| Size | Price | |
|---|---|---|
| 500mg | ||
| 1g | ||
| Other Sizes |
Purity: ≥98%
| Targets |
HBV; HIV-1/2 nucleotide reverse transcriptase
Targets HIV reverse transcriptase and Hepatitis B virus polymerase as a nucleotide reverse transcriptase inhibitor. Inhibits viral RNA replication, ultimately leading to reduced viral load in infected patients. |
|---|---|
| ln Vitro |
Tenofovir alafenamide (TAF) can be considered a new prodrug of tenofovir (TFV), as successor of tenofovir disoproxil fumarate (TDF). It is in vivo as potent against human immunodeficiency virus (HIV) at a 30-fold lower dose (10mg) than TDF (300mg). TAF has been approved in November 2015 (in the US and EU), as a single-tablet regimen (STR) containing 150mg elvitegravir (E), 150mg cobicistat (C), 200mg emtricitabine [(-)FTC] (F) and 10mg TAF, marketed as Genvoya®, on 01 March 2016 in the US as an STR containing 25mg rilpivirine (R), 200mg F and 25mg TAF, marketed as Odefsey®, and on 4 April 2016 in the US, as an STR containing 200mg F and 25mg TAF, marketed as Descovy®, for the treatment of HIV infections. STR combinations containing TAF and emtricitabine could be paired with a range of third agents, for example, darunavir and cobicistat. TAF has a much lower risk of kidney toxicity or bone density changes than TDF, and also offers long-term potential in the pre-exposure prophylaxis (PrEP) of HIV infections. TAF is specifically accumulated in lymphatic tissue, and in the liver, and hence also holds great potential for the treatment of hepatitis B virus (HBV) infections. Akin to TDF, TAF is converted intracellularly to TFV. Its active diphosphate metabolite (TFVpp) is targeted at the RNA-dependent DNA polymerase (reverse transcriptase) of either HIV or HBV[1].
Potent antiviral activity by interfering with viral RNA replication. Demonstrates activity against HIV and chronic Hepatitis B. Exhibits nucleotide reverse transcriptase inhibitor activity. Specific EC50 values against HIV and HBV are characteristic of tenofovir-based antivirals in the low nanomolar range. |
| ln Vivo |
Used potentially for the treatment of HIV and chronic Hepatitis B infection. Demonstrates potent antiviral activity by reducing viral load in infected patients. Used in research aimed at developing effective therapeutic strategies against retroviral infections. Clinically used as part of antiretroviral therapy for HIV and hepatitis B treatment.
|
| Enzyme Assay |
Reverse transcriptase inhibition assays are performed using purified HIV reverse transcriptase or HBV polymerase. The enzyme is incubated with a template-primer, dNTPs, and varying concentrations of Tenofovir disoproxil aspartate (or its active metabolite tenofovir). The incorporation of radiolabeled or fluorescent nucleotides is measured, and the IC50 for inhibition is determined.
|
| Cell Assay |
Cell-based assays are performed using HIV-infected or HBV-infected cell lines. Cells are treated with Tenofovir disoproxil aspartate, and viral replication is measured by quantifying viral RNA or DNA levels using qPCR or ELISA. Cytotoxicity is assessed in uninfected cells using MTT or CellTiter-Glo assays to determine the selectivity index.
|
| Animal Protocol |
In vivo efficacy is evaluated in animal models of HIV or HBV infection or in clinical studies. Tenofovir disoproxil aspartate is administered orally, and viral load in plasma is measured by qPCR. The reduction in viral load is quantified to assess efficacy. In humans, it is used as part of antiretroviral therapy with established clinical efficacy.
|
| References |
De Clercq E. Tenofovir alafenamide (TAF) as the successor of tenofovir disoproxil fumarate (TDF). Biochem Pharmacol. 2016 Apr 29. pii: S0006-2952(16)30069-7. doi: 10.1016/j.bcp.2016.04.015.
|
| Molecular Formula |
C23H37N6O14P
|
|---|---|
| Molecular Weight |
652.55
|
| Exact Mass |
652.2105
|
| Elemental Analysis |
C, 42.40; H, 5.88; N, 15.05; O, 31.92; P, 4.75
|
| CAS # |
1571075-19-8
|
| Related CAS # |
201341-05-1 (free);202138-50-9 (fumarate);147127-20-6 (Tenofovir);206184-49-8 (hydrate); 379270-37-8 (alafenamide); 1571075-19-8 (aspartate);
|
| PubChem CID |
73291783
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
0
|
| tPSA |
286Ų
|
| Hydrogen Bond Donor Count |
4
|
| Hydrogen Bond Acceptor Count |
19
|
| Rotatable Bond Count |
20
|
| Heavy Atom Count |
44
|
| Complexity |
831
|
| Defined Atom Stereocenter Count |
2
|
| SMILES |
N[C@@H](CC(O)=O)C(O)=O.O=C(OC(C)C)OCOP(OCOC(OC(C)C)=O)(CO[C@H](C)CN1C=NC2=C(N)N=CN=C12)=O
|
| InChi Key |
WHQLGZSDBQPTHD-KJTVYDLOSA-N
|
| InChi Code |
InChI=1S/C19H30N5O10P.C4H8N2O3/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)245-2(4(8)9)1-3(6)7/h7-8,12-14H,6,9-11H2,1-5H3,(H2,20,21,22)2H,1,5H2,(H2,6,7)(H,8,9)/t14-2-/m10/s1
|
| Chemical Name |
(R)-(((((1-(6-amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphoryl)bis(oxy))bis(methylene)
diisopropyl bis(carbonate) L-asparaginate
|
| Synonyms |
Tenofovir disoproxil aspartate; CKD-390; CKD 390; Bis-POC-PMPA aspartate; GS 4331 aspartate; CKD-390; 1571075-19-8; F06G7ZBB70; Tenofovir disoproxil aspartate [WHO-DD]; UNII-F06G7ZBB70; CKD390.
|
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5324 mL | 7.6622 mL | 15.3245 mL | |
| 5 mM | 0.3065 mL | 1.5324 mL | 3.0649 mL | |
| 10 mM | 0.1532 mL | 0.7662 mL | 1.5324 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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