Bavarostat
Based on 1 Customer Validation
Bavarostat (EKZ-001) is a blood-brain barrier-permeable, potent HDAC6 inhibitor and PET radiotracer, with an IC50 as low as 17 nM against human HDAC6. Bavarostat can be labeled with 18F and used as a probe to map HDAC6 distribution and measure target occupancy in the brains of non-human primates. Bavarostat also selectively modulates tubulin acetylation, but not histone acetylation. Bavarostat is applicable for research on Alzheimer's disease, other neurodegenerative disorders, and cancers.
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。
- 純度: 99.51%
- CAS 番号: 2134109-20-7
- 分子式: C20H27FN2O2
- 分子量:346.44
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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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
- 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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Cell Cycle/DNA Damage Compound Library
HY-L004
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Epigenetics Compound Library
HY-L005
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Histone Modification Research Compound Library
HY-L024
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Anti-Cancer Compound Library
HY-L025
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CNS-Penetrant Compound Library
HY-L028
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Anti-Aging Compound Library
HY-L034
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Reprogramming Compound Library
HY-L039
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Oxygen Sensing Compound Library
HY-L045
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Cytoskeleton Compound Library
HY-L060
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Anti-Breast Cancer Compound Library
HY-L074
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Anti-Lung Cancer Compound Library
HY-L075
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Anti-Pancreatic Cancer Compound Library
HY-L077
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Anti-Blood Cancer Compound Library
HY-L079
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Neurodegenerative Disease-related Compound Library
HY-L086
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Anti-Liver Cancer Compound Library
HY-L101
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Protein-protein Interaction Inhibitor Library
HY-L109
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Osteogenesis Compound Library
HY-L131
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Highly Selective Inhibitors Library
HY-L158
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Anti-Hematopathy Compound Library
HY-L171
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Multi-Target Compound Library
HY-L176
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Bioactive Compound Library Max
HY-L181
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MCE Bioactive Compound Library
HY-L001V
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Bioactive Compound Library
HY-L001
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Anti-Brain Cancer Compound Library
HY-L188
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High-Throughput Bioactive Compound Library
HY-L205
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High-Efficiency Gene Editing Compound Library
HY-L244
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Lactylation Compound Library
HY-L249
生物活性
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HDAC6 0.06 μM (IC50) |
HDAC9 5.2 μM (IC50) |
HDAC7 4.7 μM (IC50) |
HDAC8 8.5 μM (IC50) |
HDAC4 11.3 μM (IC50) |
HDAC5 19 μM (IC50) |
HDAC11 10 μM (IC50) |
HDAC1 >1000 μM (IC50) |
HDAC2 >1000 μM (IC50) |
HDAC3 >1000 μM (IC50) |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Baboon (female)[1]
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Dosage:0.1 mg/kg; 1 mg/kg
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Administration:i.v.; single dose; pre-treatment
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Result:Achieved ≥85% HDAC6 target occupancy in the brain.
化学情報
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CAS 番号 2134109-20-7
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性状 Solid
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分子量 346.44
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分子式 C20H27FN2O2
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Color Light yellow to yellow
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SMILES
O=C(NO)C1=CC=C(CN(C)CC2(C3)CC4CC3CC(C4)C2)C(F)=C1
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別名
EKZ-001
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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 In solvent -80°C 6 months -20°C 1 month
溶剤 & 溶解度
DMSO : 100 mg/mL (288.65 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)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.22 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (276 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
[1]. Strebl MG, et al. HDAC6 Brain Mapping with [18F]Bavarostat Enabled by a Ru-Mediated Deoxyfluorination. ACS Cent Sci. 2017 Sep 27;3(9):1006-1014. [Content Brief]
[3]. Watson PR, et al. Aromatic Ring Fluorination Patterns Modulate Inhibitory Potency of Fluorophenylhydroxamates Complexed with Histone Deacetylase 6. Biochemistry. 2022;61(18):1945-1954. [Content Brief]
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 | 1 mM | 2.8865 mL | 14.4325 mL | 28.8650 mL | 72.1626 mL |
| 5 mM | 0.5773 mL | 2.8865 mL | 5.7730 mL | 14.4325 mL | |
| 10 mM | 0.2887 mL | 1.4433 mL | 2.8865 mL | 7.2163 mL | |
| 15 mM | 0.1924 mL | 0.9622 mL | 1.9243 mL | 4.8108 mL | |
| 20 mM | 0.1443 mL | 0.7216 mL | 1.4433 mL | 3.6081 mL | |
| 25 mM | 0.1155 mL | 0.5773 mL | 1.1546 mL | 2.8865 mL | |
| 30 mM | 0.0962 mL | 0.4811 mL | 0.9622 mL | 2.4054 mL | |
| 40 mM | 0.0722 mL | 0.3608 mL | 0.7216 mL | 1.8041 mL | |
| 50 mM | 0.0577 mL | 0.2887 mL | 0.5773 mL | 1.4433 mL | |
| 60 mM | 0.0481 mL | 0.2405 mL | 0.4811 mL | 1.2027 mL | |
| 80 mM | 0.0361 mL | 0.1804 mL | 0.3608 mL | 0.9020 mL | |
| 100 mM | 0.0289 mL | 0.1443 mL | 0.2887 mL | 0.7216 mL |
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