Keap1-Nrf2-IN-1|cas:2232112-72-8|西域试剂

Keap1-Nrf2-IN-1,98.08%

产品编号：Bellancom-126245| CAS NO：2232112-72-8| 分子式：C₂₄H₂₄N₂O₇S| 分子量：484.52

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货号	价格	库存与货期
Bellancom-126245	￥4500.00	杭州北京（现货）
Bellancom-126245	￥7500.00	杭州北京（现货）
Bellancom-126245	￥22500.00	杭州北京（现货）
Bellancom-126245	￥33500.00	杭州北京（现货）

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Keap1-Nrf2-IN-1

产品介绍

Keap1-Nrf2-IN-1 是一种 Keap1-Nrf2 蛋白-蛋白相互作用抑制剂，对 Keap1 蛋白作用的 IC₅₀ 值为 43 nM。Keap1-Nrf2-IN-1 能激活 Nrf2 调节的细胞保护反应，并对乙酰氨基酚诱导的肝损伤产生拮抗作用。

生物活性

Keap1-Nrf2-IN-1 is a Keap1 (Kelch-like ECH-associated protein 1)-Nrf2 (nuclear factor erythroid 2-related factor 2) protein-protein interaction inhibitor, and with an IC₅₀ of 43 nM for Keap1 protein. Keap1-Nrf2-IN-1 activates Nrf2-regulated cytoprotective response and antagonizes Acetaminophen-induced liver injury.

体外研究

Keap1-Nrf2-IN-1 (compound 35) increases the mRNA level of Nrf2-regulated genes, NEFL2L (encoding Nrf2 protein), HO-1, NQO-1, and GCLM, in L02 cells at a concentration-dependent manner.
Keap1-Nrf2-IN-1 (0.1-10 μM; 12 hours) can concentration dependently up-regulate the protein level of Nrf2, heme oxygen-1(HO-1), NAD(P)H dehydrogenase (quinone) 1 (NQO-1), and glutamate-cysteine ligase regulatory subunit (GCLM) in L02 cells.
Keap1-Nrf2-IN-1 (1-20 μM; 12 hours) produces cytoprotective effects against Acetaminophen (HY-66005)-induced injury in L02 cells.

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

Western Blot Analysis

Cell Line:	L02 cells
Concentration:	0.1 μM, 1 μM, 5 μM, 10 μM
Incubation Time:	12 hours
Result:	Up-regulated the protein levels of Nrf2 and Nrf2 downstream proteins.

体内研究
(In Vivo)

Keap1-Nrf2-IN-1 (40 mg/kg; i.p.) antagonizes Acetaminophen-induced liver injury in vivo models.

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

Animal Model:	6-8 weeks female C57BL/6 mice (18-20 g)
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection
Result:	Ameliorated the pathological symptoms in the Acetaminophen (400 mg/kg; i.p.)-induced mouse model of acute liver injury.

体内研究

Keap1-Nrf2-IN-1 (40 mg/kg; i.p.) antagonizes Acetaminophen-induced liver injury in vivo models.

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

Animal Model:	6-8 weeks female C57BL/6 mice (18-20 g)
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection
Result:	Ameliorated the pathological symptoms in the Acetaminophen (400 mg/kg; i.p.)-induced mouse model of acute liver injury.

体内研究

Keap1-Nrf2-IN-1 (40 mg/kg; i.p.) antagonizes Acetaminophen-induced liver injury in vivo models.

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

Animal Model:	6-8 weeks female C57BL/6 mice (18-20 g)
Dosage:	40 mg/kg
Administration:	Intraperitoneal injection
Result:	Ameliorated the pathological symptoms in the Acetaminophen (400 mg/kg; i.p.)-induced mouse model of acute liver injury.

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (206.39 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0639 mL	10.3195 mL	20.6390 mL
5 mM	0.4128 mL	2.0639 mL	4.1278 mL
10 mM	0.2064 mL	1.0319 mL	2.0639 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。-80°C 储存时，请在 6 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% (20% SBE-β-CD in saline)
Solubility: ≥ 4.55 mg/mL (9.39 mM); Clear solution

此方案可获得 ≥ 4.55 mg/mL (9.39 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 45.5 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
2.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.16 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.5 mg/mL (5.16 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.16 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。