AS 1949490|1203680-76-5|-陌孚医药/Medlife

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AS 1949490

目录号: PC15241 纯度: ≥98%

CAS No. :1203680-76-5

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中文名称

AS 1949490

中文别名

3-[(4-氯苯基)甲氧基]-N-[(1S)-1-苯基乙基]-2-噻吩甲酰胺

英文名称

AS 1949490

英文别名

3-[(4-Chlorobenzyl)oxy]-N-[(1S)-1-phenylethyl]-2-thiophenecarboxa mide;AS 1949490;AS-1949490;3-[(4-Chlorophenyl)Methoxy]-N-[(1S)-1-phenylethyl]thiophene-2-carboxaMide;3-[(4-Chlorophenyl)methoxy]-N-[(1S)-1-phenylethyl]- 2-thiophenecarboxamide;AS1949490

Cas No.

1203680-76-5

分子式

C₂₀H₁₈NO₂Scl

分子量

371.88

包装储存

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

AS1949490 is a potent, orally active, selective SHIP2 phosphatase inhibitor with IC₅₀ values of 0.34, 0.62, 13, >50, >50, and >50 μM for Mouse SHIP2, Human SHIP2, Human SHIP1, Human PTEN, Human synaptojanin, and Human myotubularin, respectively. AS1949490 increases the phosphorylation of Akt, glucose consumption and glucose uptake. AS1949490 activates intracellular insulin signalling pathways. AS1949490 can be used for research of diabetes.

性状

Solid

IC50 & Target[1][2]

IC50: 0.34 nM (Mouse SHIP2), 0.62 nM (Human SHIP2), 13 nM (Human SHIP1), >50 nM (Human PTEN), >50 nM (Human synaptojanin), and >50 μM (Human myotubularin).

体外研究(In Vitro)

AS1949490 (0-16 μM; 15 min; L6 myotubes) increases insulin-induced phosphorylation of Akt.
AS1949490 (0-10 μM; 48 h) activates glucose metabolism and stimulates glucose uptake activity in L6 myotubes.
AS1949490 (0-10 μM; 24 h; L6 myotubes) decreases the level of insulin-induced gluconeogenesis.
AS1949490 (10 μM; 48 h) activates glucose metabolism via up-regulation of GLUT1 gene in L6 myotubes.

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

Western Blot Analysis

Cell Line:	L6 myotubes
Concentration:	0, 4, 8, and 16 μM; 1 nM (insulin)
Incubation Time:	15 minutes
Result:	Increased insulin-induced phosphorylation of Akt in a dose-dependent manner.

Western Blot Analysis

Cell Line:	L6 myotubes
Concentration:	10 μM
Incubation Time:	48 hours
Result:	Increased GLUT1 but not GLUT4 mRNA expression in L6 myotubes.

体内研究(In Vivo)

AS1949490 (300 mg/kg; p.o.; twice daily, for 7 or 10 d) decreases plasma glucose and activates intracellular insulin signalling in diabetic mice. AS1949490 (300 mg/kg; p.o.; once, for 8 h; male ICR mice) suppresses gluconeogenesis and the expression of related genes.

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

Animal Model:	Male C57BL/KsJ Jcl-dbm mice and db/+db mice
Dosage:	300 mg/kg
Administration:	Oral administration; twice daily, for 7 or 10 days
Result:	Decreased plasma glucose (23% reduction, relative to vehicle). Reduced fasting blood glucose (37% reduction, relative to vehicle) and the area under the blood glucose concentration time curve (AUC). Increased the phosphorylation of GSK3β in the liver without changing the overall levels of GSK3β protein.

Animal Model:	Male ICR mice (6 weeks of age)
Dosage:	300 mg/kg
Administration:	Oral administration; once, for 8 hours
Result:	Reduced an approximately 50% of both PEPCK and G6Pase mRNA levels.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
In solvent	-80°C	6 months
	-20°C	1 month

参考文献

[1]. Suwa A, et, al. Discovery and functional characterization of a novel small molecule inhibitor of the intracellular phosphatase, SHIP2. Br J Pharmacol. 2009 Oct;158(3):879-87. [Information]

[2]. Suwa A, et, al. Glucose metabolism activation by SHIP2 inhibitors via up-regulation of GLUT1 gene in L6 myotubes. Eur J Pharmacol. 2010 Sep 10;642(1-3):177-82. [Information]

溶解度数据

体外研究:

DMSO : 50 mg/mL (134.45 mM; Need ultrasonic and warming)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6890 mL	13.4452 mL	26.8904 mL
5 mM	0.5378 mL	2.6890 mL	5.3781 mL
10 mM	0.2689 mL	1.3445 mL	2.6890 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 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.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.59 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.59 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 ddH?O 中，得到澄清透明的生理盐水溶液

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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