规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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2mg |
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5mg |
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10mg |
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50mg |
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100mg |
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体外研究 (In Vitro) |
HEK293 细胞中的 IC50 约为 1 μM,在 BioE-1115 存在的情况下,该剂量被认为会导致 PASK 磷酸化丧失 [1]。当BioE-1115以10μM的剂量应用时,HepG2细胞生长速率和细胞形状没有表现出任何明显的变化,但SREBP活性显着降低[1]。
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体内研究 (In Vivo) |
在 BioE-1115 中检查的 Gpat1、Fasn 和所有其他 SREBP-1c 靶基因表达的剂量(1-100 mg/kg;临界强饲法;每天;持续 7 天;美容 Sprague-Dawley 构建体)被发现是剂量调节剂。曼哈顿的 SREBP-1 饱和度在 10、30 和 100 mg/kg 剂量的 1115 处理下也受到抑制。BioE-1115 以剂量依赖性方式应用以降低 HOMA-IR(胰岛素抵抗的计算标记物)。通过使用 BioE-1115,肝脏和血清 TAG 以剂量依赖性方式降低。接受 BioE-1115 治疗后,血清血糖水平显着下降。在最高剂量下,SREBP-1c 和 SREBP-1a 的 mRNA 持续下降。
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动物实验 |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rats (12 weeks old; 129.4 ± 0.63 g) fed a high-fructose diet [1]
Doses: 1 mg of BioE-1115 did not cause significant changes in body weight or weight [1]. /kg, 3 mg/kg, 10 mg/kg, 30 mg/kg and 100 mg/kg Route of Administration: po (oral gavage); daily; 7-day Experimental Results: Treatment with 10, 30 and 100 mg/kg, shown Dose-dependent inhibition of Gpat1, Fasn, and all other SREBP-1c target gene expression analyzed. Hepatic expression of lipogenic SREBP-1c target genes was diminished, serum triglycerides were diminished and insulin resistance was partially reversed. |
参考文献 |
[1]. Wu X, et al. PAS kinase drives lipogenesis through SREBP-1 maturation. Cell Rep. 2014 Jul 10;8(1):242-55.
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分子式 |
C₁₉H₁₈FN₃O₂
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分子量 |
339.36
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CAS号 |
1268863-35-9
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相关CAS号 |
1268863-35-9
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SMILES |
O=C(C1=CC=C2N=C(C3=CC=C(F)C=C3)C(N(C)C(C)C)=NC2=C1)O
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别名 |
BioE-1115BioE 1115BioE1115
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存储方式 |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
运输条件 |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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溶解度 (体外) |
DMSO : ~62.5 mg/mL (~184.17 mM)
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溶解度 (体内) |
Solubility in Formulation 1: 2.08 mg/mL (6.13 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.13 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. 请根据您的实验动物和给药方式选择适当的溶解配方/方案: 1、请先配制澄清的储备液(如:用DMSO配置50 或 100 mg/mL母液(储备液)); 2、取适量母液,按从左到右的顺序依次添加助溶剂,澄清后再加入下一助溶剂。以 下列配方为例说明 (注意此配方只用于说明,并不一定代表此产品 的实际溶解配方): 10% DMSO → 40% PEG300 → 5% Tween-80 → 45% ddH2O (或 saline); 假设最终工作液的体积为 1 mL, 浓度为5 mg/mL: 取 100 μL 50 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀/澄清;向上述体系中加入50 μL Tween-80,混合均匀/澄清;然后继续加入450 μL ddH2O (或 saline)定容至 1 mL; 3、溶剂前显示的百分比是指该溶剂在最终溶液/工作液中的体积所占比例; 4、 如产品在配制过程中出现沉淀/析出,可通过加热(≤50℃)或超声的方式助溶; 5、为保证最佳实验结果,工作液请现配现用! 6、如不确定怎么将母液配置成体内动物实验的工作液,请查看说明书或联系我们; 7、 以上所有助溶剂都可在 Invivochem.cn网站购买。 |
制备储备液 | 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 |
1、根据实验需要选择合适的溶剂配制储备液 (母液):对于大多数产品,InvivoChem推荐用DMSO配置母液 (比如:5、10、20mM或者10、20、50 mg/mL浓度),个别水溶性高的产品可直接溶于水。产品在DMSO 、水或其他溶剂中的具体溶解度详见上”溶解度 (体外)”部分;
2、如果您找不到您想要的溶解度信息,或者很难将产品溶解在溶液中,请联系我们;
3、建议使用下列计算器进行相关计算(摩尔浓度计算器、稀释计算器、分子量计算器、重组计算器等);
4、母液配好之后,将其分装到常规用量,并储存在-20°C或-80°C,尽量减少反复冻融循环。
计算结果:
工作液浓度: mg/mL;
DMSO母液配制方法: mg 药物溶于 μL DMSO溶液(母液浓度 mg/mL)。如该浓度超过该批次药物DMSO溶解度,请首先与我们联系。
体内配方配制方法:取 μL DMSO母液,加入 μL PEG300,混匀澄清后加入μL Tween 80,混匀澄清后加入 μL ddH2O,混匀澄清。
(1) 请确保溶液澄清之后,再加入下一种溶剂 (助溶剂) 。可利用涡旋、超声或水浴加热等方法助溶;
(2) 一定要按顺序加入溶剂 (助溶剂) 。
BioE-1115 and BioE-1197 are PASK-specific inhibitors (A) The chemical structure of BioE-1115, BioE-1197 and BioE-1428. (B) Activity of the indicated kinases was measured in the presence of either vehicle or BioE-1115 and IC50s were measured. (C) Purified PASK protein kinase activity was assayed as in (B) in the presence of the indicated concentrations of BioE-1197, BioE-1428 or BioE-1115 and the percent of vehicle-treated activity is as indicated. (D) HEK293 cells expressing a Flag-tagged PASK protein were treated with the indicated concentrations of BioE-1115, BioE-1197 or BioE-1428. PASK activity was analyzed by ELISA with both phospho-Akt substrate antibody and pan-PASK antibody. The quantitated phospho/total PASK signal is plotted ± SEM. See also Figure S3 td> |