Tenofovir hydrate

• CAT Number: I002586
• CAS Number: 206184-49-8
• Molecular Formula: C9H16N5O5P
• Molecular Weight: 305.23
• Purity: ≥95%
• Synonyms: [(2R)-1-(6-aminopurin-9-yl)propan-2-yl]oxymethylphosphonic acid;hydrate
• Target: HIV
• Solubility: 10 mM in DMSO
• Storage: Store at -20C
• IC50: 0.5-2.2 uM (HIV-1); 1.6-4.9 uM (HIV-2) [1]

Tenofovir(GS 1278, PMPA) is an antiretroviral drug known as nucleotide analogue reverse transcriptase inhibitors (NRTIs), which block reverse transcriptase, a crucial virus enzyme in HIV-1 and HBV.IC50 Value:0.5-2.2 uM (HIV-1); 1.6-4.9 uM (HIV-2) [1]Target: NRTIsin vitro: Tenofovir hydrate reduces the viral cytopathic effect of HIV-1(IIIB), HIV-2(ROD) and HIV(EHO) with EC50 of 1.15 μg/mL, 1.12 μg/mL and 1.05 μg/mL in MT-4 cells. Tenofovir hydrate also reduces the viral cytopathic effect of SIV(mac251) , SIV(B670) ,SHIV(89.6) and SHIV(RTSHIV) [2]. Tenofovir hydrate inhibits hepatitis B virus (HBV) activity in HepG2 2.2.15, HepAD38 and HepAD79 cells [3]. Tenofovir hydrate (4 μM) completely inhibits the growth of HIVIIIB in MT-2 cells. Tenofovir hydrate inhibits synthesis of negative strand strong-stop DNA with IC50 of 9 M for wild-type RT, 6 M for M184V RT and 50 M for K65R RT [4].in vivo: Tenofovir hydrate (30 mg/kg) completely prevents SIV infection in all macaques without toxicity. Tenofovir hydrate treatment reduces plasma viral RNA levels to undetectable, with parallel decreases in the infectivity of plasma and infectious cells in peripheral blood mononuclear cells and cerebrospinal fluid (CSF) and stabilization of CD4+ T-cell numbers. Tenofovir hydrate (30 mg/kg, s.c.) completely abrogates HIV infection via intravaginal exposure in pig-tailed macaques [5].Clinical indications: HIV-1 infection; hepatitis B virusinfectionsFDA Approved Date: 12 July 2006Toxicity: The mean change of eGFR from the baseline to the six months of follow-up was +/-1.32 and +/- 5.88 mL/minute in the TDF and AZT groups. Proximal tubular dysfunction was not noted at three and six months of follow-up. However patients in the TDF group had lower serum phosphate and higher renal potassium loss than the AZT group at six months of follow-up (p = 0.08 and p = 0.09, respectively). No patients in the two groups with distal tubular dysfunctions were noted [6].

Reference

[1]. http://www.immunopaedia.org.za/fileadmin/new_all/case_studies/pdfs/tenofovir.pdf
[2]. Witvrouw M, et al. Susceptibility of HIV-2, SIV and SHIV to various anti-HIV-1 compounds: implications for treatment and postexposure prophylaxis. Antivir Ther. 2004 Feb;9(1):57-65.
[3]. Ying C, et al. Inhibition of the replication of the DNA polymerase M550V mutation variant of human hepatitis B virus by adefovir,tenofovir, L-FMAU, DAPD, penciclovir and lobucavir. J Viral Hepat. 2000 Mar;7(2):161-5.
[4]. Wainberg MA, et al. In vitro selection and characterization of HIV-1 with reduced susceptibility to PMPA. Antivir Ther. 1999;4(2):87-94.
[5]. De Clercq E, et al. Clinical potential of the acyclic nucleoside phosphonates cidofovir, adefovir, and tenofovir in treatment of DNA virus and retrovirus infections. Clin Microbiol Rev. 2003 Oct;16(4):569-96.
[6]. Woratanarat K, et al. Tenofovir disoproxil fumarate-associated nephrotoxicity in HIV-infected patients: a prospective controlled study. J Med Assoc Thai. 2013 Apr;96(4):432-9.