| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| Other Sizes |
|
| ln Vitro |
3'-azido-2',3'-dideoxyuridine suppresses HIV replication in HIV-1-infected PBMC with a median effective concentration of 0.18-0.46 μM[2]. Infected human T cell lines MT-4 and ATH8, 3'-azido-2',3'-dideoxyuridine reduces HIV-mediated cell damage at a median effective concentration of 0.4 µM [3]. Cells break down 3'-azido-2',3'-dideoxyuridine in a stepwise manner to produce monophosphate, diphosphate, and triphosphate borrowing materials [3].
|
|---|---|
| ln Vivo |
The pharmacokinetic properties of 3′-Azido-2′,3′-dideoxyuridine (25–100 mg/kg, intravenous injection or gavage, once) are favorable [3]. 3′-Azido-2′ pharmacokinetic characteristics and 3′-dideoxyuridine effects in male Sprague-Dawley rats [3]. IV (25 mg/kg) IV (100 mg/kg) PO (25 mg/kg) PO (100 mg/kg) Cmax (μg/mL) 9.2±1.9 41±15 Tmax (h) 0.38±0.13 0.63±0.22 AUC (μg/mL*h) 19±1.2 156±7.0 12±0.54 70±13 CLT (L/h/kg) 1.4±0.2 0.70±0.09 CLR (L/h/kg) 0.90±0.27 0.43±0.12 t1/ 2 (h) 0.5±0.0 0.68±0.1 1.0±0.3 1.1±0.4 Vss (L/kg) 0.78±0.26 0.34±0.11 F (%) 60 46
|
| Animal Protocol |
Animal/Disease Models: Adult male SD (SD (Sprague-Dawley)) rat (300-400 g) [3]
Doses: 25, 100 mg/kg Route of Administration: intravenous (iv) (iv)bolus or po (oral gavage) (pharmacokinetic/PK/PK analysis) Experimental Results: 3'-azido-2',3'-dideoxyuridine at 25 and oral bioavailability estimates at the 100 mg/kg dose averaged 53%. |
| References |
|
| Additional Infomation |
Navuridine is a dideoxyuridine inhibitor of HIV reverse transcriptase that is related to zidovudine. Navuridine exhibits a relatively short half-life and incomplete oral bioavailability and has not been developed into a clinical drug.
|
| Molecular Formula |
C9H11N5O4
|
|---|---|
| Molecular Weight |
253.218
|
| Exact Mass |
253.081
|
| CAS # |
84472-85-5
|
| PubChem CID |
55262
|
| Appearance |
White to off-white solid powder
|
| Density |
1.357 g/cm
|
| Melting Point |
161-163ºC
|
| LogP |
-1.12
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
6
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
18
|
| Complexity |
444
|
| Defined Atom Stereocenter Count |
3
|
| SMILES |
C1[C@@H]([C@H](O[C@H]1N2C=CC(=O)NC2=O)CO)N=[N+]=[N-]
|
| InChi Key |
ZSNNBSPEFVIUDS-SHYZEUOFSA-N
|
| InChi Code |
InChI=1S/C9H11N5O4/c10-13-12-5-3-8(18-6(5)4-15)14-2-1-7(16)11-9(14)17/h1-2,5-6,8,15H,3-4H2,(H,11,16,17)/t5-,6+,8+/m0/s1
|
| Chemical Name |
1-[(2R,4S,5S)-4-azido-5-(hydroxymethyl)oxolan-2-yl]pyrimidine-2,4-dione
|
| Synonyms |
CS-87; AzUrd; AZdU
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~987.32 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.21 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 20.8 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: ≥ 2.08 mg/mL (8.21 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 20.8 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: ≥ 2.08 mg/mL (8.21 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 | 3.9491 mL | 19.7457 mL | 39.4914 mL | |
| 5 mM | 0.7898 mL | 3.9491 mL | 7.8983 mL | |
| 10 mM | 0.3949 mL | 1.9746 mL | 3.9491 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
