| Description | Censavudine (OBP-601) is a nucleoside analog, a nucleoside reverse transcriptase inhibitor, used for the prevention and treatment of human immunodeficiency virus 1 (HIV-1).Censavudine inhibits HIV-2 and HIV-1. Censavudine inhibits HIV-2 and HIV-1 with EC50 ranges of 30-81 nM and 450-890 nM, respectively. |
| In vitro | 在单循环测定中，Censavudine 对HIV-2ROD9的活性优于HIV-1NL4-3。Censavudine 对HIV-2ROD9和HIV-1NL4-3的平均EC50分别为74 nM和890 nM。在持续4天的CEMss免疫细胞系感染实验中，HIV-2ROD9对Censavudine 的敏感性更高，平均EC50值为0.14 nM，是HIV-1NL4-3（4.2 nM）EC50的30倍。此外，Censavudine 能够针对携带K65R和Q151M单氨基酸变异的逆转录酶基因组的HIV-2变体保持完整活性。 |
| In vivo | 在比较Censavudine (BMS-986001)在100至750 mg/kg剂量范围内的药代动力学参数时，采用了干血斑(DBS)测定法和血浆测定法。在大鼠所有剂量组中，BMS-986001在DBS与血浆中的AUC(0-24 h)比值和Cmax比值分别保持在0.83-0.91和0.81-0.97之间。大鼠DBS和血浆中的Tmax亦一致约在1小时处[1]。 |
| Target activity | HIV-2:30-81 nM (EC50), HIV-2 (ROD9):74 nM(EC50), HIV-1:450-890 nM, HIV-1NL4-3:890 nM(EC50) |
| Synonyms | OBP 601, BMS 986001, BMS-986001, OBP601, BMS986001, OBP-601 |
| molecular weight | 248.23 |
| Molecular formula | C12H12N2O4 |
| CAS | 634907-30-5 |
| Storage | store at low temperature|Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | H2O: 5 mg/mL (20.14 mM), Sonication is recommended. DMSO: 45 mg/mL (181.28 mM), Sonication is recommended. |
| References | 1. Long Yuan, et al. Dried Blood Spot Analysis Without Dilution: Application to the LC-MS/MS Determination of BMS-986001 in Rat Dried Blood Spot. J Chromatogr B Analyt Technol Biomed Life Sci. 2015 Oct 1;1002:201-9. 2. Robert A Smith, et al. The Nucleoside Analog BMS-986001 Shows Greater In Vitro Activity Against HIV-2 Than Against HIV-1. Antimicrob Agents Chemother. 2015 Dec;59(12):7437-46. 3. Ortiz A, Benkovics T, Beutner GL, Shi Z, Bultman M, Nye J, Sfouggatakis C, Kronenthal DR. Scalable Synthesis of the Potent HIV Inhibitor BMS-986001 by Non-Enzymatic Dynamic Kinetic Asymmetric Transformation (DYKAT). Angew Chem Int Ed Engl. 2015 Jun 8;54(24):7185-8. doi: 10.1002/anie.201502290. Epub 2015 Apr 29. PubMed PMID: 25925234. |