EA4
目录号 : GC18141
An inhibitor of PLA2 from red blood cells
Cas No.:389614-94-2
Sample solution is provided at 25 µL, 10mM.
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Ki: 130 μM
EA4 is a rPLA2 inhibitor.
rPLA2, a calcium-dependent cytosolic phospholipase A2 (cPLA2), was initially isolated and characterized from bovine and human red blood cells. With a molecular mass of 42 kDa, cPLA2 shows biochemical properties similar to cPLA2 Type IV.
In vitro: It was found that EA4 was able to inhibit a Ca(2+) ionophore-induced arachidonic acid release from both human and bovine red blood cells, demonstrating that this enzyme was responsible for the Ca(2+)-dependent arachidonic acid release from mammalian red blood cells [1]. Another study found that in mouse hepatoma Hepa-1c1c7 cells, EA4 could cause a significant induction of the CYP1A1-mediated ethoxyresorufin O-deethylase activity time- and concentration-dependently, and such induction was accompanied by an increase of the Cyp1a1 mRNA transcription. Morevoer, in human cells including MCF-7 (human breast adenocarcinoma cell line), HepG2 (human hepatocarcinoma), and HL-60 (human promyelocytic cell line), the expression of CYP1A1 mRNA could be also induced by EA4 treatment. In addition, CYP1B1 mRNA was increased by EA4 in MCF-7 cells [2].
In vivo: Up to now, there is no animal in vivo data reported.
Clinical trial: So far, no clinical study has been conducted.
References:
1. Shin, H.S.,Chin, M.R.,Kim, J.S., et al. Purification and characterization of a cytosolic, 42-kDa and Ca2+-dependent phospholipase A2 from bovine red blood cells. The Journal of Biological Chemisty 277, 21086-21094 (2002).
2. Chun, Y.J.,Lee, B.Y.,Yang, S.A., et al. Induction of cytochrome P450 1A1 gene expression by a vitamin K3 analog in mouse hepatoma Hepa-1c1c7 cells. Molecules and Cells 12, 190-196 (2001).
| Cas No. | 389614-94-2 | SDF | |
| 化学名 | 7-chloro-6-[4-(diethylamino)phenyl]-5,8-quinolinedione | ||
| Canonical SMILES | CCN(CC)c1ccc(cc1)C1=C(Cl)C(=O)c2ncccc2C1=O | ||
| 分子式 | C19H17ClN2O2 | 分子量 | 340.8 |
| 溶解度 | ≤1mg/ml in DMSO;20mg/ml in dimethyl formamide | 储存条件 | Store at -20°C, sealed storage, away from moisture and light |
| 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 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.9343 mL | 14.6714 mL | 29.3427 mL |
| 5 mM | 0.5869 mL | 2.9343 mL | 5.8685 mL |
| 10 mM | 0.2934 mL | 1.4671 mL | 2.9343 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
- View current batch:
- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet