clear |
| storage temp. | −20°C |
| SMILES string | NCCN(CC)CC1=CC=CC(Br)=C1.Cl.Cl |
| InChI | 1S/C11H17BrN2.2ClH/c1-2-14(7-6-13)9-10-4-3-5-11(12)8-10;;/h3-5,8H,2,6-7,9,13H2,1H3;2*1H |
| InChI key | AQDSZKTVQVSVNC-UHFFFAOYSA-N |
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