842964-18-5
842964-18-5 structure
- Name: δ-secretase inhibitor 11
- Chemical Name: 7-Morpholin-4-yl-benzo[1,2,5]oxadiazol-4-ylamine
- CAS Number: 842964-18-5
- Molecular Formula: C10H12N4O2
- Molecular Weight: 220.22800
- Catalog: Signaling Pathways Apoptosis Caspase
- Create Date: 2017-07-05 15:49:57
- Modify Date: 2024-01-29 06:55:06
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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].
| Name | 7-Morpholin-4-yl-benzo[1,2,5]oxadiazol-4-ylamine |
|---|---|
| Synonyms |
7-(Methylthio)xanthone-3-carboxamide
9H-Xanthene-3-carboxamide,7-(methylthio)-9-oxo 7-(morpholin-4-yl)-2,1,3-benzoxadiazol-4-amine |
| Description | 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]. |
|---|---|
| Related Catalog | |
| Target |
Caspase-3:31.86 ± 1. μM (IC50) Caspase-8:86.71 ± 10 μM (IC50) |
| In Vitro | 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: 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. |
| References |
| Molecular Formula | C10H12N4O2 |
|---|---|
| Molecular Weight | 220.22800 |
| Exact Mass | 220.09600 |
| PSA | 77.41000 |
| LogP | 1.28780 |
| HS Code | 2934999090 |
|---|
| HS Code | 2934999090 |
|---|---|
| Summary | 2934999090. other heterocyclic compounds. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |