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FKGK 11

目录号 : GC43670

A selective iPLA2 inhibitor

FKGK 11 Chemical Structure

Cas No.:1071000-98-0

规格 价格 库存 购买数量
500μg
¥616.00
现货
1mg
¥1,165.00
现货
5mg
¥4,935.00
现货
10mg
¥8,633.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

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
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溶解性数据

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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
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Research Update

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.