GS-441524

目录号: HY-103586 纯度: 99.77%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

GS-441524 是 Remdesivir 的主要活性代谢物，活性更优于 Remdesivir ，感染病毒的原代人肺和猫细胞的细胞模型中显示出相似的活性。 GS-441524 对猫传染性腹膜炎病毒 (FIPV) 有较强的抑制作用，对应的 EC₅₀ 值为 0.78 μM。

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GS-441524 Chemical Structure

CAS No. : 1191237-69-0

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规格	价格	是否有货
10 mM * 1 mL in DMSO	￥160	In-stock
50 mg	￥366	In-stock
100 mg	￥490	In-stock
200 mg		询价
500 mg		询价

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Customer Review

Other Forms of GS-441524:

MCE 顾客使用本产品发表的 23 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

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].

细胞效力
(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]

体外研究
(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.

体内研究
(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 号

1191237-69-0

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 : 83.33 mg/mL (286.10 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	3.4334 mL	17.1668 mL	34.3336 mL
5 mM	0.6867 mL	3.4334 mL	6.8667 mL
10 mM	0.3433 mL	1.7167 mL	3.4334 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： 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; 超声助溶; 酸性条件溶解 (HCL 调节，pH≈2)
方案二

请依序添加每种溶剂： 5% DMSO 40% PEG300 5% Tween-80 50% Saline
Solubility: ≥ 2.75 mg/mL (9.44 mM); 澄清溶液
方案三

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (7.14 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
方案四

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (7.14 mM); 澄清溶液

此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 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。
方案五

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (7.14 mM); 澄清溶液

此方案可获得 ≥ 2.08 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 20.8 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: 99.77%

选择批次：

Data Sheet (631 KB) SDS (252 KB)

COA (288 KB) HNMR (260 KB) RP-HPLC (109 KB)

产品使用指南 (1538 KB)

参考文献

[1]. Murphy BG, et al. The nucleoside analog GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. Vet Microbiol. 2018 Jun;219:226-233. [Content Brief]

[2]. Katherine Yang, et al. What Do We Know About Remdesivir Drug Interactions? Clin Transl Sci. 2020 May 13;10.1111/cts.12815. [Content Brief]

[3]. Victoria C. Yan, et al. Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment. ACS Med. Chem. Lett. 2020.

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.
参考文献	[1]. Murphy BG, et al. The nucleoside analog GS-441524 strongly inhibits feline infectious peritonitis (FIP) virus in tissue culture and experimental cat infection studies. Vet Microbiol. 2018 Jun;219:226-233. [Content Brief] [2]. Katherine Yang, et al. What Do We Know About Remdesivir Drug Interactions? Clin Transl Sci. 2020 May 13;10.1111/cts.12815. [Content Brief] [3]. Victoria C. Yan, et al. Advantages of the Parent Nucleoside GS-441524 over Remdesivir for Covid-19 Treatment. ACS Med. Chem. Lett. 2020.

GS-441524 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	3.4334 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.

Keywords:

GS-4415241191237-69-0GS441524GS 441524DNA/RNA SynthesisSARS-CoVSARS coronavirusfelineinfectiousperitonitisvirusFIPVInhibitorinhibitorinhibit

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GS-441524

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GS-441524

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GS-441524 相关抗体

MCE 顾客使用本产品发表的 23 篇科研文献

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参考文献

GS-441524 相关抗体:

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