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Tenofovir exalidex

Catalog No. T28946 CAS 911208-73-6

Synonyms: Tenofovir, HDP-Tenofovir, CMX-157, CMX157, CMX 157

Tenofovir exalidex (CMX 157) is a lipid-conjugated acyclic nucleotide analog of Tenofovir, demonstrating efficacy against wild-type and antiretroviral-resistant HIV strains, including those resistant to multiple nucleoside/nucleotide analogs. It effectively inhibits all major HIV-1 and HIV-2 subtypes in fresh human PBMCs, as well as all evaluated HIV-1 strains in monocyte-derived macrophages, displaying EC50 values between 0.2 and 7.2 nM. Oral administration of CMX157 shows no apparent toxicity. Additionally, Tenofovir exalidex exhibits antiviral properties against HBV.

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Tenofovir exalidex, CAS 911208-73-6

Pack Size	Availability	Price/USD
1 mg	In stock	$ 39.00
5 mg	In stock	$ 93.00
10 mg	In stock	$ 138.00
25 mg	In stock	$ 229.00
50 mg	In stock	$ 397.00
100 mg	In stock	$ 589.00

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Purity: 99.54%

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Description	Tenofovir exalidex (CMX 157) is a lipid-conjugated acyclic nucleotide analog of Tenofovir, demonstrating efficacy against wild-type and antiretroviral-resistant HIV strains, including those resistant to multiple nucleoside/nucleotide analogs. It effectively inhibits all major HIV-1 and HIV-2 subtypes in fresh human PBMCs, as well as all evaluated HIV-1 strains in monocyte-derived macrophages, displaying EC50 values between 0.2 and 7.2 nM. Oral administration of CMX157 shows no apparent toxicity. Additionally, Tenofovir exalidex exhibits antiviral properties against HBV.
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[1]. 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[3].
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].

Synonyms	Tenofovir, HDP-Tenofovir, CMX-157, CMX157, CMX 157
Molecular Weight	569.72
Formula	C28H52N5O5P
CAS No.	911208-73-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: Insoluble

References and Literature

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. 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. 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. Antimicrob Agents Chemother. 2007 Oct;51(10):3505-9. 4. Painter GR, Almond MR, Trost LC, Lampert BM, Neyts J, De Clercq E, Korba BE, Aldern KA, Beadle JR, Hostetler KY. 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. Antimicrob Agents Chemother. 2007 Oct;51(10):3505-9. Epub 2007 Jul 23. Erratum in: Antimicrob Agents Chemother. 2007 Dec;51(12):4538. PubMed PMID: 17646420; PubMed Central PMCID: PMC2043283.

Related compound libraries

This product is contained In the following compound libraries：

Drug Repurposing Compound Library Bioactive Compound Library Anti-Viral Compound Library Clinical Compound Library Bioactive Compounds Library Max

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Keywords

Tenofovir exalidex 911208-73-6 Immunology/Inflammation Antiviral Tenofovir HDP-Tenofovir CMX-157 CMX157 CMX 157 inhibitor inhibit

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