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

GS-441524 

目录号: HY-103586 纯度: 99.77%
产品使用指南

GS-441524 是 Remdesivir 的主要活性代谢物,活性更优于 Remdesivir ,感染冠状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

GS-441524 Chemical Structure

CAS No. : 1191237-69-0

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10 mM * 1 mL in DMSO ¥715
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5 mg ¥650
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10 mg ¥1105
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50 mg ¥2800
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100 mg ¥4500
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Top Publications Citing Use of Products
  • 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].

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
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 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 83.33 mg/mL (286.10 mM; Need ultrasonic)

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
*

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, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

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

  • 1.

    请依序添加每种溶剂: 5% ethanol, 30% propylene glycol, 45% PEG 400, 20% water (pH 1.5 with HCI)

    Solubility: 10 mg/mL (34.33 mM); Clear solution; Need ultrasonic and adjust pH to 2 with HCl

  • 2.

    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); Clear solution

  • 3.

    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); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.14 mM,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;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液
  • 4.

    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); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.14 mM,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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
  • 5.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (7.14 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (7.14 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    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。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献
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

纯度: 99.77%

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

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

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

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)
× = ×
C1   V1   C2   V2

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产品名称:
GS-441524
目录号:
HY-103586
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