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| 1mg |
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| 5mg |
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| 10mg |
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| 25mg |
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| Targets |
Dexelvucitabine targets HIV-1 reverse transcriptase. As a nucleoside analog, it is incorporated into viral DNA, causing chain termination and inhibiting viral replication. It is effective against HIV-1 strains resistant to thymidine analogs and those harboring the M184V mutation.
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| ln Vitro |
In vitro, dexelvucitabine is a potent nucleoside reverse transcriptase inhibitor. It inhibits viral replication in both wild-type and drug-resistant HIV-1 isolates, including those harboring the M184V mutation and thymidine analog mutations (TAMs). It shows efficacy against HIV-1-resistant viruses.
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| ln Vivo |
In monkeys, dexcitabine (Reverset; d-d4FC; 33.3 mg/kg intravenously or orally) had distribution and elimination half-lives of 0.7 and 3.6 hours, respectively (t1/2α and t1/2β, respectively). The range of Cmax is 21.1–47.5 μM [2]. In prairie dogs, dexcitabine had a lengthy half-life (4.71 and 10.75 hours following oral and intravenous methods, respectively) and favorable pharmacokinetic characteristics [2].
In vivo, dexelvucitabine is orally active. It exhibits efficacy against HIV-1 strains resistant to thymidine analogs and those harboring the M184V mutation. It is a 2′-deoxycytidine antiretroviral agent. The compound has been studied for the treatment of HIV-1 infection. |
| Enzyme Assay |
In vitro enzyme assays for dexelvucitabine measure its inhibition of HIV-1 reverse transcriptase. The enzyme is incubated with template/primer, nucleotides, and varying concentrations of the compound. DNA synthesis is measured by incorporation of radiolabeled nucleotides. IC50 values are calculated from dose-response curves.
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| Cell Assay |
In vitro cell-based assays for dexelvucitabine use HIV-1-infected cell lines. Cells are treated with serial dilutions of the compound, and viral replication is measured by quantifying viral RNA or antigen production. The EC50 for inhibition of viral replication is determined from dose-response curves. Activity against drug-resistant strains is assessed using resistant virus isolates.
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| Animal Protocol |
In vivo animal models for dexelvucitabine include models of HIV-1 infection. The compound is administered orally, and its effects on viral load and immune function are evaluated. Pharmacokinetic studies measure drug exposure and tissue distribution. Resistance studies assess activity against drug-resistant virus.
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| ADME/Pharmacokinetics |
Dexelvucitabine has a molecular formula of C₉H₁₀FN₃O₃ and a molecular weight of 227.19 g/mol. It is orally active. It is also known as 2',3'-Dideoxy-2',3'-didehydro-5-fluoro-cytidine. The compound is stored under appropriate conditions for research use.
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| Toxicity/Toxicokinetics |
The toxicity profile of dexelvucitabine is characterized in preclinical safety studies. As an NRTI, common adverse effects may include mitochondrial toxicity. The compound is for research use only and is not approved for clinical use. Appropriate safety precautions should be taken during handling.
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| References |
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| Additional Infomation |
Dexelvucitabine has been used in trials to investigate its use in the treatment of HIV infection and human immunodeficiency virus. Dexelvucitabine is a cytosine nucleoside reverse transcriptase inhibitor analog.
Dexelvucitabine is a potent nucleoside reverse transcriptase inhibitor (NRTI) targeting HIV-1 polymerase. It inhibits viral replication in wild-type and drug-resistant HIV-1 isolates, including those with M184V and thymidine analog mutations. It is a 2′-deoxycytidine antiretroviral agent. Dexelvucitabine is also known as 2',3'-Dideoxy-2',3'-didehydro-5-fluoro-cytidine. |
| Molecular Formula |
C9H10FN3O3
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|---|---|
| Molecular Weight |
227.1954
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| Exact Mass |
227.071
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| Elemental Analysis |
C, 47.58; H, 4.44; F, 8.36; N, 18.50; O, 21.13
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| CAS # |
134379-77-4
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| Related CAS # |
Dideoxycytidinene;7481-88-1
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| PubChem CID |
64973
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| Appearance |
White to off-white solid powder
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| Density |
1.66g/cm3
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| Boiling Point |
394.9ºC at 760mmHg
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| Flash Point |
192.6ºC
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| Vapour Pressure |
7.15E-08mmHg at 25°C
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| Index of Refraction |
1.665
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| LogP |
-1.3
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
16
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| Complexity |
405
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O=C1N=C(N)C(F)=CN1[C@@H]2O[C@H](CO)C=C2
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| InChi Key |
HSBKFSPNDWWPSL-CAHLUQPWSA-N
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| InChi Code |
InChI=1S/C9H10FN3O3/c10-6-3-13(9(15)12-8(6)11)7-2-1-5(4-14)16-7/h1-3,5,7,14H,4H2,(H2,11,12,15)/t5-,7+/m0/s1
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| Chemical Name |
4-amino-5-fluoro-1-[(2R,5S)-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]pyrimidin-2-one
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| Synonyms |
INCB-8721 PSI-5582YZ-817DPC-817 DOC-817 D-D-4FC beta-D-D-4FC Dexelvucitabine
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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) |
DMSO : ~50 mg/mL (~220.08 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (11.00 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (11.00 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (11.00 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.4014 mL | 22.0070 mL | 44.0141 mL | |
| 5 mM | 0.8803 mL | 4.4014 mL | 8.8028 mL | |
| 10 mM | 0.4401 mL | 2.2007 mL | 4.4014 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
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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