B022|cas:1202764-53-1|西域试剂

B022,99.76%

产品编号：Bellancom-120501| CAS NO：1202764-53-1| 分子式：C₁₉H₁₆ClN₅OS| 分子量：397.88

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货号	价格	库存与货期
Bellancom-120501	￥2050.00	杭州北京（现货）
Bellancom-120501	￥3500.00	杭州北京（现货）
Bellancom-120501	￥12500.00	杭州北京（现货）
Bellancom-120501	￥22000.00	杭州北京（现货）

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B022

产品介绍

B022 是一种有效的选择性的 NF-κB 诱导激酶 (NIK) 抑制剂，K_i 为 4.2 nM，IC₅₀ 为 15.1 nM。B022 可保护肝脏免受毒素引起的炎症，氧化应激和伤害。

生物活性

B022 is a potent and selective NF-κB-inducing kinase (NIK) inhibitor (K_i of 4.2 nM; IC₅₀=15.1 nM). B022 protects liver from toxin-induced inflammation, oxidative stress, and injury.

体外研究

B022 (0-5 μM; 12 hours; Hepa1 cells) treatment suppresses NIK-induced p52 formation in a dose-dependent manner.
B022 (0-5 μM; 12 hours; Hepa1 cells) treatment for 8 h completely blocks NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5.
B022 prevents NIK- or H2O2-induced β cell death and also ameliorates streptozotocin (STZ)-induced β cell death and hyperglycemia.

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

Western Blot Analysis

Cell Line:	Hepa1 cells
Concentration:	0 μM, 0.5 μM, 5 μM
Incubation Time:	12 hours
Result:	Suppressed NIK-induced p52 formation in a dose-dependent manner.

RT-PCR

Cell Line:	Hepa1 cells
Concentration:	0 μM, 0.5 μM, 5 μM
Incubation Time:	12 hours
Result:	Dose-dependently blocked NIK-induced expression of chemokines, cytokines, and iNOS in these cells. Completely blocked NIK-induced expression of TNF-a, IL-6, iNOS, CCL2, and CXCL5.

体内研究
(In Vivo)

B022 (30 mg/kg; intravenous injection; twice a day; for 10 days; STOP-NIK male mice) treatment inhibits NIK-triggered liver inflammation and injury in STOP-NIK mice infected with cre adenoviruses.

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

Animal Model:	STOP-NIK male mice (8 weeks) infected with Ad-cre
Dosage:	30 mg/kg
Administration:	Intravenous injection; twice a day; for 10 days
Result:	Completely prevents the lethal effect of abnormally high levels of hepatic NIK in mice. Inhibited the majority of the deteriorating effects of aberrant activation of hepatic NIK.

体内研究

B022 (30 mg/kg; intravenous injection; twice a day; for 10 days; STOP-NIK male mice) treatment inhibits NIK-triggered liver inflammation and injury in STOP-NIK mice infected with cre adenoviruses.

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

Animal Model:	STOP-NIK male mice (8 weeks) infected with Ad-cre
Dosage:	30 mg/kg
Administration:	Intravenous injection; twice a day; for 10 days
Result:	Completely prevents the lethal effect of abnormally high levels of hepatic NIK in mice. Inhibited the majority of the deteriorating effects of aberrant activation of hepatic NIK.

体内研究

B022 (30 mg/kg; intravenous injection; twice a day; for 10 days; STOP-NIK male mice) treatment inhibits NIK-triggered liver inflammation and injury in STOP-NIK mice infected with cre adenoviruses.

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

Animal Model:	STOP-NIK male mice (8 weeks) infected with Ad-cre
Dosage:	30 mg/kg
Administration:	Intravenous injection; twice a day; for 10 days
Result:	Completely prevents the lethal effect of abnormally high levels of hepatic NIK in mice. Inhibited the majority of the deteriorating effects of aberrant activation of hepatic NIK.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (628.33 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.5133 mL	12.5666 mL	25.1332 mL
5 mM	0.5027 mL	2.5133 mL	5.0266 mL
10 mM	0.2513 mL	1.2567 mL	2.5133 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 (5.23 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.23 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
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.23 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.23 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。