3BDO
(Synonyms: 3BDO,MTOR激酶激活剂,自噬抑制剂) 目录号 : GC32767
A butyrolactone derivative and autophagy inhibitor
Cas No.:890405-51-3
Sample solution is provided at 25 µL, 10mM.
3BDO is a butyrolactone derivative and inhibitor of autophagy.1,2 It increases phosphorylation of the mammalian target of rapamycin (mTOR) substrates eIF4E-binding protein 1 (EIF4EBP1) and RPS6KB1/p70S6K1 in human umbilical vein endothelial cells (HUVECs) when used at a concentration of 60 μM.1 3BDO (60 μM) also prevents rapamycin-induced MAP1LC3B puncta formation, a marker of autophagy, in HUVECs. It inhibits apoptosis, senescence, and increases in integrin β4 levels induced by serum- and FGF2-deprivation in HUVECs when used at a concentration of 40 μg/ml.3 3BDO (80 mg/kg per day) reduces cortical and hippocampal amyloid plaque burden, inhibits autophagy in the brain, and rescues learning and memory deficits in the AβPP/PS1 transgenic mouse model of Alzheimer's disease.2
1.Ge, D., Han, L., Huang, S., et al.Identification of a novel MTOR activator and discovery of a competing endogenous RNA regulating autophagy in vascular endothelial cellsAutophagy10(6)957-971(2014) 2.Wei, L., Yang, H., Xie, Z., et al.A butyrolactone derivative 3BDO alleviates memory deficits and reduces amyloid-β deposition in an AβPP/PS1 transgenic mouse modelJ. Alzheimers Dis.30(3)531-543(2012) 3.Wang, W., Liu, X., Zhang, Y., et al.Both senescence and apoptosis induced by deprivation of growth factors were inhibited by a novel butyrolactone derivative through depressing integrin β4 in vascular endothelial cellsEndothelium14(6)325-332(2007)
Kinase experiment: |
Total protein is obtained from HUVECs by using of IP lysis buffer after treatment with rapamycin (10 μM), 3BDO (60 μM) or both for 6 h. After centrifuging at 4°C, the supernatant is collected and incubated with protein A/G agarose beads and TIA1 antibody or normal mouse IgG as a control at 4°C overnight. The beads are washed 3 times with IP lysis buffer and then eluted with 4×SDS loading buffer. Ser phosphorylation is detected by western blot assay with Ser phosphorylation antibody[1]. |
Cell experiment: |
HUVECs are isolated from umbilical cords and cultured in M199 medium with 20% (v/v) fetal bovine serum and 10 IU/mL fibroblast growth factor 2 (FGF2) in a humidified incubator at 37°C with 5% CO2. Cells up to passage 10 are used for experiments. When HUVECs are grown to 80% confluency, HUVECs are treated with DMSO or 60 µM 3BDO for 24 h, then total RNA is extracted[1]. |
Animal experiment: |
Male apoE-/- mice (8 weeks old) are used in this study. ApoE-/- mice are fed an atherogenic diet (containing 21% fat and 0.15% cholesterol). To avoid the potential confounding effects of variation among batches of diet, a single batch is reserved and used throughout the experiment. Mice at 20 weeks older are divided into 3 groups for treatment (n=8 mice/group) for 8 weeks: control (DMSO), low-dose 3BDO (50 mg/kg/d; 3BDO-L) and high-dose 3BDO (100 mg/kg/d; 3BDO-H). The body weight of mice is measured every week during 3BDO injection. Blood samples are taken from the inferior vena cava, and animals are killed by exsanguination[2]. |
References: [1]. Ge D, et al. Identification of a novel MTOR activator and discovery of a competing endogenous RNA regulating autophagy in vascular endothelial cells. Autophagy. 2014 Jun;10(6):957-71. |
Cas No. | 890405-51-3 | SDF | |
别名 | 3BDO,MTOR激酶激活剂,自噬抑制剂 | ||
Canonical SMILES | O=C1OC(COC2=C([N+]([O-])=O)C=CC=C2)CC1CC3=CC=CC=C3 | ||
分子式 | C18H17NO5 | 分子量 | 327.33 |
溶解度 | DMSO : ≥ 150 mg/mL (458.25 mM) | 储存条件 | Store at -20°C |
General tips | 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 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。 为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。 |
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Shipping Condition | 评估样品解决方案:配备蓝冰进行发货。所有其他可用尺寸:配备RT,或根据请求配备蓝冰。 |
制备储备液 | |||
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1 mg | 5 mg | 10 mg |
1 mM | 3.055 mL | 15.2751 mL | 30.5502 mL |
5 mM | 0.611 mL | 3.055 mL | 6.11 mL |
10 mM | 0.3055 mL | 1.5275 mL | 3.055 mL |
第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量) | ||||||||||
给药剂量 | mg/kg | 动物平均体重 | g | 每只动物给药体积 | ul | 动物数量 | 只 | |||
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方) | ||||||||||
% DMSO % % Tween 80 % saline | ||||||||||
计算重置 |
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,
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 saline,混匀澄清。
1. 首先保证母液是澄清的;
2.
一定要按照顺序依次将溶剂加入,进行下一步操作之前必须保证上一步操作得到的是澄清的溶液,可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
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- Purity: >96.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet