PSI-6130 (Synonyms: R 1656)

目录号: HY-10165 纯度: 99.39%: FAQs
Data Sheet SDS COA 产品使用指南技术支持

PSI-6130 是高效的，有选择性的 HCV NS5B polymerase 抑制剂，能够抑制HCV复制，IC₅₀ 值为 0.6 μM。

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PSI-6130 Chemical Structure

CAS No. : 817204-33-4

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥1265	In-stock
1 mg	￥615	In-stock
2 mg	￥887	In-stock
5 mg	￥1597	In-stock
10 mg	￥2316	In-stock
25 mg	￥4169	In-stock
50 mg	现货	询价
100 mg	现货	询价
200 mg		询价
500 mg		询价

or 大包装询价

* Please select Quantity before adding items.

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

•Antiviral Res. 2019 Oct;170:104570. [Abstract]

PSI-6130 相关产品

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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

PSI-6130 is a potent and selective inhibitor of HCV NS5B polymerase, and inhibits HCV replication with a mean IC₅₀ of 0.6 μM.?

IC₅₀ & Target

IC50: 0.6 μM (HCV replication)^[2]

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
Huh-7	CC₅₀	> 100 μM Compound: 1	Cytotoxic concentration against HCV replication RNA levels in Huh7 cells determined by HCV replicon assay Cytotoxic concentration against HCV replication RNA levels in Huh7 cells determined by HCV replicon assay	[PMID: 16107149]
Huh-7	CC₅₀	> 50 μM Compound: 1, PSI-6130	Cytotoxicity against human HuH7 cells by MTS assay Cytotoxicity against human HuH7 cells by MTS assay	[PMID: 20580554]
Huh-7	CC₅₀	> 98 μM Compound: 9a, PSI-6130	Cytotoxicity against human HuH7 cells assessed as inhibition of cell proliferation after 3 days by BrdU incorporation assay Cytotoxicity against human HuH7 cells assessed as inhibition of cell proliferation after 3 days by BrdU incorporation assay	[PMID: 24345201]
Huh-7	CC₅₀	> 98.4 μM Compound: 2, PSI-6130	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	0.6 μM Compound: 17	Antiviral activity against HCV genotype 1a infected in human HuH7 cells by replicon based assay Antiviral activity against HCV genotype 1a infected in human HuH7 cells by replicon based assay	[PMID: 25650256]
Huh-7	EC₅₀	0.61 μM Compound: PSI-6130	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	1.9 μM Compound: 9a, PSI-6130	Antiviral activity against Hepatitis C virus genotype 1b in human Huh7-luc clone ET replicon cells assessed as inhibition of replicon replication after 3 days by luciferase assay Antiviral activity against Hepatitis C virus genotype 1b in human Huh7-luc clone ET replicon cells assessed as inhibition of replicon replication after 3 days by luciferase assay	[PMID: 24345201]
Huh-7	EC₅₀	1.9 μM Compound: 2, PSI-6130	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]
Huh-7	EC₅₀	2.3 μM Compound: 17	Antiviral activity against HCV genotype 1b infected in human HuH7 cells by replicon based assay Antiviral activity against HCV genotype 1b infected in human HuH7 cells by replicon based assay	[PMID: 25650256]
Huh-7	EC₅₀	4.5 μM Compound: PSI-6130	Antiviral activity against HCV infected in human Huh7 cells assessed as reduction in viral RNA replication after 4 days Antiviral activity against HCV infected in human Huh7 cells assessed as reduction in viral RNA replication after 4 days	[PMID: 27994763]
MT4	CC₅₀	> 98.4 μM Compound: 2, PSI-6130	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)

PSI-6130 对由NS5B聚合酶介导的HCV RNA复制显示出强大且特异性的抑制活性。它能够抑制HCV基因型1b（Con1株）和基因型1a（H77株）亚基因组RNA的复制，对这两种株系的平均EC₅₀值分别为0.51 μM和0.30 μM。此外，PSI-6130在40%人血清中的EC₅₀值为0.51 μM^[1]。
PSI-6130 抑制HCV复制的平均IC₅₀值为0.6 μM。而其三磷酸形式PSI-6130-TP对HCV复制酶的抑制作用更强，平均IC₅₀值为0.34 μM。PSI-6130-TP还能抑制重组HCV Con1 NS5B在源自HCV基因组负链3′端的异聚RNA模板上的活性，其IC₅₀值为0.13 μM，K_i值为0.023 μM^[2]。为了保持专业性和语言的流畅性，可以调整为：

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

分子量

259.24

Formula

C₁₀H₁₄FN₃O₄

CAS 号

817204-33-4

性状

固体

颜色

White to off-white

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 : 25 mg/mL (96.44 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	3.8575 mL	19.2874 mL	38.5747 mL
5 mM	0.7715 mL	3.8575 mL	7.7149 mL
10 mM	0.3857 mL	1.9287 mL	3.8575 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 (9.64 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 (9.64 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 (9.64 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: 99.39%

选择批次：

Data Sheet (641 KB) SDS (251 KB)

