Fosamprenavir Calcium Salt
Based on 4 publication(s) in Google Scholar
Fosamprenavir Calcium Salt (GW433908G) is an orally active inhibitor targeting HIV-1 protease and is a prodrug of Amprenavir (HY-17430). Fosamprenavir Calcium Salt is hydrolyzed into Amprenavir (VX-478) by cell phosphatases in the intestinal epithelium. Amprenavir binds to the active site of HIV-1 protease, preventing the processing of viral gag and gag-pol polyprotein precursors, thereby inhibiting the formation of mature infectious virus particles and exerting anti-HIV-1 infection activity. Fosamprenavir Calcium Salt can be used for the study of human immunodeficiency virus (HIV-1) infection.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.21%
- CAS. Nr.: 226700-81-8
- Formel: C25H34CaN3O9PS
- Molecular Weight:623.67
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Speicherung:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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HY-17430
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HY-14588
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HY-17007
SaquinavirHIV Protease Inhibitor -
HY-90001
RitonavirHIV Protease Inhibitor -
HY-17003
Saquinavir mesylateHIV Protease Inhibitor -
HY-15287A
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HY-15148
TipranavirHIV Protease Inhibitor -
HY-17367A
Atazanavir sulfateHIV Protease Inhibitor
Publications Citing Use of MedChemExpress (MCE) Fosamprenavir Calcium Salt
More
Biologische Aktivität
Beschreibung
IC50 & Target
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HIV-1 |
In Vitro
Amprenavir, the active form of Fosamprenavir Calcium Salt (GW433908G), can bind to and inhibit the activity of pepsin in vitro with an IC50 of 3.56 μM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:6-week-old female Jackson A/J mice with laryngopharyngeal reflux model (mechanical laryngeal injury once weekly for 2 weeks and pH7 solvent/pepsin instillation 3 days/week for 4 weeks)[2]
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Dosage:20 mg/kg/day Fosamprenavir
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Administration:gavage, daily, 4 weeks (5 days/week)
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Result:Prevented pepsin-mediated laryngeal damage, which was characterized by reactive epithelia, increased intraepithelial inflammatory cells, and cell apoptosis.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS. Nr. 226700-81-8
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Appearance Solid
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Molecular Weight 623.67
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Formel C25H34CaN3O9PS
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Color White to off-white
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SMILES
O=C(O[C@@H]1COCC1)N[C@@H](CC2=CC=CC=C2)[C@H](OP([O-])([O-])=O)CN(S(=O)(C3=CC=C(N)C=C3)=O)CC(C)C.[Ca+2]
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Synonyms
GW433908G
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (4)
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Journal Impact Factor
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Most Recent
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Nat Commun
Both Boceprevir and GC376 efficaciously inhibit SARS-CoV-2 by targeting its main protease. [Abstract]2020 Sep 4;11(1):4417. PMID: 32887884 -
Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744 -
Antimicrob Agents Chemother
2020 Aug 20;64(9):e00872-20. PMID: 32669265 -
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (80.17 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 0.25 mg/mL (0.40 mM; Need ultrasonic and warming)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
In Vivo:
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 (4.01 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.01 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 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Reinheit & Dokumentation
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Data Sheet (295 KB)
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SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Korean - KR (394 KB)
- Portuguese - PT (394 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Hester EK, et al. Fosamprenavir: drug development for adherence. Ann Pharmacother. 2006 Jul-Aug;40(7-8):1301-10. [Content Brief]
[2]. Johnston N, et al. Oral and Inhaled Fosamprenavir Reverses Pepsin-Induced Damage in a Laryngopharyngeal Reflux Mouse Model. Laryngoscope. 2023 Jan;133 Suppl 1(Suppl 1):S1-S11. [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 (sealed storage, away from moisture). 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 | 1.6034 mL | 8.0171 mL | 16.0341 mL | 40.0853 mL |
| 5 mM | 0.3207 mL | 1.6034 mL | 3.2068 mL | 8.0171 mL | |
| 10 mM | 0.1603 mL | 0.8017 mL | 1.6034 mL | 4.0085 mL | |
| 15 mM | 0.1069 mL | 0.5345 mL | 1.0689 mL | 2.6724 mL | |
| 20 mM | 0.0802 mL | 0.4009 mL | 0.8017 mL | 2.0043 mL | |
| 25 mM | 0.0641 mL | 0.3207 mL | 0.6414 mL | 1.6034 mL | |
| 30 mM | 0.0534 mL | 0.2672 mL | 0.5345 mL | 1.3362 mL | |
| 40 mM | 0.0401 mL | 0.2004 mL | 0.4009 mL | 1.0021 mL | |
| 50 mM | 0.0321 mL | 0.1603 mL | 0.3207 mL | 0.8017 mL | |
| 60 mM | 0.0267 mL | 0.1336 mL | 0.2672 mL | 0.6681 mL | |
| 80 mM | 0.0200 mL | 0.1002 mL | 0.2004 mL | 0.5011 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Fosamprenavir Calcium Salt Related Classifications
HY-17431 Related Classifications
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