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  2. Cell Cycle/DNA Damage Anti-infection
  3. DNA/RNA Synthesis SARS-CoV
  4. GS-441524

GS-441524 是 Remdesivir 的主要活性代謝物，活性更優(yōu)于 Remdesivir ，感染病毒的原代人肺和貓細(xì)胞的細(xì)胞模型中顯示出相似的活性。 GS-441524 對貓傳染性腹膜炎病毒 (FIPV) 有較強的抑制作用，對應(yīng)的 EC50 值為 0.78 μM。

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GS-441524 Chemical Structure

GS-441524 Chemical Structure

CAS No. : 1191237-69-0

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規(guī)格 價格 是否有貨 數(shù)量
10 mM * 1 mL in DMSO ￥160
In-stock
50 mg ￥366
In-stock
100 mg ￥490
In-stock
200 mg   詢價  
500 mg   詢價  

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Customer Review

Other Forms of GS-441524:

  • 生物活性

  • 實驗參考方法

  • 純度 & 產(chǎn)品資料

  • 參考文獻(xiàn)

生物活性

GS-441524, predominant metabolite of Remdesivir and superior to Remdesivir against Covid-19 , shows comparable efficacy in cell-based models of primary human lung and cat cells infected with coronavirus. GS-441524 could strongly inhibits feline infectious peritonitis virus (FIPV), with an EC50 of 0.78 μM[1][2][3].

