VNRX-9945
Based on 1 Customer Validation
VNRX-9945 is a potent, broadly and orally active HBV CAM (capsid assembly modulator) with an EC50 of 2.6 nM. VNRX-9945 exhibits excellent and broad antiviral activity against multiple HBV genotypes in vitro, along with favorable pharmacokinetic profiles across multiple species. VNRX-9945 demonstrates robust antiviral efficacy in the adeno-associated virus mice models of HBV (AAV-HBV) infection.
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: 99.46%
- CAS 番号: 2396680-45-6
- 分子式: C23H28FN3O4
- 分子量:429.48
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保管条件:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
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生物活性
| Species | Dose | Route | Cmax | AUC0-inf | T1/2 | F | CL |
|---|---|---|---|---|---|---|---|
| Cynomolgus Monkey | 10 mg/kg | p.o. | 2577 ng/mL | 32732 ng·h/mL | 16 h | 36 % | / |
| Cynomolgus Monkey | 3 mg/kg | i.v. | / | / | / | / | 2.64 mL/min/kg |
| Dog | 10 mg/kg | p.o. | 1937 ng/mL | 50404 ng·h/mL | 11 h | 37 % | / |
| Dog | 3 mg/kg | i.v. | / | / | / | / | 1.2 mL/min/kg |
| Rat | 10 mg/kg | p.o. | 3043 ng/mL | 11130 ng·h/mL | 3.7 h | 86 % | / |
| Rat | 5 mg/kg | i.v. | / | / | / | / | 16.3 mL/min/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AAV-HBV mice models (C57BL/6)[1]
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Dosage:10, 30, and 100 mg/kg
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Administration:Oral gavage, twice daily for 8 weeks.
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Result:Resulted in a significant, dose-dependent reduction in circulating HBV DNA and HBV pgRNA levels.
Led to a > 3 log10 reduction in HBV DNA and an ∼ 2 log10 reduction in HBV pgRNA from baseline at 100 mg/kg.
Showed no changes in HBsAg and HBeAg levels, body weight and ALT levels.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 2396680-45-6
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性状 Solid
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分子量 429.48
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分子式 C23H28FN3O4
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Color White to off-white
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SMILES
O=C(C1=C(C)N(C)C(C(C(N[C@H]2CC[C@@H](O)CC2)=O)=O)=C1C)NC3=CC=C(F)C(C)=C3
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶剤 & 溶解度
DMSO : 100 mg/mL (232.84 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 (protect from light). 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 (protect from light). 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: ≥ 5 mg/mL (11.64 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (11.64 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (272 KB)
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SDS (251 KB)
- English - EN (251 KB)
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- 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 (protect from light). 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 | 2.3284 mL | 11.6420 mL | 23.2840 mL | 58.2099 mL |
| 5 mM | 0.4657 mL | 2.3284 mL | 4.6568 mL | 11.6420 mL | |
| 10 mM | 0.2328 mL | 1.1642 mL | 2.3284 mL | 5.8210 mL | |
| 15 mM | 0.1552 mL | 0.7761 mL | 1.5523 mL | 3.8807 mL | |
| 20 mM | 0.1164 mL | 0.5821 mL | 1.1642 mL | 2.9105 mL | |
| 25 mM | 0.0931 mL | 0.4657 mL | 0.9314 mL | 2.3284 mL | |
| 30 mM | 0.0776 mL | 0.3881 mL | 0.7761 mL | 1.9403 mL | |
| 40 mM | 0.0582 mL | 0.2910 mL | 0.5821 mL | 1.4552 mL | |
| 50 mM | 0.0466 mL | 0.2328 mL | 0.4657 mL | 1.1642 mL | |
| 60 mM | 0.0388 mL | 0.1940 mL | 0.3881 mL | 0.9702 mL | |
| 80 mM | 0.0291 mL | 0.1455 mL | 0.2910 mL | 0.7276 mL | |
| 100 mM | 0.0233 mL | 0.1164 mL | 0.2328 mL | 0.5821 mL |
VNRX-9945 関連分類
HY-174819 関連分類
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