Valnivudine
Valnivudine (FV-100 free base), a proagent of CF-1743, is an orally active anti-herpes zoster (HZ) nucleoside analogue. CF-1743, a bicyclic nucleoside analog (BCNA), has highly specific antiviral activity against varicella-zoster virus (VZV). Valnivudine is rapidly and extensively converted to CF-1743 in vivo.
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- CAS No.: 956483-02-6
- 화학식: C27H35N3O6
- 분자량:497.58
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
In vitro cytotoxicity studies in normal human primary hepatocytes, keratinocytes, and rapidly dividing HepG2 cells, Valnivudine (FV-100 free base) demonstrates mean 50% cytotoxic concentration values of >10 μM[2].
CF-1743 (compound 4f) has anti-varicella-zoster virus (VZV) activity in VZV OKA (EC50=0.3 nM), VZV YS (EC50=0.1 nM) in HEL cell[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 956483-02-6
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Appearance Solid
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분자량 497.58
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화학식 C27H35N3O6
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Color Light yellow to yellow
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SMILES
O=C1N=C2C(C=C(C3=CC=C(C=C3)CCCCC)O2)=CN1[C@]4([H])O[C@@H]([C@H](C4)O)COC([C@@H](N)C(C)C)=O
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Synonyms
FV-100 free base
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
DMSO : 50 mg/mL (100.49 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.02 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.
순도&문서
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Data Sheet (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
[1]. Nathan B Price, et al. Progress in the development of new therapies for herpesvirus infections. Curr Opin Virol. 2011 Dec;1(6):548-54. [Content Brief]
[2]. Helen S Pentikis, et al. Pharmacokinetics and safety of FV-100, a novel oral anti-herpes zoster nucleoside analogue, administered in single and multiple doses to healthy young adult and elderly adult volunteers. Antimicrob Agents Chemother. 2011 Jun;55(6):2847-54. [Content Brief]
[3]. C McGuigan, et al. Highly potent and selective inhibition of varicella-zoster virus by bicyclic furopyrimidine nucleosides bearing an aryl side chain. J Med Chem. 2000 Dec 28;43(26):4993-7. [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 |
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| DMSO | 1 mM | 2.0097 mL | 10.0486 mL | 20.0973 mL | 50.2432 mL |
| 5 mM | 0.4019 mL | 2.0097 mL | 4.0195 mL | 10.0486 mL | |
| 10 mM | 0.2010 mL | 1.0049 mL | 2.0097 mL | 5.0243 mL | |
| 15 mM | 0.1340 mL | 0.6699 mL | 1.3398 mL | 3.3495 mL | |
| 20 mM | 0.1005 mL | 0.5024 mL | 1.0049 mL | 2.5122 mL | |
| 25 mM | 0.0804 mL | 0.4019 mL | 0.8039 mL | 2.0097 mL | |
| 30 mM | 0.0670 mL | 0.3350 mL | 0.6699 mL | 1.6748 mL | |
| 40 mM | 0.0502 mL | 0.2512 mL | 0.5024 mL | 1.2561 mL | |
| 50 mM | 0.0402 mL | 0.2010 mL | 0.4019 mL | 1.0049 mL | |
| 60 mM | 0.0335 mL | 0.1675 mL | 0.3350 mL | 0.8374 mL | |
| 80 mM | 0.0251 mL | 0.1256 mL | 0.2512 mL | 0.6280 mL | |
| 100 mM | 0.0201 mL | 0.1005 mL | 0.2010 mL | 0.5024 mL |
Valnivudine Related Classifications
HY-109016 Related Classifications
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