2. Anti-infection
  3. HIV Reverse Transcriptase
  4. Tenofovir alafenamide

Tenofovir alafenamide  (Synonyms: テノホビル アラフェナミド; GS-7340)

製品番号: HY-15232 純度: 99.93%
COA 取扱説明書 Technical Support

Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.

商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。

Tenofovir alafenamide

Tenofovir alafenamide 構造式

CAS 番号 : 379270-37-8

容量 価格（税別） 在庫状況 数量
>無料サンプル (0.1 - 0.2 mg)   今すぐ申し込む  
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 58 在庫あり
Solution
10 mM * 1 mL in DMSO USD 58 在庫あり
Solid
5 mg $55 在庫あり
10 mg $77 在庫あり
25 mg $105 在庫あり
50 mg $154 在庫あり
100 mg $209 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

This product is a controlled substance and not for sale in your territory.

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Based on 12 publication(s) in Google Scholar

Other Forms of Tenofovir alafenamide:

Tenofovir alafenamide 関連抗体

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製品説明

Tenofovir alafenamide (GS-7340) is an investigational oral proagent of Tenofovir. Tenofovir is a HIV-1 nucleotide reverse transcriptase inhibitor.

IC50 & Target

HIV-1

 

HIV-2

 

Cellular Effect
Cell Line Type Value Description References
HepG2 2.2.15 CC50
>100 μM
Compound: GS-7340
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability treated from day 2 to day 8 by CellTiter-Blue reagent based fluorescence analysis
Cytotoxicity against human HepG2.2.15 cells assessed as reduction in cell viability treated from day 2 to day 8 by CellTiter-Blue reagent based fluorescence analysis
[PMID: 38246114]
MT2 CC50
40 μM
Compound: GS 7340
Cytotoxicity against human MT2 cells
Cytotoxicity against human MT2 cells
[PMID: 24686012]
MT2 EC50
0.005 μM
Compound: GS 7340
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
Antiviral activity against Human immunodeficiency virus 1 3B infected in human MT2 cells assessed as inhibition of virus-induced giant cell formation after 4 to 5 days by microscopic analysis
[PMID: 24686012]
MT2 EC50
5 nM
Compound: Tenofovir alafenamide
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathic effect after 5 days by XTT assay
Antiviral activity against HIV1 3B infected in human MT2 cells assessed as protection against virus-induced cytopathic effect after 5 days by XTT assay
[PMID: 27748590]
PBMC CC50
1.32 μM
Compound: TAF
Cytotoxicity against human PHA-stimulated PBMC assessed as cell viability by tetrazolium dye assay
Cytotoxicity against human PHA-stimulated PBMC assessed as cell viability by tetrazolium dye assay
[PMID: 28682067]
体外実験

Tenofovir alafenamide (GS-7340) antiviral activities are similar across all cell types, ranging from 5 to 7 nM, while the CC50 varies from 4.7 to 42 μM for MT-4 and MT-2 cells, respectively. The antiviral activity of TAF is evaluated against a panel of HIV-1 and HIV-2 isolates, including HIV-1 group M subtypes A to G, as well as group N and O isolates. Overall, for the 29 primary HIV-1 isolates tested in PBMCs, TAF EC50s range from 0.1 to 12 nM, with a mean EC50 of 3.5 nM compared to a mean EC50 of 11.8 nM for AZT, which is used as an internal control. For the HIV-2 isolates, the mean EC50s are 1.8 nM for TAF and 6.4 nM for AZT[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Tenofovir alafenamide 関連抗体
体内実験

Tenofovir alafenamide (GS-7340) hemifumarate is an amidate prodrug of Tenofovir with good oral bioavailability and increases plasma stability compared to Tenofovir disoproxil fumarate (TDF)[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
臨床実験
分子量

476.47

分子式

C21H29N6O5P
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

NC1=NC=NC2=C1N=CN2C[C@@H](C)OC[P@](OC3=CC=CC=C3)(N[C@@H](C)C(OC(C)C)=O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : ≥ 31 mg/mL (65.06 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : 6.67 mg/mL (14.00 mM; Need ultrasonic)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0988 mL 10.4938 mL 20.9877 mL
5 mM 0.4198 mL 2.0988 mL 4.1975 mL
10 mM 0.2099 mL 1.0494 mL 2.0988 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始）

C1

×
体積 （開始）

V1

=
濃度 （終了）

C2

×
体積 （終了）

V2

体内:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (4.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (4.37 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  PBS

    Solubility: 40 mg/mL (83.95 mM); Clear solution; Need ultrasonic

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション

純度: 99.93%

COA (252 KB) HNMR (178 KB) RP-HPLC (257 KB) LCMS (93 KB)

取扱説明書 (2659 KB)
参考文献

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.0988 mL 10.4938 mL 20.9877 mL 52.4692 mL
5 mM 0.4198 mL 2.0988 mL 4.1975 mL 10.4938 mL
10 mM 0.2099 mL 1.0494 mL 2.0988 mL 5.2469 mL
DMSO 15 mM 0.1399 mL 0.6996 mL 1.3992 mL 3.4979 mL
20 mM 0.1049 mL 0.5247 mL 1.0494 mL 2.6235 mL
25 mM 0.0840 mL 0.4198 mL 0.8395 mL 2.0988 mL
30 mM 0.0700 mL 0.3498 mL 0.6996 mL 1.7490 mL
40 mM 0.0525 mL 0.2623 mL 0.5247 mL 1.3117 mL
50 mM 0.0420 mL 0.2099 mL 0.4198 mL 1.0494 mL
60 mM 0.0350 mL 0.1749 mL 0.3498 mL 0.8745 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Tenofovir alafenamide Related Classifications

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tenofovir alafenamide379270-37-8GS-7340GS7340GS 7340HIVReverse TranscriptaseHuman immunodeficiency virusInhibitorinhibitorinhibit

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製品名:
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製品番号:
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