Darunavir (Synonyms: TMC114) |
| Catalog No.GC16602 |
An HIV-1 protease inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 206361-99-1
Sample solution is provided at 25 µL, 10mM.
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Darunavir is an orally-bioavailable non-peptidic inhibitor of human immunodeficiency virus type 1 (HIV-1) protease that selectively inhibits HIV-1 protease enzyme induced cleavage of gag and gag-pol poly-proteins preventing the maturation of virions and also inhibits the dimerization of HIV-1 protease suppressing proteolytic activity and subsequent replication of HIV-1. Study results have shown that darunavir exhibits potent inhibition against HIV-1 with a value of 50% inhibition concentration IC50 of 0.003 μmol/L in HIV-1 infected MT-2 cells. Darunavir binds to HIV-1 protease with considerably high affinity and fits closely with the substrate envelop leading to its potent ability to inhibit multidrug-resistant HIV strains.
Reference
[1].McKeage K, Perry CM, Keam SJ. Darunavir: a review of its use in the management of HIV infection in adults. Drugs. 2009;69(4):477-503. doi: 10.2165/00003495-200969040-00007.
| Cas No. | 206361-99-1 | SDF | |
| Synonyms | TMC114 | ||
| Chemical Name | (E)-(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl hydrogen ((2S,3R)-4-(4-amino-N-isobutylphenylsulfonamido)-3-hydroxy-1-phenylbutan-2-yl)carbonimidate | ||
| Canonical SMILES | CC(CN(S(C1=CC=C(N)C=C1)(=O)=O)C[C@](O)([H])[C@](/N=C(O[C@@]2([H])CO[C@]3([H])[C@@]2([H])CCO3)\O)([H])CC4=CC=CC=C4)C | ||
| Formula | C27H37N3O7S | M.Wt | 547.66 |
| Solubility | ≥ 22.65mg/mL in DMSO, ≥ 4.94 mg/mL in EtOH with ultrasonic | 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 | 1.826 mL | 9.1298 mL | 18.2595 mL |
| 5 mM | 0.3652 mL | 1.826 mL | 3.6519 mL |
| 10 mM | 0.1826 mL | 0.913 mL | 1.826 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: >99.50%
- 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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