IC50 & Target

EC50: 0.78 μM (FIPV)[1].
細(xì)胞效力
(Cellular Effect)
Cell Line Type Value Description References
Fibroblast CC50
> 100 μM
Compound: GS-441524
Cytotoxicity against mock-infected human embryonic lung fibroblast cells incubated for 5 days by MTS assay
Cytotoxicity against mock-infected human embryonic lung fibroblast cells incubated for 5 days by MTS assay
[PMID: 33877845]
HEL 299 CC50
> 100 μM
Compound: GS-441524
Cytotoxicity against HEL 299 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay
Cytotoxicity against HEL 299 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay
[PMID: 35571875]
HeLa EC50
> 20 μM
Compound: 4
Antiviral activity against Ebolavirus Kikwit infected in human HeLa cells assessed as reduction in viral glycoprotein levels preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs by immunostaining based assay
Antiviral activity against Ebolavirus Kikwit infected in human HeLa cells assessed as reduction in viral glycoprotein levels preincubated with cells for 2 hrs followed by viral infection measured after 48 hrs by immunostaining based assay
[PMID: 28124907]
HeLa CC50
> 20 μM
Compound: Page no 2220, R7C1
Cytotoxicity against human HeLa after 4 to 5 days by Cell-Titer Glo viability assay
Cytotoxicity against human HeLa after 4 to 5 days by Cell-Titer Glo viability assay
[PMID: 28792763]
HeLa EC50
> 20 μM
Compound: Page no 2220, R7C1
Antiviral activity against Ebolavirus infected in human HeLa cells after 48 hrs by immuno-staining assay
Antiviral activity against Ebolavirus infected in human HeLa cells after 48 hrs by immuno-staining assay
[PMID: 28792763]
HeLa CC50
> 30 μM
Compound: 3a
Cytotoxicity against human HeLa cells by MTS assay
Cytotoxicity against human HeLa cells by MTS assay
[PMID: 22446091]
HeLa EC50
11 μM
Compound: 3a
Antiviral activity against Yellow fever virus 17D infected in human HeLa cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
Antiviral activity against Yellow fever virus 17D infected in human HeLa cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
[PMID: 22446091]
HEp-2 CC50
> 100 μM
Compound: 4
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay
Cytotoxicity against human Hep2 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay
[PMID: 28124907]
HEp-2 CC50
> 100 μM
Compound: 4
Cytotoxicity against human HEp-2 cells assessed as reduction in cell viability incubated for 4 to 5 days by CellTiter Glo viability assay
Cytotoxicity against human HEp-2 cells assessed as reduction in cell viability incubated for 4 to 5 days by CellTiter Glo viability assay
[PMID: 33835812]
HEp-2 IC50
0.35 μM
Compound: 4
Drug metabolism in human HEp-2 cells assessed as 1-NTP metabolite concentration at EC50 over 48 hrs by LC-MS/MS analysis
Drug metabolism in human HEp-2 cells assessed as 1-NTP metabolite concentration at EC50 over 48 hrs by LC-MS/MS analysis
[PMID: 33835812]
Huh-7 CC50
> 20 μM
Compound: Page no 2220, R7C1
Cytotoxicity against human HuH7 after 4 to 5 days by Cell-Titer Glo viability assay
Cytotoxicity against human HuH7 after 4 to 5 days by Cell-Titer Glo viability assay
[PMID: 28792763]
Huh-7 CC50
> 88 μM
Compound: 4
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 3 days by calcein-AM dye based fluorescence assay
Cytotoxicity against human HuH7 cells assessed as reduction in cell viability after 3 days by calcein-AM dye based fluorescence assay
[PMID: 28124907]
Huh-7 CC50
> 89 μM
Compound: 3a
Cytotoxicity against human HuH7 cells by MTS assay
Cytotoxicity against human HuH7 cells by MTS assay
[PMID: 22446091]
Huh-7 CC50
> 89 μM
Compound: 4
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 3 days by dual-Glo luciferase assay
Cytotoxicity against human Huh-7 cells assessed as reduction in cell viability measured after 3 days by dual-Glo luciferase assay
[PMID: 33835812]
Huh-7 EC50
4.1 μM
Compound: 3a
Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
Antiviral activity against Hepatitis C virus genotype 1b infected in human HuH7 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
[PMID: 22446091]
Macrophage CC50
> 20 μM
Compound: Page no 2220, R7C1
Cytotoxicity against human primary macrophages after 4 to 5 days by Cell-Titer Glo viability assay
Cytotoxicity against human primary macrophages after 4 to 5 days by Cell-Titer Glo viability assay
[PMID: 28792763]
MDCK CC50
> 30 μM
Compound: 3a
Cytotoxicity against dog MDCK cells by MTS assay
Cytotoxicity against dog MDCK cells by MTS assay
[PMID: 22446091]
MDCK EC50
27.9 μM
Compound: 3a
Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
Antiviral activity against Influenza A virus H3N2 infected in MDCK cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
[PMID: 22446091]
MRC5 EC50
> 30 μM
Compound: 3a
Antiviral activity against Coxsackievirus A7 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
Antiviral activity against Coxsackievirus A7 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
[PMID: 22446091]
MRC5 EC50
> 30 μM
Compound: 3a
Antiviral activity against Coxsackievirus A21 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
Antiviral activity against Coxsackievirus A21 infected in human MRC5 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
[PMID: 22446091]
MRC5 CC50
> 30 μM
Compound: 3a
Cytotoxicity against human MRC5 cells by MTS assay
Cytotoxicity against human MRC5 cells by MTS assay
[PMID: 22446091]
MT4 CC50
> 50 μM
Compound: 4
Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by CellTiter Glo viability assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability measured after 5 days by CellTiter Glo viability assay
[PMID: 33835812]
MT4 CC50
> 57 μM
Compound: 4
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay
Cytotoxicity against human MT4 cells assessed as reduction in cell viability after 4 to 5 days by Cell-Titer Glo assay
[PMID: 28124907]
Vero EC50
> 30 μM
Compound: 3a
Antiviral activity against West nile virus NY99 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
Antiviral activity against West nile virus NY99 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
[PMID: 22446091]
Vero CC50
> 30 μM
Compound: 3a
Cytotoxicity against african green monkey Vero cells by MTS assay
Cytotoxicity against african green monkey Vero cells by MTS assay
[PMID: 22446091]
Vero CC50
> 30 μM
Compound: 3a
Cytotoxicity against african green monkey Vero E6 cells by MTS assay
Cytotoxicity against african green monkey Vero E6 cells by MTS assay
[PMID: 22446091]
Vero EC50
1.71 μM
Compound: 3a
Antiviral activity against Parainfluenza 3 C 243 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
Antiviral activity against Parainfluenza 3 C 243 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
[PMID: 22446091]
Vero EC50
2.24 μM
Compound: 3a
Antiviral activity against SARS coronavirus Toronto-2 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
Antiviral activity against SARS coronavirus Toronto-2 infected in african green monkey Vero cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
[PMID: 22446091]
Vero EC50
9.46 μM
Compound: 3a
Antiviral activity against Dengue virus type 2 New Guinea C infected in african green monkey Vero E6 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
Antiviral activity against Dengue virus type 2 New Guinea C infected in african green monkey Vero E6 cells assessed as inhibition of virus induced cytopathic effect after 24 hrs by MTS assay
[PMID: 22446091]
Vero C1008 CC50
72.38 μM
Compound: GS-441524
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 1 to 2 hrs by MTS assay
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability incubated for 1 to 2 hrs by MTS assay
[PMID: 33962311]
Vero C1008 CC50
72.9 μM
Compound: GS-441524
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay
Cytotoxicity against African green monkey Vero E6 cells assessed as reduction in cell viability measured after 1 to 2 hrs by MTS colorimetric assay
[PMID: 35571875]
體外研究
(In Vitro)

The cells appear and grow normally at all concentrations of GS-441524 and fail to uptake the fluorescent dye CellTox Green at 24 h. The cytotoxic concentration-50% (CC50) is therefore>100 μM. The effective concentration-50% (EC50) of GS-441524 is calculated to be 0.78 μM[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
體內(nèi)研究
(In Vivo)

