AACOCF3
(Synonyms: 花生四烯基三氟甲酮,ATK, AATFMK) 目录号 : GC16115An inhibitor of cPLA2 and iPLA2
Cas No.:149301-79-1
Sample solution is provided at 25 µL, 10mM.
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Related Biological Data
Inhibition of cPLA2 activity weakens the ability of MF to promote wound healing and cell migration. (A) Representative images (Left) and quantitation (Right) of colonic epithelial cells wound closure at baseline and after 24 h of MF and three subtypes of PLA2 inhibitor intervention.
AACOCF3 (Glpbio) (10 μM), VPLB (3 μM) and BEL (0.3 μM) were added to colonic epithelial cells for scratch wound and migration experiments.
Phytomedicine 119 (2023): 154985. PMID: 37516090 IF: 7.8996 -
Related Biological Data
Production of infectious SGIV progeny in cell culture was inhibited by the cPLA2 inhibitor AACOCF3 or iPLA2 inhibitor PACOCF3. (B) The severity of CPE induced by SGIV infection at 24 h p.i. in AACOCF3-treated or PACOCF3-treated cells.
AACOCF3 was purchased from Good Laboratory Practice bioscience (GLPBIO) and was dissolved in ethanol.
Int J Mol Sci 22.22 (2021): 12597. PMID: 34830477 IF: 5.922 -
Related Biological Data
PLA2G4A inhibition enhances NK cell-mediated cytotoxicity against AML cells. (M–O) Realtime PCR results show the expression of NKG2DL genes in leukemia cell lines treated with the PLA2G4A inhibitor AACOCF3.
After treatment with AACOCF3 (GC16115, GLPBIO) at 25mM for 48 hours, we evaluated cellular apoptosis with Annexin-V by flow cytometric analysis.
Frontiers in oncology 12 (2022). PMID: 36338749 IF: 5.7382
Quality Control & SDS
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- Purity: >98.00%
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- Datasheet
AACOCF3 is a potent and selective inhibitor of cytosolic phospholipase A2 with IC50 value of 15 μM [1].
Phospholipase A2 is an enzyme that releases fatty acids from glycerol. Cytosolic phospholipase A2 (cPLA2) plays an important role in inflammation by inducing the release of arachidonic acid from membrane phospholipids.
AACOCF3 is a potent and selective inhibitor of the 85-kDa cPLA2. AACOCF3 inhibited macrophage PLA2 with IC50 value of 15 μM in a concentration-dependent way [1]. AACOCF3 inhibited the release of arachidonic acid (AA) with IC50 values of 2 and 8 μM in platelets and calcium ionophore-challenged U 937 cells, respectively. Also, AACOCF3 inhibited the production of thromboxane B and 12-hydroxyeicosatetraenoic acid (12-HETE), the major metabolites of AA in a dose-dependent way. These results suggested that cPLA2 played a critical role in the generation of AA and 12-HETE [2].
In mice, AACOCF3 inhibited chronic inflammatory responses and inhibited phorbol 12-myristate
13-acetate (PMA)-induced chronic ear edema. In ovalbumin-challenged BALB/c mice, AACOCF3 (20mg/kg) inhibited airway hyper-responsiveness and reduced cellular recruitment in the airway inflammation and airway lumen [3].
AACOCF3是一种针对细胞质磷脂酶A2的高效选择性抑制剂，其IC50值为15 μM [1]。
磷脂酶A2是一种从甘油中释放脂肪酸的酶。细胞质磷脂酶A2 (cPLA2)通过诱导磷脂质膜中的花生四烯酸释放，发挥着在炎症中的重要作用。
AACOCF3是一种对85-kDa cPLA2的高效选择性抑制剂。AACOCF3浓度依赖性地抑制巨噬细胞PLA2，其IC50值为15 μM [1]。AACOCF3可抑制血小板中花生四烯酸的释放，在血小板和钙离子拮抗剂挑战的U 937细胞中，其IC50值分别为2和8 μM。此外，AACOCF3可剂量依赖地抑制血栓素B和12-羟基二十碳四烯酸(12-HETE)的产生，这些是花生四烯酸的主要代谢产物。这些结果表明，cPLA2在花生四烯酸和12-HETE的生成中发挥了关键作用[2]。
在小鼠中，AACOCF3可抑制慢性炎症反应，并抑制了PMA诱导的慢性耳部水肿。在卵清蛋白-挑战的BALB/c小鼠中，AACOCF3 (20mg/kg)抑制了气道过度反应，并减少了气道炎症和气道腔内细胞的招募[3]。
References:
[1]. Ackermann EJ, Conde-Frieboes K, Dennis EA. Inhibition of macrophage Ca(2+)-independent phospholipase A2 by bromoenol lactone and trifluoromethyl ketones. J Biol Chem, 1995, 270(1): 445-450.
[2]. Riendeau D, Guay J, Weech PK, et al. Arachidonyl trifluoromethyl ketone, a potent inhibitor of 85-kDa phospholipase A2, blocks production of arachidonate and 12-hydroxyeicosatetraenoic acid by calcium ionophore-challenged platelets. J Biol Chem, 1994, 269(22): 15619-15624.
[3]. Malaviya R, Ansell J, Hall L, et al. Targeting cytosolic phospholipase A2 by arachidonyl trifluoromethyl ketone prevents chronic inflammation in mice. Eur J Pharmacol, 2006, 539(3): 195-204.
| Cas No. | 149301-79-1 | SDF | |
| 别名 | 花生四烯基三氟甲酮,ATK, AATFMK | ||
| 化学名 | 1,1,1-trifluoro-6Z,9Z,12Z,15Z-heneicosatetraen-2-one | ||
| Canonical SMILES | FC(F)(C(CCC/C=C\C/C=C\C/C=C\C/C=C\CCCCC)=O)F | ||
| 分子式 | C21H31F3O | 分子量 | 356.47 |
| 溶解度 | DMF: >25 mg/ml,DMSO: > 25 mg/ml,PBS pH 7.2: <50 µ g/ml | 储存条件 | Store at -20°C, protect from 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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8053 mL | 14.0264 mL | 28.0529 mL |
| 5 mM | 0.5611 mL | 2.8053 mL | 5.6106 mL |
| 10 mM | 0.2805 mL | 1.4026 mL | 2.8053 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。
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