Trovirdine
Based on 1 publication(s) in Google Scholar
Trovirdine (LY300046) is a selective non-nucleoside HIV-1 reverse transcriptase inhibitor, with an IC50 value of 0.012 μM against the wild-type enzyme. Trovirdine inhibits the replication of both wild-type and mutant HIV-1, and exerts synergistic or additive effects when combined with some antiviral drugs. Trovirdine is applicable to research related to HIV-1 infection.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Pureté : 98.62%
- CAS No.: 149488-17-5
- Formule: C13H13BrN4S
- Masse moléculaire:337.24
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Trovirdine
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Activité biologique
Description
IC50 & Target
[1]|
HIV-1 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MT4 | IC50 |
0.013 μM
|
Inhibition of wild-type HIV-1 replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
Inhibition of wild-type HIV-1 replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC90 |
0.038 μM
|
90% inhibition of wild-type HIV-1 replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
90% inhibition of wild-type HIV-1 replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC50 |
3.90 μM
|
Inhibition of HIV-1 (Ile100) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
Inhibition of HIV-1 (Ile100) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC90 |
19.0 μM
|
90% inhibition of HIV-1 (Ile100) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
90% inhibition of HIV-1 (Ile100) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC50 |
24.5 μM
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Inhibition of HIV-1 (Asn103) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
Inhibition of HIV-1 (Asn103) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC90 |
61.1 μM
|
90% inhibition of HIV-1 (Asn103) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
90% inhibition of HIV-1 (Asn103) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
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9341211 |
| MT4 | IC50 |
1.90 μM
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Inhibition of HIV-1 (Cys181) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
Inhibition of HIV-1 (Cys181) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
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9341211 |
| MT4 | IC90 |
5.80 μM
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90% inhibition of HIV-1 (Cys181) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
90% inhibition of HIV-1 (Cys181) mutant replication in MT-4 cells assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
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9341211 |
| MT4 | IC50 |
0.019 μM
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Inhibition of wild-type HIV-1 replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
Inhibition of wild-type HIV-1 replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC90 |
0.060 μM
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90% inhibition of wild-type HIV-1 replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
90% inhibition of wild-type HIV-1 replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC50 |
4.0 μM
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Inhibition of HIV-1 (Ile100) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
Inhibition of HIV-1 (Ile100) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
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9341211 |
| MT4 | IC90 |
34.8 μM
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90% inhibition of HIV-1 (Ile100) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
90% inhibition of HIV-1 (Ile100) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
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9341211 |
| MT4 | IC50 |
13.7 μM
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Inhibition of HIV-1 (Asn103) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
Inhibition of HIV-1 (Asn103) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC90 |
25.8 μM
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90% inhibition of HIV-1 (Asn103) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
90% inhibition of HIV-1 (Asn103) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC50 |
0.87 μM
|
Inhibition of HIV-1 (Cys181) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
Inhibition of HIV-1 (Cys181) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
| MT4 | IC90 |
7.25 μM
|
90% inhibition of HIV-1 (Cys181) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
90% inhibition of HIV-1 (Cys181) mutant replication in MT-4 cells (in ddI combination context) assessed via cell viability measured by XTT assay after 6-day incubation with compound and virus, followed by 6-hour incubation with XTT reagent.
|
9341211 |
In Vitro
Trovirdine potently inhibits the activity of wild-type HIV-1 reverse transcriptase with an IC50 of 0.012 μM; it also inhibits the replication of wild-type HIV-1 in MT-4 cells with an IC50 of 0.013 μM[1].
Trovirdine exhibits IC50 values of 0.34 μM and 0.33 μM against HIV‑1 RT Tyr181→Cys and HIV‑1 RT Leu100→Ile mutants with 28‑fold and 27‑fold resistance respectively. In MT‑4 cells, Trovirdine shows IC50 values of 3.90 μM, 24.5 μM and 1.90 μM for HIV‑1 Ile100, Asn103 and Cys181 mutant strains, with resistance factors >300‑fold, >1×103‑fold and >140‑fold correspondingly[1].
Trovirdine inhibits the activity of wild-type HIV‑1 reverse transcriptase (measured by the dCTP incorporation assay) with an IC50 of 0.03 μM; it also inhibits the activities of the HIV‑1 RT Tyr181→Cys mutant and HIV‑1 RT Leu100→Ile mutant, with corresponding IC50 values of 0.53 μM and 0.34 μM, respectively[1].
Trovirdine (6 days) inhibits the replication of wild-type HIV-1 as well as HIV-1 Ile100, Asn103, and Cys181 mutants in MT-4 cells in the context of combination testing with ddI, with corresponding IC50 values of 0.019 μM, 4.0 μM, 13.7 μM, and 0.87 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Chemical Information
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CAS No. 149488-17-5
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Appearance Solid
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Masse moléculaire 337.24
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Formule C13H13BrN4S
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Color White to off-white
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SMILES
S=C(NCCC1=NC=CC=C1)NC2=NC=C(Br)C=C2
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Synonyms
LY300046
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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Int J Antimicrob Agents
2019 Dec;54(6):814-819. PMID: 31479744
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (296.52 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (7.41 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.
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.
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.
Protocole
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Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.9652 mL | 14.8262 mL | 29.6525 mL | 74.1312 mL |
| 5 mM | 0.5930 mL | 2.9652 mL | 5.9305 mL | 14.8262 mL | |
| 10 mM | 0.2965 mL | 1.4826 mL | 2.9652 mL | 7.4131 mL | |
| 15 mM | 0.1977 mL | 0.9884 mL | 1.9768 mL | 4.9421 mL | |
| 20 mM | 0.1483 mL | 0.7413 mL | 1.4826 mL | 3.7066 mL | |
| 25 mM | 0.1186 mL | 0.5930 mL | 1.1861 mL | 2.9652 mL | |
| 30 mM | 0.0988 mL | 0.4942 mL | 0.9884 mL | 2.4710 mL | |
| 40 mM | 0.0741 mL | 0.3707 mL | 0.7413 mL | 1.8533 mL | |
| 50 mM | 0.0593 mL | 0.2965 mL | 0.5930 mL | 1.4826 mL | |
| 60 mM | 0.0494 mL | 0.2471 mL | 0.4942 mL | 1.2355 mL | |
| 80 mM | 0.0371 mL | 0.1853 mL | 0.3707 mL | 0.9266 mL | |
| 100 mM | 0.0297 mL | 0.1483 mL | 0.2965 mL | 0.7413 mL |
Trovirdine Related Classifications
HY-15349 Related Classifications
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