JH-X-119-01|cas:2227368-54-7|西域试剂

JH-X-119-01,98.0%

产品编号：Bellancom-103017A| CAS NO：2227368-54-7| 分子式：C₂₅H₂₀N₆O₃| 分子量：452.46

本网站销售的所有产品仅用于工业应用或者科学研究等非医疗目的,不可用于人类或动物的临床诊断或者治疗,非药用,非食用，

货号	价格	库存与货期
Bellancom-103017A	￥1800.00	杭州北京（现货）
Bellancom-103017A	￥2700.00	杭州北京（现货）
Bellancom-103017A	￥4900.00	杭州北京（现货）
Bellancom-103017A	￥7300.00	杭州北京（现货）
Bellancom-103017A	￥9900.00	杭州北京（现货）

增值税发票√顺丰快递√订货电话：18601927057

JH-X-119-01

产品介绍

JH-X-119-01 是一种有效的选择性白介素 1 受体相关激酶 1 (IRAK1) 抑制剂。JH-X-119-01 可改善 LPS 诱导的小鼠败血症。JH-X-119-01 抑制 IRAK1，IC₅₀ 为 9 nM，而在浓度高达 10 μM 时对 IRAK4 也没有抑制作用。

生物活性

JH-X-119-01 is a potent and selective interleukin-1 receptor-associated kinases 1 (IRAK1) inhibitor. JH-X-119-01 ameliorates LPS-induced sepsis in mice. JH-X-119-01 inhibits IRAK1 biochemically with an apparent IC₅₀ of 9 nM while exhibiting no inhibition of IRAK4 at concentrations up to 10 μM.

体外研究

JH-X-119-01 (10 μM) decreases phosphorylation of NF-κB and mRNA levels of IL-6 and TNFα in LPS-treated macrophages in vitro. JH-X-119-01 selectively inhibits IRAK1 phosphorylation. JH-X-119-01 exhibits off-target inhibition of only two additional kinases, YSK4 and MEK3. Dose response analysis reveals an IC₅₀ of 57 nM for YSK4. JH-X-119-01 shows moderate cell killing effects in a panel of Waldenström’s macroglobulinemia (WM) cells, Diffused Large B-cell Lymphoma (DLBCL) cells, and lymphoma cells expressing mutant MYD88, with EC₅₀s ranging from 0.59 to 9.72 μM.

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

Western Blot Analysis

Cell Line:	RAW 264.7 cells and THP-1 cells
Concentration:	10 μM
Incubation Time:	15 minutes
Result:	Decreased LPS (100 ng/mL)-induced phosphorylation of IκBα and NF-κB-P65.

体内研究
(In Vivo)

JH-X-119-01 improves survival and decreases immunopathies of LPS-challenged mice. JH-X-119-01 increases survival of mice at the dose of 5 mg/kg body weight. Survival is further improved when the dose is increased to 10 mg/kg.

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

Animal Model:	C57BL/6 (20-22 g, male) mice
Dosage:	5 mg/kg and 10 mg/kg
Administration:	Intraperitoneally injected; 5 days
Result:	Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg.

体内研究

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

Animal Model:	C57BL/6 (20-22 g, male) mice
Dosage:	5 mg/kg and 10 mg/kg
Administration:	Intraperitoneally injected; 5 days
Result:	Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg.

体内研究

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

Animal Model:	C57BL/6 (20-22 g, male) mice
Dosage:	5 mg/kg and 10 mg/kg
Administration:	Intraperitoneally injected; 5 days
Result:	Protected mice from LPS (20 mg/kg)-induced sepsis. Survival at day 5 was 13.3% in control group where septic mice were treated by vehicle, while the values were 37.5% and 56.3% for 5 mg/kg and 10 mg/kg.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (552.54 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.2101 mL	11.0507 mL	22.1014 mL
5 mM	0.4420 mL	2.2101 mL	4.4203 mL
10 mM	0.2210 mL	1.1051 mL	2.2101 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: ≥ 1.98 mg/mL (4.38 mM); Clear solution

此方案可获得 ≥ 1.98 mg/mL (4.38 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 19.8 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