δ-Secretase inhibitor 11 |
| Katalog-Nr.GC66048 |
δ-Secretase-Inhibitor 11 (Verbindung 11) ist ein oral aktiver, potenter, BHS-penetrierter, nicht toxischer, selektiver und spezifischer ⋴-Secretase-Inhibitor mit einem IC50 von 0,7 μM. δ-Secretase-Inhibitor 11 interagiert sowohl mit dem aktiven Zentrum als auch mit dem allosterischen Zentrum von δ-Secretase. δ-Secretase Inhibitor 11 schwÄcht die Spaltung von Tau und APP (Amyloid Precursor Protein) ab. δ-Secretase-Inhibitor 11 verbessert synaptische Dysfunktion und kognitive BeeintrÄchtigungen in transgenen Mausmodellen mit Tau P301S und 5XFAD. δ-Secretase Inhibitor 11 kann fÜr die Erforschung der Alzheimer-Krankheit verwendet werden.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 842964-18-5
Sample solution is provided at 25 µL, 10mM.
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δ-Secretase inhibitor 11 (compound 11) is an orally active, potent, BBB-penetrated, non-toxic, selective and specific δ-secretase inhibitor, with an IC50 of 0.7 μM. δ-Secretase inhibitor 11 interacts with both the active site and allosteric site of δ-secretase. δ-Secretase inhibitor 11 attenuates tau and APP (amyloid precursor protein) cleavage. δ-Secretase inhibitor 11 ameliorates synaptic dysfunction and cognitive impairments in tau P301S and 5XFAD transgenic mouse models. δ-Secretase inhibitor 11 can be used for Alzheimer's disease research[1].
δ-Secretase inhibitor 11 (compound 11) (0-1 μM, 10 min) inhibits δ-secretase in a concentration- and time-dependent manner[1].
δ-Secretase inhibitor 11 (0-1 μM) selectively blocks tau and APP (amyloid precursor protein) fragmentation by δ-secretase[1].
δ-Secretase inhibitor 11 (compound 11) (10 mg/kg, Orally, once daily for 3 months) attenuates neuronal injury induced by OGD (oxygen-glucose deprivation), and specifically exerts neuroprotective actions[1].
δ-Secretase inhibitor 11 (0-10 mg/kg, Orally, once daily for 1.5 and 3 months) inhibits δ-secretase activity, attenuates Aβ deposition and cognitive deficits in 5XFAD mouse model[1].
| Animal Model: | Tau P301S transgenic mice (n=4 mice per group)[1] |
| Dosage: | 10 mg/kg |
| Administration: | Orally, once daily for 3 months |
| Result: | Significantly inhibited the activity of δ-secretase in both wild-type and tau P301S mice brain, increased PP2A activity, and attenuated the truncation and phosphorylation of tau in tau P301S mice. Ameliorated synaptic loss and restored synaptic dysfunction in tau P301S mice. |
| Animal Model: | 5XFAD mice[1] |
| Dosage: | 2, 5 or 10 mg kg |
| Administration: | Orally, once daily for 1.5 and 3 months |
| Result: | Attenuated the β-secretase-mediated processing of APP, significantly decreased the concentrations of Aβ 1-40 and Aβ 1-42 in the brain lysates, and attenuated Aβ deposition in a time- and dose-dependent manner. |
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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