Fosamprenavir Calcium Salt (Synonyms: GW 433908G) |
| カタログ番号GC11300 |
アンプレナビルのプロドラッグ形式
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 226700-81-8
Sample solution is provided at 25 µL, 10mM.
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GW433908G is a selective inhibitor of antiretroviral protease with the concentration of 1395 mg nM once daily in clinical trial [1].
Antiretroviral protease is a subfamily of protease inhibitors and plays a pivotal role in treating HIV/AIDS and HCV infection. It has been reported that drugs designed as protease inhibitors can prevent viral replication by selectively binding to viral proteases (e.g. HIV-1 protease) and blocking proteolytic cleavage of protein precursors that are necessary for the production of infectious viral particles [2] [3].
GW433908 is a potent antiretroviral protease inhibitor and has improved solubility than amprenavir capsules. Many clinical studies have been done to examine GE433908 safety and pharmacokinetic profiles. In healthy male volunteers, administered GW433908 as tablets or suspension, food had slight effect on its pharmacokinetics and with fewer tablets GW433908 were well tolerated and delivered plasma amprenavir concentrations equivalent to the recommended therapeutic amprenavir dose which may be of clinical benefit in the treatment of HIV infection [4]. As a phosphate ester prodrug of the antiretroviral protease inhibitor amprenavir, GW433908 (1395 mg, QD) combined with efavirenz (200 mg, QD) decreased plasma APV exposure when tested with healthy volunteers [1].
References:
[1]. Wire, M.B., et al., Pharmacokinetics and safety of GW433908 and ritonavir, with and without efavirenz, in healthy volunteers. Aids, 2004. 18(6): p. 897-907.
[2]. Hamada, Y., et al., High incidence of renal stones among HIV-infected patients on ritonavir-boosted atazanavir than in those receiving other protease inhibitor-containing antiretroviral therapy. Clin Infect Dis, 2012. 55(9): p. 1262-9.
[3]. Zheng, Y., et al., Antiretroviral therapy and efficacy after virologic failure on first-line boosted protease inhibitor regimens. Clin Infect Dis, 2014. 59(6): p. 888-96.
[4]. Falcoz, C., et al., Pharmacokinetics of GW433908, a prodrug of amprenavir, in healthy male volunteers. J Clin Pharmacol, 2002. 42(8): p. 887-98.
| Cas No. | 226700-81-8 | SDF | |
| 同義語 | GW 433908G | ||
| Chemical Name | calcium;[(2R,3S)-1-[(4-aminophenyl)sulfonyl-(2-methylpropyl)amino]-3-[[(3S)-oxolan-3-yl]oxycarbonylamino]-4-phenylbutan-2-yl] phosphate | ||
| Canonical SMILES | CC(C)CN(CC(C(CC1=CC=CC=C1)NC(=O)OC2CCOC2)OP(=O)([O-])[O-])S(=O)(=O)C3=CC=C(C=C3)N.[Ca+2] | ||
| Formula | C25H34CaN3O9PS | M.Wt | 623.67 |
| 溶解度 | <6.51 mg/mL in DMSO, <6.24 mg/mL in Water, ≥ 40.1 mg/mL in EtOH with gentle warming | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 1.6034 mL | 8.0171 mL | 16.0341 mL |
| 5 mM | 0.3207 mL | 1.6034 mL | 3.2068 mL |
| 10 mM | 0.1603 mL | 0.8017 mL | 1.6034 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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