TH5487|cas:2304947-71-3|西域试剂

TH5487,99.23%

产品编号：Bellancom-125276| CAS NO：2304947-71-3| 分子式：C₁₉H₁₈BrIN₄O₂| 分子量：541.18

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货号	价格	库存与货期
Bellancom-125276	￥1180.00	杭州北京（现货）
Bellancom-125276	￥2000.00	杭州北京（现货）
Bellancom-125276	￥7000.00	杭州北京（现货）
Bellancom-125276	￥13000.00	杭州北京（现货）

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TH5487

产品介绍

TH5487 是一种有效的 8-氧鸟嘌呤 DNA 糖基化酶1 (OGG1) 抑制剂，IC₅₀ 为342 nM，TH5487 阻止 OGG1 识别其 DNA 底物，抑制 DNA 修复和修饰 OGG1 染色质动力学，从而抑制促炎基因。

生物活性

TH5487 is a potent 8-oxoguanine DNA glycosylase 1 (OGG1) inhibitor with an IC₅₀ of 342 nM. TH5487 stops OGG1 from recognizing its DNA substrate, inhibits DNA repair and modifies OGG1 chromatin dynamics, which results in the inhibition of proinflammatory pathway genes.

体外研究

TH5487 (5 μM; 1 hour) decreases TNFα- and LPS-induced proinflammatory gene expression to near pretreatment levels.
TH5487 (0-10 μM; 1 hour) perturbs binding of NF-κB to 8-oxoG–containing synthetic DNA in nuclear extracts from MLE 12 or hSAEC cells.

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

RT-PCR

Cell Line:	Murine airway epithelial cell line (MLE 12); Diploid human small-airway epithelial cell (hSAECs)
Concentration:	5 μM
Incubation Time:	1 hour
Result:	Inhibited proinflammatory gene expression dose-dependently.

Western Blot Analysis

Cell Line:	Murine airway epithelial cell line (MLE 12); Diploid human small-airway epithelial cell (hSAECs)
Concentration:	2.5 μM; 5 μM; 10 μM
Incubation Time:	1 hour
Result:	Decreased p50-p65 and p50-p50 expression in a dose dependent manner.

体内研究
(In Vivo)

TH5487 (prophylactic intraperitoneally injection; 8-30 mg/kg; 1-9 hours) decreases TNFα or LPS induced the robust recruitment of neutrophils to the airways, and reduces the pulmonary neutrophil count in a time-dependent manner.

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

Animal Model:	Eightweek-old female and male BALB/c mice
Dosage:	8 mg/kg, 15 mg/kg, 30 mg/kg
Administration:	Prophylactic intraperitoneally injection; 8-30 mg/kg; 1-9 hours
Result:	InterruptedTNFα-induced ongoing inflammatory processes.

体内研究

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

Animal Model:	Eightweek-old female and male BALB/c mice
Dosage:	8 mg/kg, 15 mg/kg, 30 mg/kg
Administration:	Prophylactic intraperitoneally injection; 8-30 mg/kg; 1-9 hours
Result:	InterruptedTNFα-induced ongoing inflammatory processes.

体内研究

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

Animal Model:	Eightweek-old female and male BALB/c mice
Dosage:	8 mg/kg, 15 mg/kg, 30 mg/kg
Administration:	Prophylactic intraperitoneally injection; 8-30 mg/kg; 1-9 hours
Result:	InterruptedTNFα-induced ongoing inflammatory processes.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (46.20 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8478 mL	9.2391 mL	18.4781 mL
5 mM	0.3696 mL	1.8478 mL	3.6956 mL
10 mM	0.1848 mL	0.9239 mL	1.8478 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 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (3.84 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (3.84 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