Art. -Nr.: HY-109014

Tenofovir exalidex

Name: Tenofovir exalidex
Brand: MedChemExpress
SKU: HY-109014
Price: 115.00 USD
Availability: InStock
Rating: 5 (1 reviews)

(Synonyms: CMX-157)

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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.

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Reinheit : 99.82%
CAS. Nr.: 911208-73-6
Formel: C₂₈H₅₂N₅O₅P
Molecular Weight:569.72

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

Tenofovir exalidex Chemical Structure

CAS. Nr.: 911208-73-6

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

HIV-1

HIV-2

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Cellular Effect

Cell Line	Type	Value	Description	References
Bone marrow cell	CC₅₀	2.5 μM Compound: 1, CMX157	Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay Cytotoxicity against human bone marrow cells after 24 hrs by GM-CFU assay	[PMID: 20439609]
Bone marrow cell	CC₅₀	4.6 μM Compound: 1, CMX157	Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay Cytotoxicity against human bone marrow cells after 24 hrs by BFU-E assay	[PMID: 20439609]
HepG2	EC₅₀	>18.8 μM Compound: CMX157, HDP-(R)-PMPA	Cytotoxicity against human HepG2 cells by MTS assay Cytotoxicity against human HepG2 cells by MTS assay	[PMID: 17646420]
HepG2 2.2.15	EC₅₀	>300 μM Compound: CMX157, HDP-(R)-PMPA	Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red uptake assay Cytotoxicity against human HepG2(2.2.15) cells after 24 hrs by neutral red uptake assay	[PMID: 17646420]
HepG2 2.2.15	EC₅₀	1.6 μM Compound: CMX157, HDP-(R)-PMPA	Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as viral DNA levels treated for 9 days measured after 24 hrs Antiviral activity against HBV in human HepG2(2.2.15) cells assessed as viral DNA levels treated for 9 days measured after 24 hrs	[PMID: 17646420]
MT2	CC₅₀	54 μM Compound: CMX157, HDP-(R)-PMPA	Cytotoxicity against human MT2 cells Cytotoxicity against human MT2 cells	[PMID: 17646420]
MT2	EC₅₀	<1 x 10^-5 μM Compound: CMX157, HDP-(R)-PMPA	Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of p24 antigen production by ELISA Antiviral activity against HIV1 LAI in human MT2 cells assessed as inhibition of p24 antigen production by ELISA	[PMID: 17646420]
PBMC	CC₅₀	144 μM Compound: CMX157, HDP-(R)-PMPA	Cytotoxicity against human PBMC by XTT assay Cytotoxicity against human PBMC by XTT assay	[PMID: 17646420]
PBMC	CC₅₀	>100 μM Compound: 1	Cytotoxicity against human PBMC assessed as reduction in cell viability by XTT assay Cytotoxicity against human PBMC assessed as reduction in cell viability by XTT assay	[PMID: 27405794]

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. Further protocols information, click here.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 911208-73-6
Appearance Solid
Molecular Weight 569.72
Formel C₂₈H₅₂N₅O₅P
Color White to off-white
SMILES

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

CMX-157
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

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)

Ethanol : 1 mg/mL (1.76 mM; Need ultrasonic)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7552 mL

8.7762 mL

17.5525 mL

5 mM

0.3510 mL

1.7552 mL

3.5105 mL

10 mM

0.1755 mL

0.8776 mL

1.7552 mL

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

All Signal Pathway Related

Research Protocol for Infectious Diseases
Infectious-disease experiments test how pathogens interact with host barriers, innate immune receptors, inflammatory signaling, pathogen replication, and tissue injury; pattern-recognition receptors such as TLRs, RIG-I-like receptors, NOD-like receptors, and inflammasomes detect microbial molecules and activate NF-κB, interferon, and cytokine responses. The central hypothesis is that infection severity reflects the balance between pathogen burden and host response: protective inflammation restricts pathogen growth, whereas excessive or mislocalized inflammation contributes to tissue damage and disease phenotype. Unresolved questions include which host pathways are protective versus pathogenic, why some infection models fail to translate to human disease, and which combined readouts best predict clinically relevant infection outcomes.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (288 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Lanier ER, et al. Development of hexadecyloxypropyl tenofovir (CMX157) for treatment of infection caused by wild-type and nucleoside/nucleotide-resistant HIV. Antimicrob Agents Chemother. 2010;54(7):2901-2909. [Content Brief]

[2]. Gallay P, et al. The cyclophilin inhibitor CRV431 inhibits liver HBV DNA and HBsAg in transgenic mice. PLoS One. 2019;14(6):e0217433. Published 2019 Jun 10. [Content Brief]

[3]. Painter GR, et al. Evaluation of hexadecyloxypropyl-9-R-[2-(Phosphonomethoxy)propyl]- adenine, CMX157, as a potential treatment for human immunodeficiency virus type 1 and hepatitis B virus infections [published correction appears in Antimicrob Agents Chemother. 2007 Dec;51(12):4538]. Antimicrob Agents Chemother. 2007;51(10):3505-3509. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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
Ethanol / DMSO	1 mM	1.7552 mL	8.7762 mL	17.5525 mL	43.8812 mL
DMSO	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

Alle HIV Isoform-spezifische Produkte anzeigen