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CRAC Channel Inhibitor IV, EVP4593
N4-(4-phenoxyphenethyl)quinazoline-4,6-diamine, SOC Inhibitor
A cell-permeable quinazoline derivative that blocks PMA/PHA-induced NF-κB activation in Jurkat cells (IC50 = 11 nM), but has no effect on PKC kinase, and exhibits an anti-inflammatory effect on carrageenin-induced paw edema in rats (1 mg/kg, i.p.). In addition, it is shown to inhibit the store-operated calcium entry (SOC) pathway possibly by targeting TRPC1 containing heteromeric channels in Huntington Disease (HD) neurons (SK-N-SH cells transfected with mutant Huntingtin Htt-138Q) at 300 nM. It displays neuroprotective effects in YAC128 MSN mice neurons from glutamate toxicity dose-dependently from 30 nM to 3 µM, which is consistent with TRPC1 knockdown effects, and attenuates the progressive decline in the climbing speed of the HD Drosophila, dose-dependently from 100 µM to 400 µM.
产品信息
Form Yellow powder
Molar mass 356.42
Protect from Light 是的
Packaged under inert gas 是的
Purity ≥98% by HPLC
Solubility DMSO
Chemical formula C22H20N4O
商店和运输信息
Storage +2°C to +8°C
Ship Ambient Temperature Only
Regulatory Review |