BioE-1115|cas:1268863-35-9|西域试剂

BioE-1115,98.08%

产品编号：Bellancom-129571| CAS NO：1268863-35-9| 分子式：C₁₉H₁₈FN₃O₂| 分子量：339.36

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货号	价格	库存与货期
Bellancom-129571	￥2900.00	杭州北京（现货）
Bellancom-129571	￥4800.00	杭州北京（现货）
Bellancom-129571	￥11500.00	杭州北京（现货）

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BioE-1115

产品介绍

BioE-1115 是一种高度选择性和有效的 PAS 激酶 (PASK) 抑制剂，其 IC₅₀ 值约为 4 nM。BioE-1115 还是一种有效的酪蛋白激酶 2α (casein kinase 2α) 抑制剂，IC₅₀ 值约为 10 μM。

生物活性

BioE-1115 is a highly selective and potent PAS kinase (PASK) inhibitor with an IC₅₀ of ~4 nM. BioE-1115 is also a potent casein kinase 2α inhibitor with an IC₅₀ of ~10 μM.

体外研究

In the presence of BioE-1115, shows a dose-dependent loss of PASK phosphorylation, with an IC₅₀ of ~1μM in HEK293 cells.
At the concentrations above 10μM, BioE-1115 treatment shows a significant reduction in SREBP activity, without any observable effects on cell morphology or growth rate in HepG2 cells.

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

体内研究

BioE-1115 (1-100 mg/kg; oral gavage; daily; for 7 days; male Sprague-Dawley rats) treatment shows a dose-dependent suppression of the expression of Gpat1, Fasn and all other SREBP-1c target genes analyzed. SREBP-1 maturation in liver is also suppressed in BioE-1115 treated rats at 10, 30 and 100 mg/kg doses. A calculated measure of insulin resistance, HOMA-IR, is decreased in a dose-dependent manner by BioE-1115 administration. Hepatic and serum TAG are decreased in a dose-dependent manner by BioE-1115 administration. BioE-1115 treatment causes a significant decrease in serum glucose. Both SREBP-1c and SREBP-1a mRNA are modestly decreased at the highest doses. Neither dose of BioE-1115 causes a significant change in either liver weight or body weight.

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

Animal Model:	Male Sprague-Dawley rats (12 weeks of age; 129.4 ± 0.63 g) fed with high fructose diet
Dosage:	1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg
Administration:	Oral gavage; daily; for 7 days
Result:	Treated with 10, 30 and 100 mg/kg, showed a dose-dependent suppression of the expression of Gpat1, Fasn and all other SREBP-1c target genes analyzed. Decreased hepatic expression of lipogenic SREBP-1c target genes, decreased serum triglycerides and partially reversed insulin resistance.

体内研究

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

Animal Model:	Male Sprague-Dawley rats (12 weeks of age; 129.4 ± 0.63 g) fed with high fructose diet
Dosage:	1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg
Administration:	Oral gavage; daily; for 7 days
Result:	Treated with 10, 30 and 100 mg/kg, showed a dose-dependent suppression of the expression of Gpat1, Fasn and all other SREBP-1c target genes analyzed. Decreased hepatic expression of lipogenic SREBP-1c target genes, decreased serum triglycerides and partially reversed insulin resistance.

性状

Solid

溶解性数据

In Vitro:

DMSO : 62.5 mg/mL (184.17 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.9467 mL	14.7336 mL	29.4672 mL
5 mM	0.5893 mL	2.9467 mL	5.8934 mL
10 mM	0.2947 mL	1.4734 mL	2.9467 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 (6.13 mM); Suspended solution; Need ultrasonic

此方案可获得 2.08 mg/mL (6.13 mM) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
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 (6.13 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (6.13 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。