All 10 treated cats have a rapid response to treatment and lymphocyte levels and rectal temperatures return to pre-infection levels and levels of the two asymptomatic cats. All ten of the once or twice treated cats have remained normal to date (more than eight months post infection). Injections cause a transient "stinging" reaction in some cats within 10 s of compound administration. Localized and transient pain is evidenced by unusual posturing, licking at the injection site and/or vocalizations that last for approximately 30-60 s after injection. Injection reactions are more pronounced in some animals relative to others and reactions are inconsistent from one injection to the next and decreas over time[1].
Remdesivi (IV injection) in NHP results in GS-441524 being present in serum at concentrations 1000-fold higher than Remdesivir throughout a 7-day treatment course[3].

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

291.26

Formula

C12H13N5O4
CAS 號
性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.
儲存方式
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)胞實驗： 

DMSO 中的溶解度 : 83.33 mg/mL (286.10 mM; 超聲助溶; 吸濕的 DMSO 對產(chǎn)品的溶解度有顯著影響，請使用新開封的 DMSO)

配制儲備液
濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg
1 mM 3.4334 mL 17.1668 mL 34.3336 mL
5 mM 0.6867 mL 3.4334 mL 6.8667 mL
查看完整儲備液配制表

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

  • 摩爾計算器

  • 稀釋計算器

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

質(zhì)量
=
濃度
×
體積
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

濃度 (start)

C1

×
體積 (start)

V1

=
濃度 (final)

C2

×
體積 (final)

V2

動物實驗：

請根據(jù)您的 實驗動物和給藥方式 選擇適當(dāng)?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；體內(nèi)實驗的工作液，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

    請依序添加每種溶劑： 5% Ethanol    30% Propylene glycol    45% PEG400    20% Water (pH 1.5 with HCL)

    Solubility: 10 mg/mL (34.33 mM); 澄清溶液; 超聲助溶; 酸性條件溶解 (HCL 調(diào)節(jié)，pH≈2)

  • 方案 二

    請依序添加每種溶劑： 5% DMSO    40% PEG300    5% Tween-80    50% Saline

    Solubility: ≥ 2.75 mg/mL (9.44 mM); 澄清溶液

動物溶解方案計算器
請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

g

每只動物的給藥體積

μL

動物數(shù)量

只
由于實驗過程有損耗，建議您多配一只動物的量
請輸入您的動物體內(nèi)配方組成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的動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。
計算結(jié)果
工作液所需濃度 : mg/mL
儲備液配制方法 : mg 藥物溶于 μL  DMSO（母液濃度為 mg/mL）。
您所需的儲備液濃度超過該產(chǎn)品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術(shù)支持聯(lián)系。
動物實驗體內(nèi)工作液的配制方法 : 取 μL DMSO 儲備液，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，請謹(jǐn)慎選擇該方案。
請確保第一步儲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: 99.89%

參考文獻(xiàn)
Cell Assay

To determine the toxicity of GS-441524 to CRFK cells n, CRFK cells are treated with 100, 33.3, 11.1, 3.7 or 1.2 μM GS-441524 for 24 h[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Cats[1]
The 10 cats that developed disease signs are divided into two groups and treated with either 5 mg/kg (Group A; n=5) or 2 mg/kg (Group B; n=5) GS-441524 SC q24 h starting three days after unequivocal clinical evidence of FIP (days 12-19 post infection). The two cats that do not develop disease signs serve as controls for normal blood lymphocyte counts and rectal temperature[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻(xiàn)

完整儲備液配制表

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

可選溶劑 濃度 溶劑體積 質(zhì)量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.4334 mL 17.1668 mL 34.3336 mL 85.8340 mL
5 mM 0.6867 mL 3.4334 mL 6.8667 mL 17.1668 mL
10 mM 0.3433 mL 1.7167 mL 3.4334 mL 8.5834 mL
15 mM 0.2289 mL 1.1445 mL 2.2889 mL 5.7223 mL
20 mM 0.1717 mL 0.8583 mL 1.7167 mL 4.2917 mL
25 mM 0.1373 mL 0.6867 mL 1.3733 mL 3.4334 mL
30 mM 0.1144 mL 0.5722 mL 1.1445 mL 2.8611 mL
40 mM 0.0858 mL 0.4292 mL 0.8583 mL 2.1458 mL
50 mM 0.0687 mL 0.3433 mL 0.6867 mL 1.7167 mL
60 mM 0.0572 mL 0.2861 mL 0.5722 mL 1.4306 mL
80 mM 0.0429 mL 0.2146 mL 0.4292 mL 1.0729 mL
100 mM 0.0343 mL 0.1717 mL 0.3433 mL 0.8583 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.

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產(chǎn)品名稱：
GS-441524
目錄號：
HY-103586
需求量：