R-1479 (Synonyms: 4'-Azidocytidine)

目录号: HY-10444 纯度: 99.60%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

R-1479 (4'-Azidocytidine) 是一种核苷类似物，是特异性的 HCV RNA 依赖性 RNA 聚合酶 (RdRp) 抑制剂。R-1479 在 HCV 亚基因组复制体系中抑制 HCV 复制，IC₅₀ 为 1.28 μM。R-1479 是一种点击化学试剂。它含有 Azide 基团，可以和含有 Alkyne 基团的分子发生铜催化的叠氮-炔环加成反应（CuAAc)。它还可以和含有 DBCO 或 BCN 基团的分子发生环张力驱动的炔-叠氮环加成反应 (SPAAC)。

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R-1479 Chemical Structure

CAS No. : 478182-28-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥3752	In-stock
1 mg	￥1200	In-stock
5 mg	￥2800	In-stock
10 mg	￥4100	In-stock
25 mg	现货	询价
50 mg	现货	询价
100 mg		询价
200 mg		询价

or 大包装询价

* Please select Quantity before adding items.

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MCE 顾客使用本产品发表的 3 篇科研文献

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生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

R-1479 (4'-Azidocytidine), a nucleoside analogue, is a specific inhibitor of RNA-dependent RNA polymerase (RdRp) of HCV. R-1479 inhibits HCV replication in the HCV subgenomic replicon system (IC₅₀=1.28 μM)^[1]^[2]^[3]. R-1479 is a click chemistry reagent, it contains an Azide group and can undergo copper-catalyzed azide-alkyne cycloaddition reaction (CuAAc) with molecules containing Alkyne groups. It can also undergo strain-promoted alkyne-azide cycloaddition (SPAAC) reactions with molecules containing DBCO or BCN groups.

IC₅₀ & Target

IC50: 1.28 μM (HCV replication)^[1]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
HeLa	CC₅₀	> 80 μM Compound: 1b	Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay Cytotoxicity against human HeLa cells assessed as cell viability by CellTiter-Glo luminescent assay	[PMID: 25667954]
HeLa	EC₅₀	0.67 μM Compound: 1b	Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay Antiviral activity against Respiratory syncytial virus subgenomic replicon system in 395 HeLa cells assessed as reduction in viral replication after 7 days by renilla luciferase assay	[PMID: 25667954]
Huh-5-2	CC₅₀	> 33 μM Compound: 4'-Azidocytidine	Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay Cytotoxicity against human Huh5-2 cells after 3 days by MTT assay	[PMID: 18625766]
Huh-5-2	EC₅₀	1.4 μM Compound: 4'-Azidocytidine	Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b infected in human Huh5-2 cells assessed as reduction in replicon RNA after 4 days by luciferase assay	[PMID: 18625766]
Huh-7	CC₅₀	> 200 μM Compound: 4'azidocytidine	Cytotoxicity against human HuH7 cells after3 days by MTT assay Cytotoxicity against human HuH7 cells after3 days by MTT assay	[PMID: 20337460]
Huh-7	CC₅₀	> 98.4 μM Compound: 3, R-1479	Cytotoxicity against human HuH7 cells expressing CMV-Luc after 3 days by luciferase assay Cytotoxicity against human HuH7 cells expressing CMV-Luc after 3 days by luciferase assay	[PMID: 21033671]
Huh-7	EC₅₀	1.28 μM Compound: R-1479	Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay Antiviral activity against Hepatitis C virus subtype 1b Con1 infected in human HuH7 cells after 3 days by luciferase reporter gene assay	[PMID: 18285474]
Huh-7	EC₅₀	1.4 μM Compound: 4'azidocytidine	Antiviral activity against HCV 1b infected in human HuH7 cells assessed as inhibition of viral RNA replication after 4 days by replicon assay Antiviral activity against HCV 1b infected in human HuH7 cells assessed as inhibition of viral RNA replication after 4 days by replicon assay	[PMID: 20337460]
Huh-7	EC₅₀	4.3 μM Compound: 3, R-1479	Antiviral activity against Hepatitis C virus subtype 1b with adaptive mutations of E1202G, T1280I, K1846T in NS5B polymerase infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luciferase assay Antiviral activity against Hepatitis C virus subtype 1b with adaptive mutations of E1202G, T1280I, K1846T in NS5B polymerase infected in human HuH7 cells assessed as inhibition of viral replication after 3 days by luciferase assay	[PMID: 21033671]
MT4	CC₅₀	> 98.4 μM Compound: 3, R-1479	Cytotoxicity against human MT4 cells expressing LTR-Luc after 3 days by luciferase assay Cytotoxicity against human MT4 cells expressing LTR-Luc after 3 days by luciferase assay	[PMID: 21033671]

体外研究
(In Vitro)

R-1479 (R1479) inhibits HCV RNA replication with a mean IC₅₀ value of 1.28 μM when measured as dose-dependent reduction of Renillaluciferase activity after a 72 h incubation of proliferating replicon cells. R-1479 shows no effect on cell viability or proliferation of HCV replicon or Huh-7 cells at concentrations up to 2 mM^[1]. The most potent and non-cytotoxic derivative is R-1479 with an IC₅₀ of 1.28 μM in the HCV replicon system. The triphosphate of R-1479 is prepared and shown to be an inhibitor of RNA synthesis mediated by NS5B (IC₅₀=320 nM), the RNA polymerase encoded by HCV. R-1479 displays good activity in the replicon assay with no measurable cytotoxic or cytostatic effect^[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

