HBF-0259
Based on 1 Customer Validation
HBF-0259 is a potent and selective inhibitor of hepatitis B virus (HBV) surface antigen (HBsAg) secretion, with an EC50 of 1.5 μM in HepG2.2.15 cells. HBF-0259 has no effect on HBV DNA synthesis.
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: 99.99%
- CAS 番号: 957011-15-3
- 分子式: C16H12Cl2FN5
- 分子量:364.20
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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
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HepG2 | EC50 |
14.2 μM
Compound: 5
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Antiviral activity against lamivudine/telbivudine-resistant Hepatitis B virus harboring polymerase L528M and M552V mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
Antiviral activity against lamivudine/telbivudine-resistant Hepatitis B virus harboring polymerase L528M and M552V mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
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[PMID: 21786803] |
| HepG2 | EC50 |
32 μM
Compound: 5
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Antiviral activity against wild-type Hepatitis B virus infected in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
Antiviral activity against wild-type Hepatitis B virus infected in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
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[PMID: 21786803] |
| HepG2 | EC50 |
5.5 μM
Compound: 5
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Antiviral activity against lamivudine/telbivudine-resistant Hepatitis B virus harboring polymerase M552I mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
Antiviral activity against lamivudine/telbivudine-resistant Hepatitis B virus harboring polymerase M552I mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
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[PMID: 21786803] |
| HepG2 | EC50 |
5.6 μM
Compound: 5
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Antiviral activity against adefovir-resistant Hepatitis B virus harboring polymerase N584T mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
Antiviral activity against adefovir-resistant Hepatitis B virus harboring polymerase N584T mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
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[PMID: 21786803] |
| HepG2 | EC50 |
6.4 μM
Compound: 5
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Antiviral activity against entecavir-resistant Hepatitis B virus harboring polymerase L528M, M552V, T532G and S550I mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
Antiviral activity against entecavir-resistant Hepatitis B virus harboring polymerase L528M, M552V, T532G and S550I mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
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[PMID: 21786803] |
| HepG2 | EC50 |
9 μM
Compound: 5
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Antiviral activity against adefovir-resistant Hepatitis B virus harboring polymerase A529V mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
Antiviral activity against adefovir-resistant Hepatitis B virus harboring polymerase A529V mutant in human HepG2 cells assessed as inhibition of HBsAg secretion by ELISA
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[PMID: 21786803] |
| HepG2 2.2.15 | CC50 |
>50 μM
Compound: 194
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Cytotoxicity against human HepG2.2.15 cells by MTT assay
Cytotoxicity against human HepG2.2.15 cells by MTT assay
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[PMID: 24549242] |
| HepG2 2.2.15 | CC50 |
>50 μM
Compound: 5
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Cytotoxicity against human HepG2(2.2.15) cells by MTT assay
Cytotoxicity against human HepG2(2.2.15) cells by MTT assay
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[PMID: 21786803] |
| HepG2 2.2.15 | EC50 |
11.3 μM
Compound: 5
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Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of HBsAg secretion after 6 days by ELISA
Antiviral activity against Hepatitis B virus infected in human HepG2(2.2.15) cells assessed as inhibition of HBsAg secretion after 6 days by ELISA
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[PMID: 21786803] |
| HepG2 2.2.15 | EC50 |
3 μM
Compound: HBF-0259
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Antiviral activity against Hepatitis B virus in human HepG2(2.2.15) cells assessed as reduction of large HBsAg secretion after 6 days by densitometric analysis
Antiviral activity against Hepatitis B virus in human HepG2(2.2.15) cells assessed as reduction of large HBsAg secretion after 6 days by densitometric analysis
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[PMID: 17875990] |
| HepG2 2.2.15 | EC50 |
4 μM
Compound: HBF-0259
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Antiviral activity against Hepatitis B virus in human HepG2(2.2.15) cells assessed as reduction of medium HBsAg secretion after 6 days by densitometric analysis
Antiviral activity against Hepatitis B virus in human HepG2(2.2.15) cells assessed as reduction of medium HBsAg secretion after 6 days by densitometric analysis
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[PMID: 17875990] |
体外実験
HBF-0259 (0.0158-50.0 μM) inhibits the HBsAg secretion (EC50=1.5 μM) in HepDE19 cells, with an CC50 of >50 μM[1].
HBF-0259 (2-8 μM) significantly reduces the abundance of both L and M in the supernatants of HepG2.2.15 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
化学情報
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CAS 番号 957011-15-3
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性状 Solid
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分子量 364.20
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分子式 C16H12Cl2FN5
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Color White to off-white
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SMILES
ClC1=CC=C(C2N=C3N(NN=N3)C(C4=C(F)C=CC=C4Cl)C2)C=C1
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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 : 100 mg/mL (274.57 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)
体内:
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: ≥ 2.08 mg/mL (5.71 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
In Vivo Dissolution Calculator
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 (275 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]. Dougherty AM, et, al. A substituted tetrahydro-tetrazolo-pyrimidine is a specific and novel inhibitor of hepatitis B virus surface antigen secretion. Antimicrob Agents Chemother. 2007 Dec;51(12):4427-37. [Content Brief]
[2]. Yu W, et, al. Design, synthesis, and biological evaluation of triazolo-pyrimidine derivatives as novel inhibitors of hepatitis B virus surface antigen (HBsAg) secretion. J Med Chem. 2011 Aug 25;54(16):5660-70. [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 | 2.7457 mL | 13.7287 mL | 27.4574 mL | 68.6436 mL |
| 5 mM | 0.5491 mL | 2.7457 mL | 5.4915 mL | 13.7287 mL | |
| 10 mM | 0.2746 mL | 1.3729 mL | 2.7457 mL | 6.8644 mL | |
| 15 mM | 0.1830 mL | 0.9152 mL | 1.8305 mL | 4.5762 mL | |
| 20 mM | 0.1373 mL | 0.6864 mL | 1.3729 mL | 3.4322 mL | |
| 25 mM | 0.1098 mL | 0.5491 mL | 1.0983 mL | 2.7457 mL | |
| 30 mM | 0.0915 mL | 0.4576 mL | 0.9152 mL | 2.2881 mL | |
| 40 mM | 0.0686 mL | 0.3432 mL | 0.6864 mL | 1.7161 mL | |
| 50 mM | 0.0549 mL | 0.2746 mL | 0.5491 mL | 1.3729 mL | |
| 60 mM | 0.0458 mL | 0.2288 mL | 0.4576 mL | 1.1441 mL | |
| 80 mM | 0.0343 mL | 0.1716 mL | 0.3432 mL | 0.8580 mL | |
| 100 mM | 0.0275 mL | 0.1373 mL | 0.2746 mL | 0.6864 mL |
HBF-0259 関連分類
HY-126970 関連分類
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