Introduction：Basic information about CAS 147127-20-6|Tenofovir, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Tenofovir |
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| CAS Number | 147127-20-6 | Molecular Weight | 287.212 |
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| Density | 1.8±0.1 g/cm3 | Boiling Point | 616.1±65.0 °C at 760 mmHg |
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| Molecular Formula | C9H14N5O4P | Melting Point | 276-280°C |
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| MSDS | / | Flash Point | 326.4±34.3 °C |
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Names
| Name | Tenofovir |
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| Synonym | More Synonyms |
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Tenofovir BiologicalActivity
| Description | Tenofovir is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B. |
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| Related Catalog | Signaling Pathways >>Anti-infection >>HIVSignaling Pathways >>Anti-infection >>Reverse TranscriptaseResearch Areas >>Infection |
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| 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]. |
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| 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]. |
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| 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]. |
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| 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]. |
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| 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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Chemical & Physical Properties
| Density | 1.8±0.1 g/cm3 |
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| Boiling Point | 616.1±65.0 °C at 760 mmHg |
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| Melting Point | 276-280°C |
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| Molecular Formula | C9H14N5O4P |
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| Molecular Weight | 287.212 |
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| Flash Point | 326.4±34.3 °C |
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| Exact Mass | 287.078339 |
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| PSA | 146.19000 |
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| LogP | -1.71 |
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| Vapour Pressure | 0.0±1.9 mmHg at 25°C |
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| Index of Refraction | 1.740 |
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| InChIKey | SGOIRFVFHAKUTI-ZCFIWIBFSA-N |
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| SMILES | CC(Cn1cnc2c(N)ncnc21)OCP(=O)(O)O |
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| Storage condition | Store at -20°C |
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| Water Solubility | 13.4 mg/mL (25 ºC) |
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Safety Information
| Hazard Codes | C |
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| Risk Phrases | R34:Causes burns. |
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| Safety Phrases | S22-S26-S27-S36/37/39-S45 |
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| RIDADR | UN 3261 8/PG 2 |
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| WGK Germany | 3 |
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| RTECS | DB8930000 |
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| Packaging Group | III |
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| Hazard Class | 8 |
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| HS Code | 2933990090 |
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Customs
| HS Code | 2933990090 |
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| 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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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 |