284.23

Formula

C₉H₁₂N₆O₅

CAS 号

478182-28-4

性状

固体

颜色

White to off-white

中文名称

4'-叠氮基胞嘧啶核苷

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性数据

细胞实验：

DMSO 中的溶解度 : 100 mg/mL (351.83 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	3.5183 mL	17.5914 mL	35.1828 mL
5 mM	0.7037 mL	3.5183 mL	7.0366 mL
10 mM	0.3518 mL	1.7591 mL	3.5183 mL

查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (8.80 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (8.80 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.80 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.60%

选择批次：

Data Sheet (638 KB) SDS (251 KB)

COA (198 KB) RP-HPLC (232 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Klumpp K, et al. The novel nucleoside analog R1479 (4'-azidocytidine) is a potent inhibitor of NS5B-dependent RNA synthesis and hepatitis C virus replication in cell culture. J Biol Chem. 2006 Feb 17;281(7):3793-9. [Content Brief]

[2]. Smith DB, et al. Design, synthesis, and antiviral properties of 4'-substituted ribonucleosides as inhibitors of hepatitis C virus replication: the discovery of R1479. Bioorg Med Chem Lett. 2007 May 1;17(9):2570-6. [Content Brief]

[3]. Nguyen NM, et al. A randomized, double-blind placebo controlled trial of balapiravir, a polymerase inhibitor, in adult dengue patients. J Infect Dis. 2013 May 1;207(9):1442-1450. [Content Brief]

Kinase Assay ^[1]	The membrane-associated, native HCV replicase complex is isolated from 2209-23 HCV replicon cells and a derived cell line carrying HCV replicon RNA with a S282T mutation in the NS5B coding sequence. The in vitro replicase assay contain 10 μL of cytoplasmic membrane fraction, 50 mM HEPES (pH 7.5), 10 mM KCl, 10 mM dithiothreitol, 5 mM MgCl₂, 20 μg/mL actinomycin D, 1 mM ATP, 1 mM GTP, 1 mM UTP, 30 μCi of [α-³³P]CTP (3000 Ci/mmol, 10 mCi/mL), 1 unit/μL SUPERase•In, 10 mM creatine phosphate, and 200 μg/mL creatine phosphokinase in a final volume of 25 μL. Inhibition by nucleotide analogs is determined^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Cell Assay ^[1]	The effect of R-1479 on the incorporation of tritiated thymidine into cellular DNA is measured using the [³H]thymidine incorporation scintillation proximity assay system. MTT and WST-1 assay systems are used to measure cell viability. The ATP bioluminescence assay kit HSII is used to measure intracellular ATP levels^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Klumpp K, et al. The novel nucleoside analog R1479 (4'-azidocytidine) is a potent inhibitor of NS5B-dependent RNA synthesis and hepatitis C virus replication in cell culture. J Biol Chem. 2006 Feb 17;281(7):3793-9. [Content Brief] [2]. Smith DB, et al. Design, synthesis, and antiviral properties of 4'-substituted ribonucleosides as inhibitors of hepatitis C virus replication: the discovery of R1479. Bioorg Med Chem Lett. 2007 May 1;17(9):2570-6. [Content Brief] [3]. Nguyen NM, et al. A randomized, double-blind placebo controlled trial of balapiravir, a polymerase inhibitor, in adult dengue patients. J Infect Dis. 2013 May 1;207(9):1442-1450. [Content Brief]

R-1479 相关分类

Infection

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.5183 mL	17.5914 mL	35.1828 mL	87.9569 mL
	5 mM	0.7037 mL	3.5183 mL	7.0366 mL	17.5914 mL
	10 mM	0.3518 mL	1.7591 mL	3.5183 mL	8.7957 mL
	15 mM	0.2346 mL	1.1728 mL	2.3455 mL	5.8638 mL
	20 mM	0.1759 mL	0.8796 mL	1.7591 mL	4.3978 mL
	25 mM	0.1407 mL	0.7037 mL	1.4073 mL	3.5183 mL
	30 mM	0.1173 mL	0.5864 mL	1.1728 mL	2.9319 mL
	40 mM	0.0880 mL	0.4398 mL	0.8796 mL	2.1989 mL
	50 mM	0.0704 mL	0.3518 mL	0.7037 mL	1.7591 mL
	60 mM	0.0586 mL	0.2932 mL	0.5864 mL	1.4659 mL
	80 mM	0.0440 mL	0.2199 mL	0.4398 mL	1.0995 mL
	100 mM	0.0352 mL	0.1759 mL	0.3518 mL	0.8796 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

R-1479478182-28-44'-Azidocytidine4'-叠氮基胞嘧啶核苷R1479R 1479HCVDNA/RNA SynthesisHepatitis C virusnucleosideRdRpreplicationBalapiravirR1626Inhibitorinhibitorinhibit

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MedChemExpress (MCE) 只为有资质的科研机构、医药企业基于科学研究或药证申报的用途提供医药研发服务，不为任何个人或者非科研性质的、非用于药证申报使用等其他用途提供服务。

站点地图隐私声明

沪ICP备15051369号-4

上海工商

沪公网安备31011502019417

沪(浦)应急管危经许[2021]201709(QFYS)

营业执照（三证合一）

R-1479 (Synonyms: 4'-Azidocytidine)

Customer Review

MCE 顾客使用本产品发表的 3 篇科研文献