2. Anti-infection Cell Cycle/DNA Damage
  3. HIV HBV Nucleoside Antimetabolite/Analog
  4. Tenofovir exalidex

Tenofovir exalidex  (Synonyms: CMX-157)

Cat. No.: HY-109014 Assay: 98.70%
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Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV.

For research use only. We do not sell to patients.

Tenofovir exalidex Chemical Structure

Tenofovir exalidex Chemical Structure

CAS No. : 911208-73-6

Size Price Stock Quantity
5 mg USD 115 In-stock
10 mg USD 170 In-stock
25 mg USD 330 In-stock
50 mg USD 500 In-stock
100 mg USD 750 Get quote
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Based on 1 publication(s) in Google Scholar

Tenofovir exalidex Related Antibodies

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  • Purity & Documentation

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Description

Tenofovir exalidex (CMX157) is a lipid conjugate of the acyclic nucleotide analog Tenofovir with activity against both wild-type and antiretroviral drug-resistant HIV strains, including multidrug nucleoside/nucleotide analog-resistant viruses. Tenofovir exalidex is active against all major subtypes of HIV-1 and HIV-2 in fresh human PBMCs and against all HIV-1 strains evaluated in monocyte-derived macrophages, with EC50s ranging between 0.2 and 7.2 nM. CMX157 is orally available and has no apparent toxicity. Tenofovir exalidex also shows antiviral activity against HBV[1][2][3].

IC50 & Target

HIV-1

 

HIV-2

 

In Vitro

Tenofovir exalidex is consistently >300-fold more active than Tenofovir against multiple viruses in several different cell systems. Tenofovir exalidex will be effective against MNR mutants, including those that are unresponsive to all currently available NRTIs. Notably, the average EC50 in PBMCs for CMX157 against a panel of 27 wild-type HIV-1 isolates representing group M subtypes A to G and group O was 2.6 nM (range, 0.2 to 7.2 nM)[1].
Tenofovir exalidex exerts its therapeutic actions by inhibiting HBV polymerase-mediated HBV DNA elongation, but there is no known binding of cyclophilins to HBV polymerase nor participation of cyclophilins in DNA elongation. The combinational effect of CRV431 (host-targeting) and Tenofovir exalidex (direct-acting) on HBV DNA production is more consistent with the two compounds acting on distinct steps of the HBV life cycle[3].

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

Tenofovir exalidex Related Antibodies
In Vivo

Tenofovir exalidex (Sprague-Dawley rats) is orally available and has no apparent toxicity when given orally to rats for 7 days at doses of 10, 30, or 100 mg/kg/day[2]. Tenofovir exalidex (5-10 mg/kg; oral gavage; daily for a period of 16 days) decreases liver HBV DNA levels dose-dependently[3].

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

Animal Model: Female transgenic mice HBV transgenic Tg05 mice (C57BL/6)[1]
Dosage: 5 mg/kg, 10 mg/kg
Administration: Oral gavage; daily for a period of 16 days
Result: The reductions in HBV DNA were 55% and 97% for low-dose (5 mg/kg/day) and high-dose (10 mg/kg/day), respectively.
Clinical Trial
Molecular Weight

569.72

Formula

C28H52N5O5P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

NC1=C2N=CN(C[C@H](OCP(O)(OCCCOCCCCCCCCCCCCCCCC)=O)C)C2=NC=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (175.52 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.7552 mL 8.7762 mL 17.5525 mL
5 mM 0.3510 mL 1.7552 mL 3.5105 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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    90% Corn Oil

    Solubility: ≥ 2 mg/mL (3.51 mM); Clear solution

    This protocol yields a clear solution of ≥ 2 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Purity & Documentation
References

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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.7552 mL 8.7762 mL 17.5525 mL 43.8812 mL
5 mM 0.3510 mL 1.7552 mL 3.5105 mL 8.7762 mL
10 mM 0.1755 mL 0.8776 mL 1.7552 mL 4.3881 mL
15 mM 0.1170 mL 0.5851 mL 1.1702 mL 2.9254 mL
20 mM 0.0878 mL 0.4388 mL 0.8776 mL 2.1941 mL
25 mM 0.0702 mL 0.3510 mL 0.7021 mL 1.7552 mL
30 mM 0.0585 mL 0.2925 mL 0.5851 mL 1.4627 mL
40 mM 0.0439 mL 0.2194 mL 0.4388 mL 1.0970 mL
50 mM 0.0351 mL 0.1755 mL 0.3510 mL 0.8776 mL
60 mM 0.0293 mL 0.1463 mL 0.2925 mL 0.7314 mL
80 mM 0.0219 mL 0.1097 mL 0.2194 mL 0.5485 mL
100 mM 0.0176 mL 0.0878 mL 0.1755 mL 0.4388 mL
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Tenofovir exalidex Related Classifications

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 exalidex911208-73-6CMX-157CMX157CMX 157HIVHBVNucleoside Antimetabolite/AnalogHuman immunodeficiency virusHepatitis B virusnucleotideanalogPBMCmonocytederivedmacrophagesoralresistantsubtypesInhibitorinhibitorinhibit

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