Censavudine|634907-30-5|(Festinavir; BMS-986001; OBP-601)-陌孚医药/Medlife

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Censavudine (Synonyms: Festinavir; BMS-986001; OBP-601)

目录号: PL08002 纯度: ≥98%

CAS No. :634907-30-5

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中文名称	Censavudine
英文名称	Censavudine
英文别名	2,4(1H,3H)-Pyrimidinedione,1-[(2R,5R)-5-ethynyl-2,5-dihydro-5-(hydroxymethyl)-2-furanyl]-5-methyl-;1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-5-methylpyrimidine-2,4-dione;OBP-601;BMS-986001;Censavudine;Festinavir;4'-ethynylstavudine;4'-Ed4T;4'-Ethynyl D4T;2',3'-Didehydro-3'-deoxy-4'-ethynylthymidine;4'-Ethynyl-d4T;6IE83O6NGA;4'-ethynyl-2',3'-didehydro-3'-deoxythymidine;1-((2R,5R)-5-Ethynyl-5-(hydroxymethyl)-2H-furan-2-yl)-5-methyl-pyrimidine-2,4-dione;1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2,5-dihydrofuran-2-yl]-5-methylpyrimidine-2,4(1H,3H)-dione;Ed4T;Censavudine [USAN:INN];OBP601;1-[(2R,5R)-5-ethynyl-5-(hydroxymethyl)-2H-furan-2-yl]-
Cas No.	634907-30-5
分子式	C₁₂H₁₂N₂O₄
分子量	248.23
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Censavudine (OBP-601; BMS-986001)，一种核苷类似物，是一种核苷逆转录酶 (nucleoside reverse transcriptase) 抑制剂。Censavudine 是一种有效的 HIV 抑制剂，对 HIV-2 和 HIV-1 的 EC₅₀ 范围分别为 30-81 nM 和 450-890 nM。

生物活性

Censavudine (OBP-601; BMS-986001), a nucleoside analog, is a nucleoside reverse transcriptase inhibitor. Censavudine is a potent HIV inhibitor with EC 50 ranges from 30 nM to 81 nM and 450 nM to 890 nM for HIV-2 and HIV-1, respectively.

性状

Solid

IC50 & Target[1][2]

HIV-2 30-81 nM (EC50) HIV-1 450-890 nM (IC

体外研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(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. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. 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.
[2]. 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.

溶解度数据	In Vitro: DMSO : 52 mg/mL (209.48 mM; Need ultrasonic)H₂O : 10 mg/mL (40.29 mM; ultrasonic and warming and heat to 60°C)配制储备液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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