Censavudine
Based on 1 Customer Validation
Censavudine (OBP-601; BMS-986001), a nucleoside analog, is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1, respectively. Censavudine is a click chemistry reagent, it contains an Alkyne group and can undergo copper-catalyzed azide-alkyne cycloaddition (CuAAc) with molecules containing Azide groups.
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- Purity: 98.00%
- CAS No.: 634907-30-5
- 화학식: C12H12N2O4
- 분자량:248.24
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보관:
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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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Biological Activity
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HIV-2 30-81 nM (EC50) |
HIV-1 450-890 nM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HEK-293T | CC50 |
>100 μM
Compound: 4'-Ed4T
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Cytotoxicity against human 293T cells assessed as inhibition of cell proliferation by tetrazolium dye method
Cytotoxicity against human 293T cells assessed as inhibition of cell proliferation by tetrazolium dye method
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[PMID: 17470654] |
| MT2 | CC50 |
>100 μM
Compound: 15
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Cytotoxic concentration required to reduce the viability of mock-infected MT-2 cells by 50%
Cytotoxic concentration required to reduce the viability of mock-infected MT-2 cells by 50%
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[PMID: 14552777] |
| MT2 | CC50 |
>256 μM
Compound: 22
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Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
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[PMID: 32031378] |
| MT2 | IC50 |
0.2 μM
Compound: 15
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Inhibitory activity against HIV-1 IIIB to achieve 50% protection of MT-2 cells
Inhibitory activity against HIV-1 IIIB to achieve 50% protection of MT-2 cells
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[PMID: 14552777] |
| MT4 | CC50 |
>100 μM
Compound: 4
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Cytotoxicity against MT4 cells MTT assay
Cytotoxicity against MT4 cells MTT assay
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[PMID: 17181169] |
| MT4 | EC50 |
0.06 μM
Compound: 4
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Antiviral activity against HIV1 3B in MT4 cells by MTT assay
Antiviral activity against HIV1 3B in MT4 cells by MTT assay
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[PMID: 17181169] |
BMS-986001 shows greater activity against HIV-2ROD9 than against HIV-1NL4-3; the mean EC50s for BMS-986001 are 74 nM for HIV-2ROD9 and 890 nM for HIV-1NL4-3 in the single-cycle assay. HIV-2ROD9 also showes greater sensitivity to BMS-986001 in 4-day infections of an immortalized T cell line (CEMss), with the mean EC50 for HIV-2ROD9 (EC50 of 0.14 nM) being 30-fold lower than that for HIV-1NL4-3 (EC50 of 4.2 nM)[1].
BMS-986001 also exhibits full activity against HIV-2 variants whose genomes encoded the single amino acid changes K65R and Q151M in reverse transcriptase[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 634907-30-5
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Appearance Solid
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분자량 248.24
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화학식 C12H12N2O4
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Color Light yellow to yellow
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SMILES
C#C[C@@]1(O[C@](N(C=C2C)C(NC2=O)=O)([H])C=C1)CO
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Synonyms
Festinavir; BMS-986001; OBP-601
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
용액&용해도
DMSO : 52 mg/mL (209.48 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 10 mg/mL (40.28 mM; ultrasonic and warming and heat to 60°C)
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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: ≥ 2.83 mg/mL (11.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (28.3 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: ≥ 2.83 mg/mL (11.40 mM); Clear solution
This protocol yields a clear solution of ≥ 2.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (28.3 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.
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.
순도&문서
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Data Sheet (278 KB)
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SDS (419 KB)
- English - EN (419 KB)
- Français - FR (419 KB)
- Deutsch - DE (419 KB)
- Norwegian - NO (419 KB)
- Español - ES (419 KB)
- Swedish - SV (419 KB)
- Italian - IT (419 KB)
- Korean - KR (419 KB)
- Portuguese - PT (419 KB)
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Handling Instructions (2659 KB)
References
[1]. Robert A Smith, et al. The Nucleoside Analog BMS-986001 Shows Greater In Vitro Activity Against HIV-2 Than Against HIV-1. Antimicrob Agents Chemother. 2015 Dec;59(12):7437-46. [Content Brief]
[2]. Long Yuan, et al. Dried Blood Spot Analysis Without Dilution: Application to the LC-MS/MS Determination of BMS-986001 in Rat Dried Blood Spot. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:201-9. [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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 4.0284 mL | 20.1420 mL | 40.2839 mL | 100.7098 mL |
| 5 mM | 0.8057 mL | 4.0284 mL | 8.0568 mL | 20.1420 mL | |
| 10 mM | 0.4028 mL | 2.0142 mL | 4.0284 mL | 10.0710 mL | |
| 15 mM | 0.2686 mL | 1.3428 mL | 2.6856 mL | 6.7140 mL | |
| 20 mM | 0.2014 mL | 1.0071 mL | 2.0142 mL | 5.0355 mL | |
| 25 mM | 0.1611 mL | 0.8057 mL | 1.6114 mL | 4.0284 mL | |
| 30 mM | 0.1343 mL | 0.6714 mL | 1.3428 mL | 3.3570 mL | |
| 40 mM | 0.1007 mL | 0.5035 mL | 1.0071 mL | 2.5177 mL | |
| DMSO | 50 mM | 0.0806 mL | 0.4028 mL | 0.8057 mL | 2.0142 mL |
| 60 mM | 0.0671 mL | 0.3357 mL | 0.6714 mL | 1.6785 mL | |
| 80 mM | 0.0504 mL | 0.2518 mL | 0.5035 mL | 1.2589 mL | |
| 100 mM | 0.0403 mL | 0.2014 mL | 0.4028 mL | 1.0071 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.
Censavudine Related Classifications
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