(Rac)-Tenofovir
(Rac)-Tenofovir ((Rac)-GS 1278; (Rac)-PMPA) is an isomer of Tenofovir (HY-13910). Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B (HBV).
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- CAS No.: 107021-12-5
- Formule: C9H14N5O4P
- Masse moléculaire:287.21
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Stockage:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Activité biologique
Description
In Vitro
(Rac)-Tenofovir is an isomer of Tenofovir (HY-13910). Tenofovir displays cytotoxicity against HK-2 cells, with IC50 values of 9.21 μM at 48 h and 2.77 μM at 72 h determined by MTT assay. It reduces intracellular ATP levels, elevates oxidative stress and protein carbonylation, and triggers mitochondria-mediated apoptosis in HK-2 cells[1].
(Rac)-Tenofovir is an isomer of Tenofovir. Tenofovir formulated with M48U1 in 0.25% HEC inhibits the replication of R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and suppresses a panel of laboratory HIV-1 strains and patient-derived primary HIV-1 isolates. The combined formulation of Tenofovir and M48U1 in 0.25% HEC delivers synergistic antiretroviral activity against R5-tropic HIV-1BaL infection and exhibits no cytotoxicity toward PBMCs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
(Rac)-Tenofovir is an isomer of Tenofovir. Tenofovir Disoproxil Fumarate (50-300 mg/kg) significantly reduces HIV transmission in BLT mice[3].
(Rac)-Tenofovir is an isomer of Tenofovir. Tenofovir Disoproxil Fumarate (0.5-5.0 mg/kg/day, p.o.) induces a dose-dependent decrease in serum viremia in marmots with chronic WHV infection and is safe and effective in a marmot model of chronic HBV infection[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 107021-12-5
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Appearance Solid
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Masse moléculaire 287.21
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Formule C9H14N5O4P
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Color White to off-white
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SMILES
O=P(O)(COC(CN1C=NC2=C1N=CN=C2N)C)O
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Synonyms
(Rac)-GS 1278; (Rac)-PMPA
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Pureté et documentation
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Fiche technique (271 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Murphy RA, et al. Establishment of HK-2 Cells as a Relevant Model to Study Tenofovir-Induced Cytotoxicity. Int J Mol Sci. 2017 Mar 1;18(3). [Content Brief]
[2]. Musumeci G, et al. M48U1 and Tenofovir combination synergistically inhibits HIV infection in activated PBMCs and human cervicovaginal histocultures. Sci Rep. 2017 Feb 1;7:41018. [Content Brief]
[3]. Wahl A, et al. Predicting HIV Pre-exposure Prophylaxis Efficacy for Women using a Preclinical Pharmacokinetic-Pharmacodynamic In Vivo Model. Sci Rep. 2017 Feb 1;7:41098. [Content Brief]
[4]. Menne S, Cote PJ, Korba BE, Antiviral effect of oral administration of tenofovir disoproxil fumarate in woodchucks with chronic woodchuck hepatitis virus infection. Antimicrob Agents Chemother. 2005 Jul;49(7):2720-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
(Rac)-Tenofovir Related Classifications
HY-13910C Related Classifications
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