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Antiviral API
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- Antiviral intermediates
Censavudine
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| Category | Human immunodeficiency Virus (HIV) |
| CAS | 634907-30-5 |
| Description | Censavudine is a nucleoside reverse transcriptase inhibitor. It is active against HIV resistant to both abacavir and tenofovir. It is a candidate for people with multi-drug resistant (MDR) strains of the virus. It is a derivative of stavudine (d4T), but is less toxic. It has demonstrated potent in vitro activity against HIV-2. It was developed by Bristol Myers-Squibb and in clinic phase 2 trials. |
Product Information
| Synonyms | OBP-601; OBP601; OBP 601; BMS-986001; BMS 986001; BMS986001; festinavir; 4'-Ed4T; 2',3'-Didehydro-3'-deoxy-4'-ethynylthymidine; 4'-Ethynyl D4T |
| IUPAC Name | 1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione |
| Molecular Weight | 248.24 |
| Molecular Formula | C12H12N2O4 |
| Canonical SMILES | CC1=CN(C(=O)NC1=O)C2C=CC(O2)(CO)C#C |
| InChI | InChI=1S/C12H12N2O4/c1-3-12(7-15)5-4-9(18-12)14-6-8(2)10(16)13-11(14)17/h1,4-6,9,15H,7H2,2H3,(H,13,16,17)/t9-,12+/m1/s1 |
| InChIKey | OSYWBJSVKUFFSU-SKDRFNHKSA-N |
| Melting Point | 207-209 °C |
| Purity | 95% |
| Density | 1.42±0.1 g/cm3 | Condition: Temp: 20 °C Press: 760 Torr |
| Solubility | Soluble in DMSO, not in water |
| Appearance | Light Yellow to Yellow Solid |
| Application | Censavudine is active against HIV resistant to both abacavir and tenofovir. |
| Storage | Store at -20 °C |
| Complexity | 513 |
| Exact Mass | 248.07970687 |
| In Vitro | BMS-986001 shows greater activity against HIV-2ROD9 than against HIV-1NL4-3; the mean EC50s for BMS-986001 are 74 nM for HIV-2ROD9 and 890 nM for HIV-1NL4-3 in the single-cycle assay. HIV-2ROD9 also showes greater sensitivity to BMS-986001 in 4-day infections of an immortalized T cell line (CEMss), with the mean EC50 for HIV-2ROD9 (EC50 of 0.14 nM) being 30-fold lower than that for HIV-1NL4-3 (EC50 of 4.2 nM). BMS-986001 also exhibits full activity against HIV-2 variants whose genomes encoded the single amino acid changes K65R and Q151M in reverse transcriptase. |
| In Vivo | The pharmacokinetic parameters of Censavudine (BMS-986001; 100-750 mg/kg) generated from the dried blood spot (DBS) assay and the plasma assay is compared. The ratios of the AUC(0-24 h) and C max for BMS-986001 in DBS compared to those in plasma are consistent at 0.83-0.91 and 0.81-0.97, respectively, across all dose groups in rats. The T max in rat DBS and plasma are also consistent at about 1 h. |
| PSA | 84.58000 |
| Target | HIV-2:30-81 nM (EC50) HIV-1:450-890 nM (IC50) |
| XLogP3-AA | -0.7 |
