PACOCF3
(Synonyms: 1,1,1-三氟-2-十七烷酮,Palmityltrifluoromet?hylketone) 目录号 : GC16714Antagonizes DP receptor agonist effects
Cas No.:141022-99-3
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
PACOCF3 is a inhibitor of both Ca2+-dependent cytosolic cPLA2 and Ca2+-independent phospholipases A2 iPLA2 with IC50 values of 45 µM and 3.8 µM [1,2], which is an innovate and potential candidate drug for inflammation, atherosclerosis, diabetes mellitus, therapeutic shock, cancer therapyetc [3,4,5,6]. It has been reported that PACOCF3 can inhibit PLA2 and reduce the inflammatory response. PACOCF3 also can stimulate insulin release at basal glucose levels (2 mmol/l). Application of PACOCF3 can inhibit endogenous arachidonic acid generation which significantly decreased the amplitude of the insulin secretory response to 20 mmol/l glucose [7,8]. PACOCF3 have a dual protective role in diabetes which could minimize β-cell dysfunction while maintaining insulin secretory output through enhancing endogenous arachidonic acid levels.
References:
1. Murakami M et al.Emerging roles of secreted phospholipase A2 enzymes: The 3rd edition.Biochimie. 2014 Sep 16. pii: S0300-9084(14)00252-1.
2. Quach ND et al. Secretory phospholipase A2 enzymes as pharmacological targets for treatment of disease. Biochem Pharmacol. 2014 Aug 15;90(4):338-48.
3. Chalimoniuk M. Secretory phospholipase A2 and its role in oxidative stress and inflammation]. Postepy Biochem. 2012;58(2):204-8.
4. Persaud SJ.et al. The role of arachidonic acid and its metabolites in insulin secretion from human islets of langerhans. Diabetes. 2007 Jan;56(1):197-203.
5. Khakpour H et al. Lipoprotein-associated phospholipase A2: an independent predictor of cardiovascular risk and a novel target for immunomodulation therapy. Cardiol Rev. 2009 Sep-Oct;17(5):222-9.
6. Narendra Sharath Chandra JN1 et al. Chemistry and structural evaluation of different phospholipase A2 inhibitors in arachidonic acid pathway mediated inflammation and snake venom toxicity. Curr Top Med Chem. 2007;7(8):787-800.
7. Packard CJ. Lipoprotein-associated phospholipase A2 as a biomarker of coronary heart disease and a therapeutic target. Curr Opin Cardiol. 2009 Jul;24(4):358-63.
8. Lucas R et al. Synthesis and enzyme inhibitory activities of a series of lipidic diamine and aminoalcohol derivatives on cytosolic and secretory phospholipases A2. Bioorg Med Chem Lett. 2000 Feb 7;10(3):285-8.
| Cas No. | 141022-99-3 | SDF | |
| 别名 | 1,1,1-三氟-2-十七烷酮,Palmityltrifluoromet?hylketone | ||
| 化学名 | 1,1,1-trifluoroheptadecan-2-one | ||
| Canonical SMILES | FC(F)(C(CCCCCCCCCCCCCCC)=O)F | ||
| 分子式 | C17H31F3O | 分子量 | 308.43 |
| 溶解度 | basic PBS: freely soluble,DMF: >50 mg/ml,DMSO: >30 mg/ml,Ethanol: >50 mg/ml,PBS pH 7.2: <50 µ g/ml (from ATK) | 储存条件 | Desiccate at -20°C |
| 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 | 3.2422 mL | 16.2111 mL | 32.4223 mL |
| 5 mM | 0.6484 mL | 3.2422 mL | 6.4845 mL |
| 10 mM | 0.3242 mL | 1.6211 mL | 3.2422 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。