| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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Dexelvucitabine (INCB-8721; PSI-5582; YZ-817; DPC-817; DOC-817) is a novel and potent nucleoside reverse transcriptase inhibitor that has failed clinical trials for the management of HIV infection.
| 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].
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| References |
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| Additional Infomation |
Dexelvucitabine has been used in trials studying the treatment of HIV Infections and Human Immunodeficiency Virus.
Dexelvucitabine is a nucleoside reverse transcriptase inhibitor analog of cytosine. |
| Molecular Formula |
C9H10FN3O3
|
|---|---|
| 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
|
| 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
|
| 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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