BioE-1115 - CAS:1268863-35-9

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BioE-1115

目录号 : KM9280 CAS No. : 1268863-35-9 纯度 : 98%

Data Sheet 产品使用指南

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。

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg	询价	In-stock
200mg	询价	In-stock

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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.

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.

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.

分子式

C₁₉H₁₈FN₃O₂

分子量

339.36

CAS号

1268863-35-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

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。
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。