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147127-20-6

147127-20-6 structure
147127-20-6 structure
  • Name: Tenofovir
  • Chemical Name: Tenofovir
  • CAS Number: 147127-20-6
  • Molecular Formula: C9H14N5O4P
  • Molecular Weight: 287.212
  • Catalog: API Synthetic anti-infective drugs Antiviral drugs
  • Create Date: 2018-02-07 08:00:00
  • Modify Date: 2025-08-20 19:37:11
  • Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
Name Tenofovir
Synonyms (R)-(((1-(6-Amino-9H-purin-9-yl)propan-2-yl)oxy)methyl)phosphonic acid
(R)-(1-(6-amino-9H-purin-9-yl)propan-2-yloxy)methylphosphonic acid
D,L-TENOFOVIR
Apropovir
9-Pmpa
MFCD07357269
Tenefovir
GS-1278
1-(6-Aminopurin-9-yl)propan-2-yloxymethylphosphonic acid
Description Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.
Related Catalog
In Vitro Tenofovir shows cytotoxic effects on cell viability in HK-2 cells, with IC50 values of 9.21 and 2.77 μM at 48 and 72 h in MTT assay, respectively. Tenofovir diminishes ATP levels in HK-2 cells. Tenofovir (3.0 to 28.8 μM) increases oxidative stress and protein carbonylation in HK-2 cells. Furthermore, Tenofovir induces apoptosis in HK-2 cells, and that apoptosis is induced via mitochondrial damage[1]. Tenofovir and M48U1 formulated in 0.25% HEC each inhibits the replication of both R5-tropic HIV-1BaL and X4-tropic HIV-1IIIb in activated PBMCs, and inhibits several laboratory strains and patient-derived HIV-1 isolates. The combined formulation of M48U1 and tenofovir in 0.25% HEC exhibits synergistic antiretroviral activity against infection with R5-tropic HIV-1BaL, and is not toxic to PBMCs[2].
In Vivo Tenofovir Disoproxil Fumarate (20, 50, 140, or 300 mg/kg) administered to BLT mice, shows dose dependent activity during vaginal HIV challenge in BLT humanized mice. Tenofovir Disoproxil Fumarate (50, 140, 300 mg/kg) significantly reduces HIV transmission in BLT mice[3]. Tenofovir Disoproxil Fumarate (0.5, 1.5, or 5.0 mg/kg/day, p.o.) induces a dose-dependent decline in serum viremia in woodchucks chronically infected with WHV. Tenofovir Disoproxil Fumarate administration is safe and effective in the woodchuck model of chronic HBV infection[4].
Cell Assay Cells are plated into 48-well tissue culture plates (39,000 cells/mL) and allowed to grow for 48 h followed by treatment with vehicle or Tenofovir. Following the treatment period, cell viability is assessed using the MTT assay. The MTT assay relies on the conversion of tetrazolium dye 3-(4,5-dimethlthiazol-2-yl)-2,5-diphenyltetrazolium bromide (MTT) to formazan by NAD(P)H-dependent oxidoreductases[1].
Animal Admin Twenty adult chronic WHV carrier woodchucks are stratified equally by age, sex, body weight, and serum GGT activity into five treatment groups consisting of four animals each: (i) Tenofovir Disoproxil Fumarate at 15.0 mg/kg once per day, (ii) Tenofovir Disoproxil Fumarate at 5.0 mg/kg/day, (iii) Tenofovir Disoproxil Fumarate at 1.5 mg/kg/day, (iv) Tenofovir Disoproxil Fumarate at 0.5 mg/kg/day, and (v) a placebo control. The woodchucks are treated daily for 4 weeks and observed for an additional 12 weeks following cessation of drug treatment[4].
References

[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).

[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.

[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.

[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.
Density 1.8±0.1 g/cm3
Boiling Point 616.1±65.0 °C at 760 mmHg
Melting Point 276-280°C
Molecular Formula C9H14N5O4P
Molecular Weight 287.212
Flash Point 326.4±34.3 °C
Exact Mass 287.078339
PSA 146.19000
LogP -1.71
Vapour Pressure 0.0±1.9 mmHg at 25°C
Index of Refraction 1.740
Storage condition Store at -20°C
Water Solubility 13.4 mg/mL (25 ºC)
Hazard Codes C
Risk Phrases R34:Causes burns.
Safety Phrases S22-S26-S27-S36/37/39-S45
RIDADR UN 3261 8/PG 2
WGK Germany 3
RTECS DB8930000
Packaging Group III
Hazard Class 8
HS Code 2933990090
HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%
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