| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
HIV-1 HIV-1 (K103N) HIV-1 (Y181C)
Fosdevirine targets HIV-1 reverse transcriptase, a key enzyme required for viral replication. As a non-nucleoside reverse transcriptase inhibitor (NNRTI), it binds to an allosteric site on the reverse transcriptase enzyme, distinct from the nucleoside binding site. This binding induces a conformational change that inhibits the enzyme's polymerase activity, thereby blocking the transcription of viral RNA into DNA and preventing viral replication. It demonstrates activity against both wild-type and drug-resistant HIV-1 strains, including the K103N and Y181C single point mutations. |
|---|---|
| ln Vitro |
Fosdevirine shows significant in vitro antiviral activity against the majority of double mutants as well as the K103N and Y181C single point alterations [1].
In vitro, Fosdevirine demonstrates significant antiviral activity against the majority of HIV-1 double mutants as well as the K103N and Y181C single point alterations. It shows low nanomolar activity in vitro with an EC50 of 11 nM. Fosdevirine exhibits potent antiviral activity against a variety of HIV-1 strains, including those resistant to efavirenz. Its high potency and activity against resistant strains make it a valuable tool for studying HIV-1 resistance mechanisms and developing new therapeutic strategies. |
| ln Vivo |
In vivo data for Fosdevirine is derived from clinical studies in HIV-infected subjects. It demonstrated potent antiviral activity in treatment-naive HIV-infected subjects and had favorable pharmacokinetic and resistance profiles. The compound was investigated for use in HIV infection and acquired immune deficiency syndrome (AIDS). However, specific published in vivo efficacy studies in animal models are not detailed in the available literature. Fosdevirine is primarily used as a research compound for studying HIV-1 replication and resistance.
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| Enzyme Assay |
The in vitro antiviral assay for Fosdevirine is conducted in HIV-1-infected cell lines. Cells are infected with HIV-1 in the presence of varying concentrations of the compound, and viral replication is measured by quantifying viral RNA, p24 antigen production, or reporter gene expression. EC₅₀ values are calculated from dose-response curves. The compound's activity against drug-resistant strains is assessed using recombinant viruses carrying specific mutations such as K103N and Y181C. Cell viability is assessed to confirm that antiviral activity is not due to cytotoxicity.
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| Cell Assay |
Cellular assays for Fosdevirine are conducted in HIV-1-susceptible cell lines such as MT-4 or CEM cells. Cells are infected with HIV-1 and treated with varying concentrations of the compound. Viral replication is measured by quantifying viral RNA, p24 antigen, or by using reporter viruses. EC₅₀ values are calculated from dose-response curves. The compound's activity against drug-resistant strains is evaluated using recombinant viruses. Cell viability is assessed using standard assays such as MTT to confirm that inhibition is due to antiviral activity.
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| Animal Protocol |
In vivo studies for Fosdevirine have been conducted in clinical trials involving HIV-infected subjects. The compound was administered orally as a once-daily dose. Efficacy was assessed by measuring viral load reduction in plasma. Pharmacokinetic parameters were evaluated to determine the compound's absorption, distribution, metabolism, and excretion profile. However, specific published in vivo protocols in animal models are not detailed in the available literature. Fosdevirine has been investigated for use in HIV infection and AIDS.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Fosdevirine indicates that it has favorable pharmacokinetic properties, supporting once-daily dosing. In clinical studies, the compound demonstrated a favorable PK profile in HIV-infected subjects. It has a molecular weight of 413.8 g/mol and a LogP of 2.94. Storage conditions: powder at -20°C for 3 years or 4°C for 2 years; in solvent at -80°C for 6 months or -20°C for 1 month. Detailed PK parameters such as half-life and bioavailability are not extensively reported.
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| Toxicity/Toxicokinetics |
Toxicity data for Fosdevirine is derived from clinical studies in HIV-infected subjects. As with all research compounds, Fosdevirine is intended for research use only and not for human therapeutic applications outside of approved clinical trials. The compound's safety profile was evaluated in clinical studies, but specific toxicity data is not detailed in the available literature. Comprehensive toxicology studies would be required for therapeutic development.
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| References | |
| Additional Infomation |
See also: Fostivirine (note moved to).
Drug Indications It has been studied for the treatment of HIV infection, acquired immunodeficiency syndrome (AIDS), and AIDS-related infections. Fosdevirine (GSK2248761) is a potent, selective NNRTI of HIV-1 replication with low nanomolar activity. It is a novel, once-daily inhibitor with activity against efavirenz-resistant strains. Fosdevirine has demonstrated potent antiviral activity in treatment-naive HIV-infected subjects and has favorable PK and resistance profiles. It has been investigated for use in HIV infection and AIDS. The compound has a molecular formula of C₂₀H₁₇ClN₃O₃P and a molecular weight of 413.8 g/mol. |
| Molecular Formula |
C20H17CLN3O3P
|
|---|---|
| Exact Mass |
413.069
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| CAS # |
1018450-26-4
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| PubChem CID |
23583058
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| Appearance |
Typically exists as solid at room temperature
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
686.4±65.0 °C at 760 mmHg
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| Flash Point |
368.9±34.3 °C
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| Vapour Pressure |
0.0±2.1 mmHg at 25°C
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| Index of Refraction |
1.664
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| LogP |
2.94
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
|
| Rotatable Bond Count |
5
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| Heavy Atom Count |
28
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| Complexity |
721
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
N#C/C=C/C1C=C(C)C=C(P(C2=C(C(=O)N)NC3=CC=C(C=C23)Cl)(=O)OC)C=1
|
| InChi Key |
CGBYTKOSZYQOPV-ONEGZZNKSA-N
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| InChi Code |
InChI=1S/C20H17ClN3O3P/c1-12-8-13(4-3-7-22)10-15(9-12)28(26,27-2)19-16-11-14(21)5-6-17(16)24-18(19)20(23)25/h3-6,8-11,24H,1-2H3,(H2,23,25)/b4-3+
|
| Chemical Name |
5-chloro-3-[[3-[(E)-2-cyanoethenyl]-5-methylphenyl]-methoxyphosphoryl]-1H-indole-2-carboxamide
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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