Torcitabine
(Synonyms: 2'-脱氧-L-胞苷,2'-Deoxy-L-cytidine; L-dC) 目录号 : GC61339
Torcitabine(2'-Deoxy-L-cytidine)是一种抗病毒药物。Torcitabine可用于慢性乙型肝炎病毒感染的研究。
Cas No.:40093-94-5
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Torcitabine (2'-Deoxy-L-cytidine) is an antiviral agent. Torcitabine has the potential for chronic hepatitis B virus infection treatment[1][2].
Torcitabine (2'-Deoxy-L-cytidine) shows greater inhibition of first strand than second strand DNA synthesis[2].
[1]. Buti M, et al. Drugs in development for hepatitis B. Drugs. 2005;65(11):1451‐1460. [2]. Keam SJ. Telbivudine. Drugs. 2007;67(13):1917‐1929.
| Cas No. | 40093-94-5 | SDF | |
| 别名 | 2'-脱氧-L-胞苷,2'-Deoxy-L-cytidine; L-dC | ||
| Canonical SMILES | O=C1N=C(C=CN1[C@@H]2C[C@@H](O)[C@@H](O2)CO)N | ||
| 分子式 | C9H13N3O4 | 分子量 | 227.22 |
| 溶解度 | DMSO: 250 mg/mL (1100.26 mM); Water: 250 mg/mL (1100.26 mM) | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 4.401 mL | 22.0051 mL | 44.0102 mL |
| 5 mM | 0.8802 mL | 4.401 mL | 8.802 mL |
| 10 mM | 0.4401 mL | 2.2005 mL | 4.401 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Telbivudine/Torcitabine Idenix/Novartis
Curr Opin Investig Drugs 2004 Feb;5(2):232-41.PMID:15043399doi
Idenix (formerly Novirio) and Novartis are developing two beta-L-deoxynucleosides, telbivudine and Torcitabine, for the potential treatment of hepatitis B virus infection. Phase III trials of telbivudine were underway by August 2002 and phase I/II trials of the Torcitabine prodrug, valtorcitabine, were ongoing in November 2003.
In vitro susceptibility of adefovir-associated hepatitis B virus polymerase mutations to other antiviral agents
Antivir Ther 2007;12(3):355-62.PMID:17591025doi
Background: Adefovir dipivoxil is a nucleotide prodrug approved for the treatment of chronic hepatitis B. During clinical trials, ADV-associated mutations were observed in 0, 3, 11, 18 and 29% of patients after 48, 96, 144, 192 and 240 weeks of therapy, respectively. Hepatitis B virus (HBV) polymerase mutations associated with virological breakthrough to ADV include rtA181V and rtN236T, which occur alone or in combination. The rtA181T mutation has also been observed at low frequency, alone or in combination with rtN236T. Methods: To investigate the in vitro activity of adefovir and other anti-HBV agents against these mutants, we generated five stable cell lines that each expressed one of the following HBV mutants: rtN236T, rtA181V, rtA181V + rtN236T, rtA181T + rtN236T and rtA181T. Using these cell lines, we quantified in vitro changes in drug susceptibility for eight nucleotide/nucleoside analogues. Results: The rtN236T mutant had 7-fold resistance to adefovir but remained sensitive to entecavir, telbivudine and Torcitabine (53.2-fold reduced susceptibility). The A181V mutant had 4.3-fold resistance to adefovir and had reduced susceptibility to multiple other agents ranging from 3.2-fold (tenofovir) to >191-fold (clevudine). The A181V + rtN236T double mutant was the most highly resistant showing 18-fold resistance to adefovir and higher levels of resistance to other tested drugs with the exception of tenofovir (10-fold reduced susceptibility). Our results and preliminary clinical data suggest that patients with rtN236T or rtA181V remain susceptible to tenofovir, entecavir and lamivudine. Further clinical data are necessary to precisely define in vitro cutoffs indicative of clinically-relevant resistance, particularly for drugs in development such as emtricitabine, telbivudine, Torcitabine and clevudine.
Cross-resistance testing of next-generation nucleoside and nucleotide analogues against lamivudine-resistant HBV
Antivir Ther 2005;10(5):625-33.PMID:16152756doi
Several next-generation nucleoside and nucleotide analogues are currently in clinical development for the treatment of chronic hepatitis B. However, the efficacy of newer agents against lamivudine-resistant hepatitis B virus (HBV) has not been fully explored. To investigate this in vitro, we generated novel stable cell lines expressing HBV encoding the four major patterns of lamivudine resistance mutations (rtL180M+rtM204V, rtV173L+rtL180M+rtM204V, rtM204I and rtL180M+ rtM204I). Using these cell lines, we assessed the susceptibility of all four strains of lamivudine-resistant HBV to eleven nucleoside analogues in various stages of clinical development. Our studies indicate that lamivudine-resistant HBV remain sensitive to acyclic phosphonate nucleotides (adefovir, tenofovir, and alamifovir), have reduced susceptibility to entecavir, and have high-level cross-resistance to all L-nucleosides tested including emtricitabine, telbivudine, clevudine, and Torcitabine.