GS143|cas:916232-21-8|西域试剂

GS143,98.30%

产品编号：Bellancom-110261| CAS NO：916232-21-8| 分子式：C₂₈H₁₉FN₂O₄| 分子量：466.46

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货号	价格	库存与货期
Bellancom-110261	￥1000.00	杭州北京（现货）
Bellancom-110261	￥1600.00	杭州北京（现货）
Bellancom-110261	￥3200.00	杭州北京（现货）
Bellancom-110261	￥5000.00	杭州北京（现货）
Bellancom-110261	￥8500.00	杭州北京（现货）

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GS143

产品介绍

GS143 是一种选择性的 IκBα 泛素化抑制剂，对于 SCF^βTrCP1 介导的 IκBα 泛素化作用的 IC₅₀ 为 5.2 μM。GS143 抑制靶基因的 NF-κB 活化和转录，并且不抑制蛋白酶体的活性，并具有抗哮喘作用。

生物活性

GS143 is a selective IκBα ubiquitination inhibitor with an IC₅₀ of 5.2 μM for SCF^βTrCP1-mediated IκBα ubiquitylation. GS143 suppresses NF-κB activation and transcription of target genes and does not inhibit proteasome activity. GS143 has anti-asthma effect.

体外研究

GS143 (10 μM or 20 μM) inhibits antigen-induced differentiation of Th2 cells but not of Th1 cells in vitro. The IL-4 production in Th2-polarizing condition is markedly suppressed by GS143 in a dose-dependent manner.
GS143 suppresses the transcription of TNFα-induced NF-κB with a mean IC₅₀ value of 10.5 μM. GS143 also inhibits TNFα-induced expression of ICAM-1 in HT-29 colon cancer cells with an IC₅₀ value of 6.1 μM. The production levels of TNFα and IL-1β in LPS-activated THP-1 cells are inhibited with IC₅₀ values of 5.3 μM and 2.1 μM, respectively. GS143 does not inhibit p53 and β-catenin.

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

体内研究

GS143 (16-32 μg/body; intranasal administration; once; BALB/c mice) treatment suppresses antigen-induced NF-κB activation in the lung of sensitized mice. GS143 treatment also inhibits antigen-induced eosinophil and lymphocyte recruitment into the airways and the expression of Th2 cytokines and eotaxin in the airways.

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

Animal Model:	BALB/c mice (age 7-8weeks) injected with ovalbumin
Dosage:	16 μg/body or 32 μg/body
Administration:	Intranasal administration; once
Result:	Suppressed antigen-induced NF-κB activation in the lung of sensitized mice.

体内研究

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

Animal Model:	BALB/c mice (age 7-8weeks) injected with ovalbumin
Dosage:	16 μg/body or 32 μg/body
Administration:	Intranasal administration; once
Result:	Suppressed antigen-induced NF-κB activation in the lung of sensitized mice.

性状

Solid

溶解性数据

In Vitro:

DMSO : 37.5 mg/mL (80.39 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1438 mL	10.7190 mL	21.4381 mL
5 mM	0.4288 mL	2.1438 mL	4.2876 mL
10 mM	0.2144 mL	1.0719 mL	2.1438 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： 10% DMSO 90% corn oil
Solubility: 2.08 mg/mL (4.46 mM); Clear solution; Need ultrasonic

此方案可获得 2.08 mg/mL (4.46 mM) 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。
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: 1.88 mg/mL (4.03 mM); Suspended solution; Need ultrasonic

此方案可获得 1.88 mg/mL (4.03 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 18.8 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