Bioactivity | 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]. |
Invitro | 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]. |
In Vivo | 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: |
Name | δ-Secretase inhibitor 11 |
CAS | 842964-18-5 |
Formula | C10H12N4O2 |
Molar Mass | 220.23 |
Appearance | Solid |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
Reference | [1]. Zhang Z, et al. Inhibition of delta-secretase improves cognitive functions in mouse models of Alzheimer's disease. Nat Commun. 2017 Mar 27;8:14740. |