ASK1-IN-2|cas:2541792-70-3|西域试剂

ASK1-IN-2,98.49%

产品编号：Bellancom-131969| CAS NO：2541792-70-3| 分子式：C₁₉H₁₇FN₆O| 分子量：364.38

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-131969	￥3500.00	杭州北京（现货）
Bellancom-131969	￥5800.00	杭州北京（现货）
Bellancom-131969	￥11000.00	杭州北京（现货）
Bellancom-131969	￥17000.00	杭州北京（现货）
Bellancom-131969	￥25000.00	杭州北京（现货）

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ASK1-IN-2

产品介绍

ASK1-IN-2 是一种有效的，具有口服活性的凋亡信号调节激酶 1 (ASK1) 抑制剂，IC₅₀ 值为 32.8 nM。ASK1-IN-2 可用于溃疡性结肠炎的研究。

生物活性

ASK1-IN-2 is a potent and orally active inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with an IC₅₀ of 32.8 nM. ASK1-IN-2 can be used for the research of ulcerative colitis.

体外研究

ASK1-IN-2 (compound 19) (10 mM; 1 h) inhibits the luciferase reporter activity in AP1-HEK293 cells, with inhibition rate of 95.59%.

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

体内研究

ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) improves dextran sulphate sodium (DSS)-induced ulcerative colitis (UC) in mice.
ASK1-IN-2 (25 mg/kg; p.o. daily for 7 d) blocks ASK1-p38/JNK signaling pathways and reduces inflammatory cytokine levels in DSS-induced mouse colon tissues.
ASK1-IN-2 (1 mg/kg; i.v.) shows low clearance (CL=1.38 L/h/kg) and moderate half-life (T_1/2=1.45 h) in rats.
ASK1-IN-2 (10 mg/kg; p.o.) shows high oral exposure (AUC_last=4517 h•ng/mL), 62.2% oral bioavailability and acceptable terminal half-life (T_1/2=2.31 h) in rats.

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

Animal Model:	Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water
Dosage:	25 mg/kg
Administration:	P.o. daily for 7 days
Result:	Induced a significant recovery of body weight loss, with an increase of +11.2%. Decreased the disease activity index (DAI) score about a 2 unit. Significantly prevented colon shortening. Attenuated a severe colonic tissue damage and infiltration of inflammatory cells.

Animal Model:	Male SD rats
Dosage:	1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:	I.v. and p.o. administration
Result:	I.v.: CL=1.38 L/h/kg; T_1/2=1.45 h. P.o.: AUC_last=4517 h•ng/mL; F=62.2%; T_1/2=2.31 h.

体内研究

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

Animal Model:	Male ICR mice (18-22 g, 6-8 weeks) were given 3% DSS (w/v) orally in drinking water
Dosage:	25 mg/kg
Administration:	P.o. daily for 7 days
Result:	Induced a significant recovery of body weight loss, with an increase of +11.2%. Decreased the disease activity index (DAI) score about a 2 unit. Significantly prevented colon shortening. Attenuated a severe colonic tissue damage and infiltration of inflammatory cells.

Animal Model:	Male SD rats
Dosage:	1 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration:	I.v. and p.o. administration
Result:	I.v.: CL=1.38 L/h/kg; T_1/2=1.45 h. P.o.: AUC_last=4517 h•ng/mL; F=62.2%; T_1/2=2.31 h.

性状

Solid

溶解性数据

In Vitro:

DMSO : 250 mg/mL (686.10 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7444 mL	13.7219 mL	27.4439 mL
5 mM	0.5489 mL	2.7444 mL	5.4888 mL
10 mM	0.2744 mL	1.3722 mL	2.7444 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 (5.71 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.71 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 (5.71 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.71 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。