δ-Secretase inhibitor 11 |
| Catalog No.GC66048 |
δ-세크레타제 억제제 11(화합물 11)은 경구 활성, 강력, BBB 침투성, 무독성, 선택적 및 특이성 δ-세크레타제 억제제, IC50 0.7 μM. 821d96072c2d58d8970e76f526b0f6b8δ-세크레타제 억제제 11은 δ-세크레타제의 활성 부위 및 알로스테릭 부위 모두와 상호작용한다. 821d96072c2d58d8970e76f526b0f6b8δ-세크레타제 억제제 11은 타우 및 APP(아밀로이드 전구체 단백질) 절단을 약화시킵니다. 821d96072c2d58d8970e76f526b0f6b8δ- 세크레타제 억제제 11은 tau P301S 및 5XFAD 트랜스제닉 마우스 모델에서 시냅스 기능 장애 및 인지 장애를 개선합니다. 821d96072c2d58d8970e76f526b0f6b8δ-Secretase 억제제 11은 알츠하이머병 연구에 사용할 수 있습니다.821d96072c2d58d8970e76f526b0f6b8
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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