规格 | 价格 | 库存 | 数量 |
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10 mM * 1 mL in DMSO |
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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 |
serine protease
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体外研究 (In Vitro) |
体外活性:AEBSF 通过直接抑制五种不同的人类细胞系(神经细胞系和非神经细胞系)中的 β-分泌酶来抑制 Aβ 的组成型产生。 AEBSF 作为丝氨酸蛋白酶抑制剂,抑制人巨噬细胞对白血病细胞的裂解,但不抑制巨噬细胞分泌 TNF-α 和 IL-1β。 AEBSF 还通过改变蛋白质分泌模式扰乱子宫内膜细胞上囊胚的生长并抑制 HeLa 细胞在 HUVEC 上的粘附。 细胞分析:发现 AEBSF 可以抑制多种细胞系中 Aβ 的产生。在用βAPP695 (K695sw)转染的K293细胞中,AEBSF表现出Aβ的剂量依赖性减少,IC50值约为1 mM。在野生型APP695转染的HS695和SKN695细胞中,AEBSF表现出抑制作用,IC50值约为300 μM。 AEBSF 还被发现可以增加 α-裂解并抑制 β-裂解。
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体内研究 (In Vivo) |
AEBSF(每日 ip 76.8 mg/kg)可延长感染致命弓形虫的小鼠的存活时间。 AEBSF 还可以减少蟑螂过敏原诱导的小鼠模型中的气道反应和潜在炎症。
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细胞实验 |
将悬浮于含 10% FCS 的 RPMI-1640 培养基中的 HeLa 细胞接种到 96 孔微孔板中,每孔分配 5×103 个细胞/200 μL。在 37°C 下孵育 24 小时后,用不同剂量的 AEBSF(0、25、50 和 100 μg/mL)处理细胞 48 小时。随后,每孔加入 20 μL 新鲜的 3-(4,5)-二甲基硫氮杂氮 (-z-y1)-3,5-二苯四唑啉 (MTT) 试剂 (5 μg/μL),并将细胞再培养 4小时,37°C,5% CO2。小心丢弃介质后,添加 150 μL DMSO。在酶标仪上,在两个不同波长下测量吸光度:540 和 620 nm。
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动物实验 |
Mice that receive a 2.5×103 parasite injection are randomly allocated to one of the following treatment groups: vehicle alone (control group), pyrimethamine alone at various doses, LY311727 alone at various doses, AEBSF alone at various doses, or AEBSF 76.8 mg/kg plus pyrimethamine 10 mg/kg. Each treatment group has ten animals in it. After the parasite inoculation, treatment is started 24 hours later and lasts for seven days in a row. In live mice, mouse survival is tracked every day for 15 days after infection. Every experiment is run three times, and the results displayed are the total of those runs.
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参考文献 |
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分子式 |
C8H11CLFNO2S
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分子量 |
239.69
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精确质量 |
239.02
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元素分析 |
C, 40.09; H, 4.63; Cl, 14.79; F, 7.93; N, 5.84; O, 13.35; S, 13.38
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CAS号 |
30827-99-7
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相关CAS号 |
34284-75-8;30827-99-7 (HCl);
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外观&性状 |
Solid powder
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SMILES |
C1=CC(=CC=C1CCN)S(=O)(=O)F.Cl
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InChi Key |
WRDABNWSWOHGMS-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C8H10FNO2S.ClH/c9-13(11,12)8-3-1-7(2-4-8)5-6-10;/h1-4H,5-6,10H2;1H
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化学名 |
4-(2-aminoethyl)benzenesulfonyl fluoride;hydrochloride
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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) |
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溶解度 (体内) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (8.68 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (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 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 (8.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (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 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (8.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 100 mg/mL (417.21 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Solubility in Formulation 5: 100 mg/mL (417.21 mM) in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. 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 | 4.1721 mL | 20.8603 mL | 41.7206 mL | |
5 mM | 0.8344 mL | 4.1721 mL | 8.3441 mL | |
10 mM | 0.4172 mL | 2.0860 mL | 4.1721 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) 。
AEBSF Stabilizes Full-Length βAPP. Neuron . 1996 Jul;17(1):171-9. td> |
AEBSF Increases α-Secretion. Neuron . 1996 Jul;17(1):171-9. td> |
AEBSF Increases Aβ Production in the Cell Lines F690P and D597Δ. Neuron . 1996 Jul;17(1):171-9. td> |
Radiosequencing of Aβ Proteins Secreted by the Cell Lines F690P and D597Δ with and without AEBSF Treatment. Neuron . 1996 Jul;17(1):171-9. td> |