CAS 206184-49-8|Tenofovir Monohydrate
Introduction：Basic information about CAS 206184-49-8|Tenofovir Monohydrate, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
| Common Name | Tenofovir Monohydrate | ||
|---|---|---|---|
| CAS Number | 206184-49-8 | Molecular Weight | 305.22800 |
| Density | 1.79g/cm3 | Boiling Point | 616.1ºC at 760mmHg |
| Molecular Formula | C9H16N5O5P | Melting Point | / |
| MSDS | / | Flash Point | 326.4ºC |
| Symbol | GHS06 | Signal Word | Danger |
Names
| Name | tenofovir hydrate |
|---|---|
| Synonym | More Synonyms |
Tenofovir Monohydrate BiologicalActivity
| Description | Tenofovir hydrate is a nucleotide reverse transcriptase inhibitor to treat HIV and chronic Hepatitis B. |
|---|---|
| Related Catalog | Signaling Pathways >>Anti-infection >>HIVSignaling Pathways >>Anti-infection >>Reverse TranscriptaseResearch Areas >>Infection |
| 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. |
Chemical & Physical Properties
| Density | 1.79g/cm3 |
|---|---|
| Boiling Point | 616.1ºC at 760mmHg |
| Molecular Formula | C9H16N5O5P |
| Molecular Weight | 305.22800 |
| Flash Point | 326.4ºC |
| Exact Mass | 305.08900 |
| PSA | 155.42000 |
| LogP | 0.46570 |
| InChIKey | PINIEAOMWQJGBW-FYZOBXCZSA-N |
| SMILES | CC(Cn1cnc2c(N)ncnc21)OCP(=O)(O)O.O |
| Storage condition | 2-8℃ |
Safety Information
| Symbol | GHS06 |
|---|---|
| Signal Word | Danger |
| Hazard Statements | H301 |
| Precautionary Statements | Missing Phrase - N15.00950417 |
| RIDADR | NONH for all modes of transport |
| HS Code | 2933990090 |
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% |
Synonyms
| Tenofovir Monohydrate |
| Unii-99yxe507il |
| 9-[(R)-2-(Phosphonomethoxy)propyl]adenine monohydrate |
| Tenofovir hydrate |
| Tenofovir (hydrate) |
