| 中文名称: | BVT948 | ||||
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| 英文名称: | BVT948 | ||||
| 别名: | 4-羟基-3,3-二甲基-2H-苯并[g]吲哚-2,5(3H)-二酮 4-HYDROXY-3,3-DIMETHYL-2H-BENZO[G]INDOLE-2,5(3H)-DIONE;4-HYDROXY-3,3-DIMETHYL-2H-BENZ[G]INDOLE-2,5(3H)-DIONE;BVT 948;3,3-dimethyl-1H-benzo[g]indole-2,4,5-trione;BVT-948;Tocris-2176;4-Hydroxy-3,3-dimethyl-2H-benzo[g]indole-2,5(3H)-dione | ||||
| CAS No: | 39674-97-0 | 分子式: | C14H11NO3 | 分子量: | 241.24 |
| CAS No: | 39674-97-0 | ||||
| 分子式: | C14H11NO3 | ||||
| 分子量: | 241.24 | ||||
基本信息
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产品编号： |
B10801 |
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产品名称： |
BVT948 |
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CAS: |
39674-97-0 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
两年 |
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分子量 |
241.24 |
-20℃ |
一个月 |
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化学名： |
4-Hydroxy-3,3-dimethyl-2H-benzo[g]indole-2,5(3H)-dione |
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Solubility (25°C)： |
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体外:
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DMSO |
48mg/mL(198.97mM) |
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Ethanol |
5mg/mL(20.72mM) |
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Water |
Insoluble |
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体内(现配现用): |
1.请依序添加每种溶剂：10% DMSO→40% PEG300→5% Tween-80→45% saline Solubility:≥2.08mg/mL(8.62mM);Clear solution |
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此⽅案可获得≥2.08mg/mL(8.62mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到400μL PEG300中，混合均匀；向上述体系中加⼊50μL Tween-80，混合均匀；然后继续加⼊450μL⽣理盐⽔定容⾄1mL。 |
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2.请依序添加每种溶剂：10% DMSO→90% (20% SBE-β-CD in saline) Solubility:≥2.08mg/mL(8.62mM);Clear solution |
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此⽅案可获得≥2.08mg/mL(8.62mM，饱和度未知)的澄清溶液。以1mL⼯作液为例，取100μL20.8mg/mL的澄清DMSO储备液加到900μL20%的SBE-β-CD⽣理盐⽔⽔溶液中，混合均匀。 |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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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。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
4.1452mL |
20.7262mL |
41.4525mL |
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5mM |
0.8290mL |
4.1452mL |
8.2905mL |
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10mM |
0.4145mL |
2.0726mL |
4.1452mL |
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50mM |
0.0829mL |
0.4145mL |
0.8290mL |
生物活性
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产品描述 |
一种蛋白酪氨酸磷酸酶 (PTP) 的抑制剂，也可以抑制几种细胞色素 P450 (P450) 异构体和赖氨酸甲基转移酶 SETD8 (KMT5A)。 |
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靶点 |
SHP-2 0.09μM |
YopH 0.7μM |
PTP1B 0.9μM |
LAR 1.5μM |
TCPTP 1.7μM |
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体外研究 |
Results show that the effect of BVT948 (BVT.948) is to strengthen the insulin signal and has no effects on the duration of the signal. BVT948 appears to be an effective inhibitor of both protein tyrosine phosphatases (PTP activity and P450 activity). BVT948 efficiently and selectively suppresses cellular H4 lysine 20 (H4K20me1) at doses lower than 5μM within 24 h. The cells treated with BVT948 recapitulate cell-cycle-arrest phenotypes similar to what are reported for knocking down SETD8 by RNAi. Treatment of MCF-7 cells with 0.5, 1 or 5μM of BVT948 for 24 h does not cause any significant changes in cell viability. BVT948 inhibits TPA-inducedmMP-9 up-regulation in a dose-dependent manner. Treatment with BVT948 inhibits TPA-stimulated NF-κB binding activity, but not AP-1 binding activity. BVT948 does not affect the MAPK phosphorylation by TPA. Treatment with BVT948 diminishes the TPA-induced cell invasion by 50% |
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体内研究 |
Results show that 3μMol/kg BVT948 (BVT.948) significantly enhances glucose clearance from the blood stream in response to insulin compare with vehicle-treated controls |
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推荐实验方法(仅供参考)
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Kinase Assay |
To determine the reversibility of the inhibition of protein tyrosine phosphatases (PTP) activity by BVT948 (BVT.948), 50ng of PTP1B is incubated in 100μL of assay buffer with 20μM BVT948 for 10 min in a concentration device. The sample is then centrifuged at 14,000 rpm at 4°C for 12 min. The concentrate is subsequently washed three times with 100μL of assay buffer followed by centrifugation. After washing, 190μL of assay buffer is added to the sample, increasing the volume to 200μL. Twenty microliters are used in assays measuring enzyme activity remaining using para-nitrophenyl phosphate (pNPP) as a substrate. Controls includes enzyme, which is treated with inhibitor but not washed, and enzyme, which is not treated with BVT948 but is put through the incubation and washing procedures |
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Cell Assay |
L6 myocytes are maintained in minimum essential medium-alpha (α-MEM) supplemented with 10% fetal bovine serum and 100 IU/mL penicillin-streptomycin at 37°C in 5% CO2. Cells are seeded into 24-well plates, and the medium is replaced with α-MEM containing 2% fetal calf serum to induce differentiation into myotubes. The medium is changed every other day, and cytidine (0.24 mg/mL medium) is added to the cultures at days 7 to 9 to suspend cycling cells. The cells are used in experiments after overnight serum starvation at days 11 to 16. They are treated with or without 25μM BVT948 (BVT.948) for 30 min followed by 5 min of insulin (25 nM) stimulation. After freezing with liquid N2, the cells are lysed with a Tris-HCl buffer, pH 7.4, containing 1% Nonidet-40, 0.25% sodium deoxycholate, 150mM NaCl, 1mM EDTA, 1mM EGTA, 1mM sodium orthovanadate, 10mM β-glycerophosphate, 5mM sodium pyrophosphate, and complete protease inhibitor cocktail The cell extracts are centrifuged at 14,000 g for 10 min, and the supernatants are used in the Delfia assay |
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Animal Administration |
Male mice 12 to 14 weeks old are used in this study. They are divided into equal groups (n=9) based on blood glucose levels. At time 0, the mice are injected with vehicle (NaCl with 10% DMSO) or BVT948 (BVT.948) (0.3 and 3μMol/kg) and 1 U/kg insulin intraperitoneally. Blood glucose is determined from tail vein sampling at 0, 30, 60, and 120 min using a glucometer |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
