BACE1-IN-1
Based on 1 Customer Validation
BACE1-IN-1 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 reduces cerebral Aβ40 levels in mice. BACE1-IN-1 can be used in studies related to Alzheimer's disease and type 2 diabetes.
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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。
- 純度 : 98.72%
- CAS 番号: 1310347-50-2
- 分子式: C18H14F3N5O2
- 分子量:389.33
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- プロトコル
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
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PF-06751979BACE1 Inhibitor -
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ElenbecestatBACE-1 Inhibitor -
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LY2811376 (Standard)Reference Standard -
HY-100182R
BACE1-IN-1 (Standard)Reference Standard -
HY-119689
UmibecestatBACE-1/2 Inhibitor -
HY-16759R
Verubecestat (Standard)BACE1/2 Inhibitor
生物活性
製品説明
IC50 & Target
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BACE1 23 nM (IC50) |
BACE2 24 nM (IC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK293 | IC50 |
0.021 μM
Compound: 14d
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Inhibition of human BACE1 in HEK293 cells transfected with wild type APP assessed as reduction of amyloid beta40 level after 18 to 20 hrs by AlphaLISA technique
Inhibition of human BACE1 in HEK293 cells transfected with wild type APP assessed as reduction of amyloid beta40 level after 18 to 20 hrs by AlphaLISA technique
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[PMID: 23590342] |
体外実験
BACE1-IN-1 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.
体内実験
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female C57Bl/6J wild-type mice[2]
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Dosage:10 mg/kg, 30 mg/kg
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Administration:Oral gavage (p.o.)
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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
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CAS 番号 1310347-50-2
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性状 Solid
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分子量 389.33
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分子式 C18H14F3N5O2
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Color White to off-white
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SMILES
O=C(C1=NC=C(C#N)C=C1)NC2=CC=C(F)C([C@@]3(C)N=C(N)OCC3(F)F)=C2
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
体外:
DMSO : 85 mg/mL (218.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMSO : 85 mg/mL (218.32 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
純度とドキュメンテーション
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データシート (295 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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取扱説明書 (2659 KB)
参考文献
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / DMSO | 1 mM | 2.5685 mL | 12.8426 mL | 25.6852 mL | 64.2129 mL |
| 5 mM | 0.5137 mL | 2.5685 mL | 5.1370 mL | 12.8426 mL | |
| 10 mM | 0.2569 mL | 1.2843 mL | 2.5685 mL | 6.4213 mL | |
| 15 mM | 0.1712 mL | 0.8562 mL | 1.7123 mL | 4.2809 mL | |
| 20 mM | 0.1284 mL | 0.6421 mL | 1.2843 mL | 3.2106 mL | |
| 25 mM | 0.1027 mL | 0.5137 mL | 1.0274 mL | 2.5685 mL | |
| 30 mM | 0.0856 mL | 0.4281 mL | 0.8562 mL | 2.1404 mL | |
| 40 mM | 0.0642 mL | 0.3211 mL | 0.6421 mL | 1.6053 mL | |
| 50 mM | 0.0514 mL | 0.2569 mL | 0.5137 mL | 1.2843 mL | |
| 60 mM | 0.0428 mL | 0.2140 mL | 0.4281 mL | 1.0702 mL | |
| 80 mM | 0.0321 mL | 0.1605 mL | 0.3211 mL | 0.8027 mL | |
| 100 mM | 0.0257 mL | 0.1284 mL | 0.2569 mL | 0.6421 mL |
BACE1-IN-1 関連分類
HY-100182 関連分類
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