BACE1-IN-1 hydrochloride
BACE1-IN-1 hydrochloride is an orally active, blood-brain barrier penetrant dual-target inhibitor of BACE1/2, with IC50 values of 23 nM and 24 nM against human BACE1 and BACE2, respectively. BACE1-IN-1 hydrochloride reduces cerebral Aβ40 levels in mice. BACE1-IN-1 hydrochloride can be used in studies related to Alzheimer's disease and type 2 diabetes.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 1310349-35-9
- 分子式: C18H15ClF3N5O2
- 分子量:425.79
-
保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
|
BACE1 23 nM (IC50) |
BACE2 24 nM (IC50) |
体外実験
BACE1-IN-1 hydrochloride inhibits Aβ40 production in HEK293 cells with an IC50 of 0.018-0.021 μM; it exhibits an enzymatic IC50 of 0.023 μM against hBACE1, an enzymatic IC50 of 0.024 μM against hBACE2, and an IC50 of 0.074 μM for inhibiting BACE2 in INS-TMEM27 cells[1][2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:Female C57Bl/6J wild-type mice[2]
-
Dosage:10 mg/kg, 30 mg/kg
-
Administration:Oral gavage (p.o.)
-
Result:Animals were sacrificed 4 hours after administration, and brain tissue was taken to detect Aβ40 levels.
Brain Aβ40 decreased by 78% in the 10 mg/kg group.
Brain Aβ40 decreased by 84% in the 30 mg/kg group.
化学情報
-
CAS 番号 1310349-35-9
-
分子量 425.79
-
分子式 C18H15ClF3N5O2
-
SMILES
C[C@]1(C(F)(COC(N)=N1)F)C2=CC(NC(C3=CC=C(C=N3)C#N)=O)=CC=C2F.Cl
-
輸送条件
Room temperature in continental US; may vary elsewhere.
-
保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
-
Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
-
Research Protocol for Metabolic Diseases
AMP-activated protein kinase, AMPK, is a conserved cellular energy sensor that responds to reduced cellular energy status and coordinates metabolism by increasing ATP-generating catabolic pathways while suppressing ATP-consuming anabolic processes. In metabolic disease research, the AMPK pathway is experimentally relevant because it regulates hepatic lipid synthesis, fatty acid oxidation, glucose production, skeletal-muscle glucose disposal, mTORC1-linked biosynthesis, autophagy, mitochondrial homeostasis, and whole-body energy balance. The central pathway logic is that energy stress, metformin, exercise-like stimulation, or direct AMPK activators increase AMPKα Thr172 phosphorylation and downstream substrate phosphorylation, including ACC and RAPTOR. Phosphorylation of ACC suppresses lipogenesis and supports fatty acid oxidation, whereas phosphorylation of RAPTOR suppresses mTORC1 signaling and links cellular energy status to growth and protein synthesis control. The pathway is linked
-
Alzheimer’s Disease Modeling
Alzheimer’s Disease (AD) is a neurodegenerative disorder characterized by a progressive decline in cognitive functions and loss of specific types of neurons and synapses. Alzheimer's symptoms can be simulated in mice by injecting drugs (such as Aβ) or genetically modified.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)