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  3. HIT212000206
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HIT212000206
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HIT212000206
  • HIT ID:HIT212000206
  • Cas No:1071001-09-6
  • 常用名:FKGK 18
  • IUPAC:1,1,1-trifluoro-6-(naphthalen-2-yl)hexan-2-one
    IUPAC:1,1,1-trifluoro-6-(naphthalen-2-yl)hexan-2-one
  • InChI key:VCWWTQMRNJSJGC-UHFFFAOYSA-N
  • 分子式:C16H15F3O
  • 分子量:280.29
  • 氢键供体数 (HBD):0
  • 氢键受体数 (HBA):1
  • LogP:5.396131
  • SMILES:FC(F)(F)C(=O)CCCCc1ccc2ccccc2c1
    SMILES:FC(F)(F)C(=O)CCCCc1ccc2ccccc2c1
  • FKGK 18 is an inhibitor of group VIA (GVIA) calcium-independent phospholipase A2 (iPLA2). It inhibits GVIA iPLA2 by 99.9% at 0.091 mole fraction in a mixed micelle activity assay and is selective for GVIA iPLA2 over GIVA cPLA2 and GV sPLA2 where it shows 80.8 and 36.8% inhibition, respectively. FKGK 18 inhibits iPLA2β activity in cytosolic extracts from INS-1 cells overexpressing iPLA2β (IC50 = ~50 nM) as well as iPLA2γ activity in mouse heart membrane fractions (IC50s = ~1-3 μM). It inhibits glucose-induced increases in prostaglandin E2 production and insulin secretion in human pancreatic islets when used at a concentration of 10 μM and inhibits thapsigargin-induced apoptosis in INS-1 cells overexpressing iPLA2β in a concentration-dependent manner. FKGK 18 (20 mg/kg, 3 times per week) reduces blood glucose levels in an intraperitoneal glucose tolerance test, decreases the incidence of diabetes, and increases serum insulin levels in non-obese diabetic (NOD) mice.
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    TargetMolSC
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    ¥ 2,970.00
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  • 供应商
    BIONET-Key OrganicsBB
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    4-6周
    纯度
    -
    待询
    1

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