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Purity: ≥98%
Tenofovir disoproxil [Bis(POC)-PMPA; GS 4331)] is an antiretroviral drug and prodrug of Tenofovir, acting as a nucleotide reverse transcriptase inhibitor to prevent and treat HIV/AIDS and to treat chronic hepatitis B. The active substance is tenofovir, while tenofovir disoproxil is a prodrug that is used because of its better absorption in the gut.
| ln Vitro |
According to the MTT experiment, tenofovir has a deleterious effect on HK-2 cell viability, with IC50 values of 2.77 μM and 9.21 μM at 48 and 72 hours, respectively. ATP levels in HK-2 cells are lowered by tenofovir. In HK-2 cells, tenofovir (3.0 to 28.8 μM) elevates protein carbonylation and oxidative stress. Furthermore, tenofovir has the ability to cause HK-2 cells to undergo apoptosis, which is brought on by damage to the mitochondria [1]. The replication of R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMC was suppressed by tenofovir and M48U1, which were compounded in 0.25% HEC. Additionally, several laboratory strains and patient-derived HIV-1 isolates were inhibited. In addition to being non-toxic to PBMC, the combination formulation of M48U1 and tenofovir in 0.25% HEC demonstrated synergistic antiretroviral efficacy against R5-tropic HIV-1BaL infection [2].
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| ln Vivo |
In BLT humanized mice, tenofovir disoproxil fumarate (20, 50, 140, or 300 mg/kg) administration resulted in dose-dependent activity during vaginal HIV challenge. HIV transmission in BLT mice is dramatically decreased by tenofovir disoproxil fumarate (50, 140, or 300 mg/kg) [3]. In woodchucks that are chronically infected with WHV, tenofovir disoproxil fumarate (0.5, 1.5, or 5.0 mg/kg/day) causes a dose-dependent decrease in serum viremia. For treating a persistent HBV infection in woodchucks, tenofovir disoproxil fumarate is both safe and efficacious [4].
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| References |
[1]. Murphy RA, et al. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3)
[2]. Musumeci G, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures. Sci Rep. 2017 Feb 1;7:41018 [3]. Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017 Feb 1;7:41098 [4]. Menne S, Cote PJ, Korba BE, Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronic woodchuck hepatitis virus infection. Antimicrob Agents Chemother. 2005 Jul;49(7):2720-8 |
| Molecular Formula |
C19H30N5O10P
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|---|---|
| Molecular Weight |
519.4478
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| Exact Mass |
519.173
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| CAS # |
201341-05-1
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| Related CAS # |
Tenofovir Disoproxil fumarate;202138-50-9
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| SMILES |
NC1=C2C(N(C[C@H](OCP(OCOC(OC(C)C)=O)(OCOC(OC(C)C)=O)=O)C)C=N2)=NC=N1
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| InChi Key |
JFVZFKDSXNQEJW-CQSZACIVSA-N
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| InChi Code |
InChI=1S/C19H30N5O10P/c1-12(2)33-18(25)28-9-31-35(27,32-10-29-19(26)34-13(3)4)11-30-14(5)6-24-8-23-15-16(20)21-7-22-17(15)24/h7-8,12-14H,6,9-11H2,1-5H3,(H2,20,21,22)/t14-/m1/s1
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| Synonyms |
GS 4331GS-4331GS4331Bis(POC)PMPA PMPA prodrug Viread.
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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 : ≥ 38 mg/mL (~73.16 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.00 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 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 (4.00 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 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 (4.00 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 | 1.9251 mL | 9.6256 mL | 19.2511 mL | |
| 5 mM | 0.3850 mL | 1.9251 mL | 3.8502 mL | |
| 10 mM | 0.1925 mL | 0.9626 mL | 1.9251 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
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