PSI-6130 (Synonyms: R 1656)

目錄號(hào): HY-10165 純度: 99.39%: FAQs
Data Sheet SDS COA 產(chǎn)品使用指南

摩爾計(jì)算器

PSI-6130 是高效的，有選擇性的 HCV NS5B polymerase 抑制劑，能夠抑制HCV復(fù)制，IC₅₀ 值為 0.6 μM。

MCE 的所有產(chǎn)品僅用作科學(xué)研究或藥證申報(bào)，我們不為任何個(gè)人用途提供產(chǎn)品和服務(wù)

PSI-6130 Chemical Structure

CAS No. : 817204-33-4

1. 客戶無需承擔(dān)相應(yīng)的運(yùn)輸費(fèi)用。

2. 同一機(jī)構(gòu)（單位）同一產(chǎn)品試用裝僅限申領(lǐng)一次，同一機(jī)構(gòu)（單位）一年內(nèi)

可免費(fèi)申領(lǐng)三個(gè)不同產(chǎn)品的試用裝。

3. 試用裝只面向終端客戶。

規(guī)格	價(jià)格	是否有貨
Free Sample (0.1 - 0.2 mg)		Apply now
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	現(xiàn)貨	詢價(jià)
100 mg	現(xiàn)貨	詢價(jià)
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Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)

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

PSI-6130 相關(guān)產(chǎn)品

•相關(guān)化合物庫:

•同靶點(diǎn)產(chǎn)品:

•同靶點(diǎn)蛋白產(chǎn)品:

生物活性
實(shí)驗(yàn)參考方法
純度 & 產(chǎn)品資料
參考文獻(xiàn)

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]

細(xì)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]

體外研究
(In Vitro)

PSI-6130 對(duì)由NS5B聚合酶介導(dǎo)的HCV RNA復(fù)制顯示出強(qiáng)大且特異性的抑制活性。它能夠抑制HCV基因型1b（Con1株）和基因型1a（H77株）亞基因組RNA的復(fù)制，對(duì)這兩種株系的平均EC₅₀值分別為0.51 μM和0.30 μM。此外，PSI-6130在40%人血清中的EC₅₀值為0.51 μM^[1]。
PSI-6130 抑制HCV復(fù)制的平均IC₅₀值為0.6 μM。而其三磷酸形式PSI-6130-TP對(duì)HCV復(fù)制酶的抑制作用更強(qiáng)，平均IC₅₀值為0.34 μM。PSI-6130-TP還能抑制重組HCV Con1 NS5B在源自HCV基因組負(fù)鏈3′端的異聚RNA模板上的活性，其IC₅₀值為0.13 μM，K_i值為0.023 μM^[2]。為了保持專業(yè)性和語言的流暢性，可以調(diào)整為：

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

分子量

259.24

Formula

C₁₀H₁₄FN₃O₄

CAS 號(hào)

817204-33-4

性狀

固體

顏色

White to off-white

運(yùn)輸條件

Room temperature in continental US; may vary elsewhere.

儲(chǔ)存方式

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

溶解性數(shù)據(jù)

細(xì)胞實(shí)驗(yàn)：

DMSO 中的溶解度 : 25 mg/mL (96.44 mM; 超聲助溶; 吸濕的 DMSO 對(duì)產(chǎn)品的溶解度有顯著影響，請(qǐng)使用新開封的 DMSO)

配制儲(chǔ)備液

濃度溶劑體積質(zhì)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

查看完整儲(chǔ)備液配制表

* 請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲(chǔ)備液；一旦配成溶液，請(qǐng)分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用， -20°C儲(chǔ)存時(shí)，請(qǐng)?jiān)?年內(nèi)使用。

摩爾計(jì)算器
稀釋計(jì)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

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動(dòng)物實(shí)驗(yàn)：

請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥方式選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請(qǐng)先按照 In Vitro 方式配制澄清的儲(chǔ)備液，再依次添加助溶劑：
——為保證實(shí)驗(yàn)結(jié)果的可靠性，澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；體內(nèi)實(shí)驗(yàn)的工作液，建議您現(xiàn)用現(xiàn)配，當(dāng)天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.64 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (9.64 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請(qǐng)依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.64 mM); 澄清溶液

此方案可獲得 ≥ 2.5 mg/mL（飽和度未知）的澄清溶液，此方案實(shí)驗(yàn)周期在半個(gè)月以上的動(dòng)物實(shí)驗(yàn)酌情使用。
以 1 mL 工作液為例，取 100 μL 25.0 mg/mL 的澄清 DMSO 儲(chǔ)備液加到 900 μL玉米油中，混合均勻。

動(dòng)物溶解方案計(jì)算器

請(qǐng)輸入動(dòng)物實(shí)驗(yàn)的基本信息：

給藥劑量

mg/kg

動(dòng)物的平均體重

每只動(dòng)物的給藥體積

μL

動(dòng)物數(shù)量

只

由于實(shí)驗(yàn)過程有損耗，建議您多配一只動(dòng)物的量

請(qǐng)輸入您的動(dòng)物體內(nèi)配方組成：

DMSO +

Tween-80 +

Saline

如果您的動(dòng)物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網(wǎng)站選購。，Tween 80，均可在 MCE 網(wǎng)站選購。

計(jì)算結(jié)果

工作液所需濃度 : mg/mL

儲(chǔ)備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲(chǔ)備液濃度超過該產(chǎn)品的實(shí)測(cè)溶解度，以下方案僅供參考，如有需要，請(qǐng)與 MCE 中國技術(shù)支持聯(lián)系。

動(dòng)物實(shí)驗(yàn)體內(nèi)工作液的配制方法 : 取 μL DMSO 儲(chǔ)備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請(qǐng)謹(jǐn)慎選擇該方案。

請(qǐng)確保第一步儲(chǔ)備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產(chǎn)品資料

純度: 99.39%

選擇批次：

Data Sheet (641 KB) SDS (251 KB)

COA (193 KB) LCMS (94 KB)

產(chǎn)品使用指南 (1538 KB)

參考文獻(xiàn)

[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.
參考文獻(xiàn)	[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.

參考文獻(xiàn)

[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 相關(guān)分類

Infection

完整儲(chǔ)備液配制表

可選溶劑	濃度溶劑體積質(zhì)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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PSI-6130 (Synonyms: R 1656)

Customer Review

MCE 顧客使用本產(chǎn)品發(fā)表的 1 篇科研文獻(xiàn)