规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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1mg |
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2mg |
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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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靶点 |
CRISPR/Cas9; HSV-1
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体外研究 (In Vitro) |
用布雷菲德菌素 A (BFA) 处理 15 或 40 小时后,内质网 (ER) 显着肿胀并移动到正常肾 (NRK) 细胞的外周。长期 Brefeldin A 治疗会显着破坏肌动蛋白和 MT 细胞骨架 [1]。 Brefeldin A 和 ADPR 缀合物介导 BARS 的 ADP 核糖基化。当使用从用 BFA 处理的 CD38+ HeLa 细胞获得的细胞创建时,条形图显示了 BAC 结合 [3]。 Brefeldin A 减少 3D 和 2D 培养物中的 MDA-MB-231 集落形成,促进 MDA-MB-231 乳腺癌细胞中身份无关的细胞死亡,并阻断 MDA-MB 迁移和 MMP 9(基质金属肽酶 9)活性 - 231 [2]。
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细胞实验 |
Brefeldin A(BFA)是一种在真核细胞中诱导内质网(ER)应激的霉菌毒素。我们发现,与粘附培养相比,亚微克/毫升浓度的BFA在MDA-MB-231悬浮培养物(EC50:0.016µg/mL)中优先诱导细胞死亡。BFA还有效地抑制了MDA-MB-231细胞的克隆形成活性和迁移以及基质金属蛋白酶-9(MMP-9)活性。Western印迹分析表明,BFA的作用可能是通过下调乳腺CSC标志物CD44和抗凋亡蛋白Bcl-2和Mcl-1,以及逆转上皮间质转化来介导的。此外,BFA对悬浮的MDA-MB-468细胞也表现出选择性细胞毒性,并抑制了T47D和MDA-MB-453细胞中的瘤球形成,表明BFA可能对各种表型的乳腺癌症细胞有效[2]。
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动物实验 |
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参考文献 |
[1]. Alvarez C, et al. Brefeldin A (BFA) disrupts the organization of the microtubule and the actin cytoskeletons. Eur J Cell Biol. 1999 Jan;78(1):1-14.
[2]. Tseng CN, et al. Brefeldin A reduces anchorage-independent survival, cancer stem cell potential and migration of MDA-MB-231 human breast cancer cells. Molecules. 2014 Oct 29;19(11):17464-77. [3]. Wang J, et al. Erythroleukemia cells acquire an alternative mitophagy capability. Sci Rep. 2016 Apr 19;6:24641. [4]. Colanzi A, et al. Molecular mechanism and functional role of brefeldin A-mediated ADP-ribosylation of CtBP1/BARS. Proc Natl Acad Sci U S A. 2013 Jun 11;110(24):9794-9. [5]. Yu C, et al. Small molecules enhance CRISPR genome editing in pluripotent stem cells. Cell Stem Cell. 2015 Feb 5;16(2):142-7. [6]. Nozawa N, et al. Subcellular localization of herpes simplex virus type 1 UL51 protein and role of palmitoylation in Golgi apparatus targeting. J Virol. 2003 Mar;77(5):3204-16. [7]. Jensen HL, Rygaard J, Norrild B. A time-related study of Brefeldin A effects in HSV-1 infected cultured human fibroblasts. APMIS. 1995;103(7-8):530-539. doi:10.1111/j.1699-0463.1995.tb01402.x |
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其他信息 |
Brefeldin A is a metabolite from Penicillium brefeldianum that exhibits a wide range of antibiotic activity. It has a role as a Penicillium metabolite.
A metabolite from Penicillium brefeldianum that exhibits a wide range of antibiotic activity. brefeldin A is a natural product found in Penicillium camemberti, Penicillium brefeldianum, and other organisms with data available. A fungal metabolite which is a macrocyclic lactone exhibiting a wide range of antibiotic activity. Previous inquiries into the effects of Brefeldin A (BFA) have largely concentrated on dynamics of ER-Golgi membrane traffic, predominantly after relatively short treatments with the drug. We have now analyzed the effects of long BFA treatment on overall cell morphology, behavior of resident and cycling Golgi proteins, and microtubular and actin cytoskeletons organization. Prolonged (15 h or 40 h) treatment of normal rat kidney (NRK) cells with BFA caused dramatic swelling of the Endoplasmic Reticulum (ER) and shifted its localization to the periphery of the cells. The Golgi complex was disassembled and Golgi proteins redistributed and persisted in partially distinct compartments. Prolonged BFA treatment resulted in marked disruption of the MT and actin cytoskeleton. Peripheral MT were absent and tubulin staining was concentrated in short astral MT emanating from the microtubule organizing center (MTOC). Actin stress fibers were largely absent and actin staining was concentrated within a perinuclear area. Within this region, actin localization overlapped that of the membrane transport factor p115. BFA effects on Golgi structure and on MT and actin organization showed the same threshold -- all could be partially reversed after 30 min and 15 h BFA treatment but were irreversible after 40h incubation with the drug. The observed effects were not induced by signaling pathways involved in apoptotic phenomena or in ER stress response pathways. These results suggest that BFA inhibits the activity of key molecules that regulate MT and actin cytoskeleton dynamics. The findings can be used as the basis for elucidating the molecular mechanism of BFA action on the cytoskeleton.[1] |
分子式 |
C16H24O4
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分子量 |
280.36
