Tenofovir exalidex

SKU: orb1699154

Description

Tenofovir exalidex (CMX 157) is a lipid-conjugated prodrug of tenofovir with potent activity against wild-type and drug-resistant HIV-1, HIV-2, and HBV. It demonstrates low nanomolar EC50 values in primary human PBMCs and macrophages, and has shown oral bioavailability with a favorable toxicity profile in preclinical studies, supporting its investigation as a broad-spectrum antiviral agent.

Research Area

Cell Biology, Immunology & Inflammation, Infectious Disease & Virology, Molecular Biology, Protein Biochemistry

Key Properties

• CAS Number: 911208-73-6
• MW: 569.72
• Purity: 99.83%
• Formula: C₂₈H₅₂N₅O₅P
• SMILES: C([C@H](OCP(OCCCOCCCCCCCCCCCCCCCC)(=O)O)C)N1C=2C(N=C1)=C(N)N=CN2
• Target: Nucleoside Antimetabolite/Analog,HBV,HIV Protease,Antiviral
• Solubility: DMSO:Insoluble

Bioactivity

• In Vivo:
  Tenofovir exalidex (Sprague-Dawley rats) is orally available and shows no apparent toxicity at 10, 30, or 100 mg/kg/day doses for 7 days. It decreases liver HBV DNA levels dose-dependently when administered via oral gavage at 5-10 mg/kg daily for 16 days.
• In Vitro:
  Tenofovir exalidex demonstrates over 300-fold greater activity than Tenofovir against a broad spectrum of viruses across various cell systems and shows efficacy against MNR mutants resistant to all current NRTIs. Particularly, in PBMCs, CMX157 exhibits an average EC50 of 2.6 nM (ranging from 0.2 to 7.2 nM) against 27 wild-type HIV-1 isolates from group M subtypes A to G and group O. The mechanism of action involves inhibiting HBV polymerase to prevent HBV DNA elongation, without the involvement of cyclophilins in this process. Moreover, the combination of CRV431 (host-targeting) and Tenofovir exalidex (direct-acting) leads to a synergistic effect in inhibiting HBV DNA synthesis, indicating their actions target different stages of the HBV life cycle.

Storage & Handling

• Storage: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

HDP-Tenofovir, Antiviral, CMX 157, CMX157, CMX-157, Tenofovir exalidex

Compound Identifiers

PubChem CID

23628250