FKGK 11
目录号 : GC43670A selective iPLA2 inhibitor
Cas No.:1071000-98-0
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Phospholipase A2 (PLA2) catalyzes the hydrolysis of fatty acids at the sn-2 position of glycerophospholipids, yielding a free fatty acid and a lysophospholipid as products. There are three broad classes of PLA2, secretory (sPLA2), calcium-dependent cytosolic (cPLA2), and calcium-independent cytosolic (iPLA2), that have different functions. FKGK 11 is a selective inhibitor of iPLA2 that demonstrates an XI(50) value of 0.0073, where XI(50) equals the mole fraction of FKGK 11 in the total substrate interface required to inhibit iPLA2 by 50%. In comparison, mole fractions as high as 0.091 do not inhibit cPLA2 activity and cause only slight inhibition of sPLA2.
Cas No. | 1071000-98-0 | SDF | |
Canonical SMILES | O=C(C(F)(F)C(F)(F)F)CCCCC1=CC=CC=C1 | ||
分子式 | C13H13F5O | 分子量 | 280.2 |
溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 30 mg/ml,PBS (pH 7.2): 2 mg/ml | 储存条件 | Store 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 | |||
1 mg | 5 mg | 10 mg | |
1 mM | 3.5689 mL | 17.8444 mL | 35.6888 mL |
5 mM | 0.7138 mL | 3.5689 mL | 7.1378 mL |
10 mM | 0.3569 mL | 1.7844 mL | 3.5689 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。
Group VIA phospholipase A2 is a target for vasopressin signaling in the thick ascending limb
Am J Physiol Renal Physiol 2012 Apr 1;302(7):F865-74.PMID:22218592DOI:10.1152/ajprenal.00222.2011
Na(+)-K(+)-2Cl(-) cotransporter (NKCC2)-mediated NaCl reabsorption in the thick ascending limb (TAL) is stimulated by AVP via V2 receptor/PKA/cAMP signaling. This process is antagonized by locally produced eicosanoids such as 20-HETE or prostaglandin E(2), which are synthesized in a phospholipase A(2)-dependent reaction cascade. Using microarray-based gene expression analysis, we found evidence for an AVP-dependent downregulation of the calcium-independent isoform of PLA(2), iPLA(2)β, in the outer medulla of rats. In the present study, we therefore examined the contribution of iPLA(2)β to NKCC2 regulation. Immunoreactive iPLA(2)β protein was detected in cultured mTAL cells as well as in the entire TAL of rodents and humans with the exception of the macula densa. Administration of the V2 receptor-selective agonist desmopressin (5 ng/h; 3 days) to AVP-deficient diabetes insipidus rats increased outer medullary phosphorylated NKCC2 (pNKCC2) levels more than twofold in association with a marked reduction in iPLA(2)β abundance (-65%; P < 0.05), thus confirming microarray results. Inhibition of iPLA(2)β in Sprague-Dawley rats with FKGK 11 (0.5 μM) or in mTAL cells with FKGK 11 (10 μM) or (S)-bromoenol lactone (5 μM) for 1 h markedly increased pNKCC2 levels without affecting total NKCC2 expression. Collectively, these data indicate that iPLA(2)β acts as an inhibitory modulator of NKCC2 activity and suggest that downregulation of iPLA(2)β may be a relevant step in AVP-mediated urine concentration.