AACOCF3 (Synonyms: ATK, AATFMK) |
カタログ番号GC16115
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AACOCF3（アラキドニルトリフルオロメチルケトン）は、細胞質ホスホリパーゼA2 (cPLA2)の有力な阻害剤で、IC50値は約10μMである。酵素の活性部位を不可逆的にアルキル化し、AACOCF3はアラキドン酸の遊離と炎症促進のエイコサノイドの後続の生産の放出を遮断する。AACOCF3は、炎症経路、神経炎症と脂質シグナル機能の研究では広く使われている。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 149301-79-1
Sample solution is provided at 25 µL, 10mM.
AACOCF3（アラキドニルトリフルオロメチルケトン）は、細胞質ホスホリパーゼA2 (cPLA2)の有力な阻害剤で、IC50値は約10μMである。酵素の活性部位を不可逆的にアルキル化し、AACOCF3はアラキドン酸の遊離と炎症促進のエイコサノイドの後続の生産の放出を遮断する。AACOCF3は、炎症経路、神経炎症と脂質シグナル機能の研究では広く使われている[1]。cPLA2が骨格筋におけるカルパインの活性にも関与しているため、AACOCF3はミトコンドリア機能の制御にも有力である[2]。最近、cPLA2は様々な癌の進行に緊密に関連していて、AACOCF3は、闘癌の潜在的な薬物だと考えられている[3, 4]。
試験管内実験では、AACOCF3 (5μM)は、MARKシグナル経路を通じて、上皮性成長因子（EGF）でプロスタグランジン(PGs)の活性化を遮断でき、よって角膜上皮細胞における有糸分裂を阻害する[5]。AACOCF3 (1.3–10μM)は、リポ多糖類(LPS)に誘発されたcPLA2の活性化を阻害し、小膠細胞における活性酸素種(ROS)と一酸化窒素の生産を減らし、初代小膠細胞の活性に関連する形態変化を阻止する[6]。
生体内実験では、損傷の30分前に、AACOCF3(4mM、50μL)を静脈内注射し、その後、AACOCF3 (4 mM, 200 μL)を毎日腹腔内注射する処理レジメンの結果、脊髄損傷(SCI)マウスの障害部位を著しく減らし、後肢運動機能の指標を改善し、バランスと協調能力をも向上させた[7]。脊髄損傷のラットモデルでは、AACOCF3(7.13mg/kg)の静脈内注射は、ラットモデルにおける生存神経細胞とオリゴデンドロサイトの数を著しく増やし、ラットに神経保護作用を発揮する[8]。
References:
[1] 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 Jun 3;269(22):15619-24.
[2] Supinski GS, Alimov AP, Wang L, et al. Calcium-dependent phospholipase A2 modulates infection-induced diaphragm dysfunction. Am J Physiol Lung Cell Mol Physiol. 2016 May 15;310(10):L975-84.
[3] Pan P, Qin G, Wang B, et al. HDAC5 Loss Enhances Phospholipid-Derived Arachidonic Acid Generation and Confers Sensitivity to cPLA2 Inhibition in Pancreatic Cancer. Cancer Res. 2022 Dec 16;82(24):4542-4554.
[4] Li J, Zhang M, Sun Q, et al. CENPF interaction with PLA2G4A promotes glioma growth by modulating mTORC1 and NF-κB pathways. Cancer Cell Int. 2025 Mar 1;25(1):73.
[5] Kang SS, Li T, Xu D, et al. Inhibitory effect of PGE2 on EGF-induced MAP kinase activity and rabbit corneal epithelial proliferation. Invest Ophthalmol Vis Sci. 2000 Jul;41(8):2164-9.
[6] Chuang DY, Simonyi A, Kotzbauer PT, et al. Cytosolic phospholipase A2 plays a crucial role in ROS/NO signaling during microglial activation through the lipoxygenase pathway. J Neuroinflammation. 2015 Oct 31;12:199.
[7] Liu NK, Deng LX, Zhang YP, et al. Cytosolic phospholipase A2 protein as a novel therapeutic target for spinal cord injury. Ann Neurol. 2014 May;75(5):644-58.
[8] Huang W、Bhavsar A、Ward RE, et al. Arachidonyl trifluoromethyl ketone is neuroprotective after spinal cord injury. J Neurotrauma. 2009 Aug;26(8):1429-34.
| 細胞実験[1]: | |
細胞株 | BV-2細胞 |
準備方法 | フェノールレッドなしのDMEMで、BV-2細胞を3時間血清飢餓させ、特定の濃度でAACOCF3と1時間培養した。その後、細胞をIFNγまたはLPSで37℃で16時間培養した。 |
反応条件 | 1.3μM, 2.5μM, 5μM, 10μM, 1時間 |
アプリケーション | AACOCF3は、BV-2細胞で、ROSと一酸化窒素の生産を減らす。 |
| 動物実験 [2]: | |
動物モデル | 脊髄損傷(SCI) C57BL/6マウス |
準備方法 | 損傷の30分後、AACOCF3を脊髄損傷(SCI)のマウスに静脈内投与し、その後は2週間、2日ごとに腹腔内注射した。 |
投与形態 | 4mM、損傷の30分後に50μlを静脈内注射し、その後は200μlを2週間2日ごとに腹腔内注射 |
アプリケーション | AACOCF3は、SCIマウスの障害部位を著しく減らし、後肢の運動機能を改善し、バランスと協調能力をも向上させた。 |
References: | |
| Cas No. | 149301-79-1 | SDF | |
| 同義語 | ATK, AATFMK | ||
| Chemical Name | 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 | ||
| Formula | C21H31F3O | M.Wt | 356.47 |
| 溶解度 | DMF: >25 mg/ml,DMSO: > 25 mg/ml,PBS pH 7.2: <50 µ g/ml | Storage | Store at -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8053 mL | 14.0264 mL | 28.0529 mL |
| 5 mM | 561.1 μL | 2.8053 mL | 5.6106 mL |
| 10 mM | 280.5 μL | 1.4026 mL | 2.8053 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.00% Appearance: A liquid
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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
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