COA (193 KB) LCMS (94 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Ali S, et al. Selected replicon variants with low-level in vitro resistance to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack cross-resistance with R1479. Antimicrob Agents Chemother. 2008 Dec;52(12):4356-69. [Content Brief]

[2]. Ma H, et al. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. J Biol Chem. 2007 Oct 12;282(41):29812-20. Epub 2007 Aug 13. [Content Brief]

Kinase Assay ^[1]	The inhibition potency of compounds with respect to the RdRp activity of recombinant NS5B570-BK, NS5B570-Con1, and NS5B570-H77 proteins is determined by measuring the incorporation of radiolabeled NMP into acid-insoluble RNA products by use of a complement strand of internal ribosomal entry site (cIRES) RNA template. Briefly, 50% inhibitory concentration (IC₅₀) determinations are carried out using 200 nM in vitro-transcribed cIRES RNA template, 1 μCi of tritiated UTP (42 Ci/mmol), 500 μM ATP, 500 μM GTP, 1 μM CTP, 1× TMDN buffer (40 mM Tris-HCl [pH 8.0], 4 mM MgCl₂, 4 mM dithiothreitol, 40 mM NaCl), and 200 nM enzyme. The inhibition potency of compounds with respect to the RdRp activity of NS5B570-S282T-Con1 is determined under GT-1b assay conditions as. NS5B570-BK and NS5B570-Con1 enzymes are used as controls. The final reaction volume is 50 μL under all assay conditions. All reactions contain a final 10% dimethyl sulfoxide. K_m and K_i values are measured. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[1]. Ali S, et al. Selected replicon variants with low-level in vitro resistance to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack cross-resistance with R1479. Antimicrob Agents Chemother. 2008 Dec;52(12):4356-69. [Content Brief] [2]. Ma H, et al. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. J Biol Chem. 2007 Oct 12;282(41):29812-20. Epub 2007 Aug 13. [Content Brief]

Kinase Assay
^[1]

The inhibition potency of compounds with respect to the RdRp activity of recombinant NS5B570-BK, NS5B570-Con1, and NS5B570-H77 proteins is determined by measuring the incorporation of radiolabeled NMP into acid-insoluble RNA products by use of a complement strand of internal ribosomal entry site (cIRES) RNA template. Briefly, 50% inhibitory concentration (IC₅₀) determinations are carried out using 200 nM in vitro-transcribed cIRES RNA template, 1 μCi of tritiated UTP (42 Ci/mmol), 500 μM ATP, 500 μM GTP, 1 μM CTP, 1× TMDN buffer (40 mM Tris-HCl [pH 8.0], 4 mM MgCl₂, 4 mM dithiothreitol, 40 mM NaCl), and 200 nM enzyme. The inhibition potency of compounds with respect to the RdRp activity of NS5B570-S282T-Con1 is determined under GT-1b assay conditions as. NS5B570-BK and NS5B570-Con1 enzymes are used as controls. The final reaction volume is 50 μL under all assay conditions. All reactions contain a final 10% dimethyl sulfoxide. K_m and K_i values are measured.

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

参考文献

[1]. Ali S, et al. Selected replicon variants with low-level in vitro resistance to the hepatitis C virus NS5B polymerase inhibitor PSI-6130 lack cross-resistance with R1479. Antimicrob Agents Chemother. 2008 Dec;52(12):4356-69. [Content Brief]

[2]. Ma H, et al. Characterization of the metabolic activation of hepatitis C virus nucleoside inhibitor beta-D-2'-Deoxy-2'-fluoro-2'-C-methylcytidine (PSI-6130) and identification of a novel active 5'-triphosphate species. J Biol Chem. 2007 Oct 12;282(41):29812-20. Epub 2007 Aug 13. [Content Brief]

PSI-6130 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	3.8575 mL	19.2874 mL	38.5747 mL	96.4369 mL
	5 mM	0.7715 mL	3.8575 mL	7.7149 mL	19.2874 mL
	10 mM	0.3857 mL	1.9287 mL	3.8575 mL	9.6437 mL
	15 mM	0.2572 mL	1.2858 mL	2.5716 mL	6.4291 mL
	20 mM	0.1929 mL	0.9644 mL	1.9287 mL	4.8218 mL
	25 mM	0.1543 mL	0.7715 mL	1.5430 mL	3.8575 mL
	30 mM	0.1286 mL	0.6429 mL	1.2858 mL	3.2146 mL
	40 mM	0.0964 mL	0.4822 mL	0.9644 mL	2.4109 mL
	50 mM	0.0771 mL	0.3857 mL	0.7715 mL	1.9287 mL
	60 mM	0.0643 mL	0.3215 mL	0.6429 mL	1.6073 mL
	80 mM	0.0482 mL	0.2411 mL	0.4822 mL	1.2055 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:

PSI-6130817204-33-4R 1656PSI6130PSI 6130R1656R-1656HCVHepatitis C virusInhibitorinhibitorinhibit

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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

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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）

PSI-6130 (Synonyms: R 1656)

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献