Tenofovir

Modify Date: 2019-06-17 12:07:59

Tenofovir Structure
Tenofovir structure
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Common Name Tenofovir
CAS Number 147127-20-6 Molecular Weight 287.212
Density 1.8±0.1 g/cm3 Boiling Point 616.1±65.0 °C at 760 mmHg
Molecular Formula C9H14N5O4P Melting Point 276-280°C
MSDS N/A Flash Point 326.4±34.3 °C

 Use of Tenofovir


Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B.

 Names

Name Tenofovir
Synonym More Synonyms

 Tenofovir Biological Activity

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].
Solvent
In Vitro:

H2O : 2 mg/mL (6.96 mM; Need ultrasonic)

Solubility
1 mM 3.4818 mL 17.4089 mL 34.8177 mL
5 mM 0.6964 mL 3.4818 mL 6.9635 mL
10 mM 0.3482 mL 1.7409 mL 3.4818 mL
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].
Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping Room temperature in continental US; may vary elsewhere
SMILES C[C@@H](OCP(O)(O)=O)CN1C=NC2=C(N)N=CN=C12
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.

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Related Doc

SDS |COA |LCMS

*The above documents are provided by Medchemexpress and are for scientific research only.

 Chemical & Physical Properties

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)

 Safety Information

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

 Synthetic Route

 Customs

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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