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精确质量 |
280.167
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元素分析 |
C, 68.55; H, 8.63; O, 22.83
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CAS号 |
20350-15-6
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相关CAS号 |
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PubChem CID |
5287620
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外观&性状 |
Typically exists as White to off-white solids at room temperature
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密度 |
1.1±0.1 g/cm3
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沸点 |
492.7±45.0 °C at 760 mmHg
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熔点 |
200-205ºC
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闪点 |
180.8±22.2 °C
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蒸汽压 |
0.0±2.8 mmHg at 25°C
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折射率 |
1.513
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LogP |
1.61
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tPSA |
66.76
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SMILES |
O([H])[C@]1([H])C([H])([H])[C@]2([H])C([H])=C([H])C([H])([H])C([H])([H])C([H])([H])[C@@]([H])(C([H])([H])[H])OC(C([H])=C([H])C([H])([C@@]2([H])C1([H])[H])O[H])=O |c:10,t:31|
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InChi Key |
KQNZDYYTLMIZCT-KQPMLPITSA-N
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InChi Code |
InChI=1S/C16H24O4/c1-11-5-3-2-4-6-12-9-13(17)10-14(12)15(18)7-8-16(19)20-11/h4,6-8,11-15,17-18H,2-3,5,9-10H2,1H3/b6-4+,8-7+/t11-,12+,13-,14+,15+/m0/s1
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化学名 |
(1S,2E,7S,10E,12R,13R,15S)-12,15-Dihydroxy-7-methyl-8-oxabicyclo[11.3.0]hexadeca-2,10-dien-9-one
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别名 |
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HS Tariff Code |
2934.99.9001
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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 |
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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 (体外实验) |
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溶解度 (体外实验) |
配方 1 中的溶解度: ≥ 2.5 mg/mL (8.92 mM) (饱和度未知) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。
例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL澄清DMSO储备液加入到400 μL PEG300中,混匀;然后向上述溶液中加入50 μL Tween-80,混匀;加入450 μL生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 2 中的溶解度: ≥ 2.5 mg/mL (8.92 mM) (饱和度未知) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL澄清DMSO储备液加入900 μL 20% SBE-β-CD生理盐水溶液中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 View More
配方 3 中的溶解度: ≥ 2.5 mg/mL (8.92 mM) (饱和度未知) in 10% DMSO + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 配方 4 中的溶解度: ≥ 2.5 mg/mL (8.92 mM) (饱和度未知) in 10% EtOH + 40% PEG300 + 5% Tween80 + 45% Saline (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将100 μL 25.0 mg/mL 澄清 EtOH 储备液加入400 μL PEG300 中,混匀;再向上述溶液中加入50 μL Tween-80,混匀;然后加入450 μL 生理盐水定容至1 mL。 *生理盐水的制备:将 0.9 g 氯化钠溶解在 100 mL ddH₂O中,得到澄清溶液。 配方 5 中的溶解度: ≥ 2.5 mg/mL (8.92 mM) (饱和度未知) in 10% EtOH + 90% (20% SBE-β-CD in Saline) (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将100μL 25.0mg/mL澄清EtOH储备液加入到900μL 20%SBE-β-CD生理盐水中,混匀。 *20% SBE-β-CD 生理盐水溶液的制备(4°C,1 周):将 2 g SBE-β-CD 溶解于 10 mL 生理盐水中,得到澄清溶液。 配方 6 中的溶解度: ≥ 2.5 mg/mL (8.92 mM) (饱和度未知) in 10% EtOH + 90% Corn Oil (这些助溶剂从左到右依次添加,逐一添加), 澄清溶液。 例如,若需制备1 mL的工作液,可将 100 μL 25.0 mg/mL 澄清乙醇储备液加入到 900 μL 玉米油中并混合均匀。 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 | 3.5668 mL | 17.8342 mL | 35.6684 mL | |
5 mM | 0.7134 mL | 3.5668 mL | 7.1337 mL | |
10 mM | 0.3567 mL | 1.7834 mL | 3.5668 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) 。
NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
NCT05969353 | Recruiting | Other: accupunture | Assessing the Effectiveness of BFA as a Non-pharmacologic Pain Management Intervention: A Randomised Sham Controlled Study |
Bnai Zion Medical Center | July 23, 2023 | Not Applicable |
NCT04094246 | Recruiting | Procedure: Battlefield Acupuncture | Shoulder Injuries Pain,Postoperative |
Keller Army Community Hospital | September 25, 2019 | Not Applicable |
NCT06333938 | Not yet recruiting NEW |
Device: Bridge Device: BFA |
Anesthesia Surgery |
Durham VA Medical Center | June 2024 | Phase 4 |
NCT06128772 | Not yet recruiting | Other: Battlefield Acupuncture | Chronic Pain Substance Use Disorders |
Edith Nourse Rogers Memorial Veterans Hospital |
November 30, 2023 | Not Applicable |
th> |
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Inhibition of intracellular protein trafficking by Brefeldin A td> |
Brefeldin A inhibits STING-induced IRF activity in THP1-Dual™ cells td> |