产品
编 号：F144730
分子式：C24H21F6NO7
分子量：549.42
分子式：C24H21F6NO7
分子量：549.42
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
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10mg
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50mg
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100mg
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结构图
CAS No: 1380424-42-9
产品详情
生物活性：
KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.
体内研究：
KML29 enhibits antinociceptive activity without cannabimimetic side effects.KML29 (20 mg/kg) has a significant but modest protective effectagainst LPS-induced fever.Animal Model:C57Bl/6 mice.
Dosage:1-40 mg/kg.
Administration:P.O. single dose.
Result:Selectively inhibited MAGL in mice.
Animal Model:Wistar albino male rats.
Dosage:20 mg/kg (+LPS E. coli O111:B4 (250 μg/kg, sc)).
Administration:SC.
Result:Administration of KML29 simultaneously with LPS E. coli O111:B4 significantly decreased ?T (with 5% type 1 error, 1.7 fold) compared to saline+LPS E. coli O111:B4. Administration of KML29 simultaneously with LPS E. coli O111:B4 resulted in decreased plateau phase of fever compared to LPS E. E. coli O111:B4+saline administration.
体外研究：
KML29 dose-dependently elevates brain 2-AG level up to10-fold without alteration in brain levels of anandamide, palmitoylethanolamide, and oleoylethanolamide.KML29 is a potent inhibitor of 2-AG hydrolysis, but did not affect AEA hydrolysis at any concentration tested.
KML29 is an extremely selective, orally active and irreversible MAGL inhibitor, with IC50 values of 15 nM, 43 nM and 5.9 nM for mouse, rat and human MAGL, respectively. KML29 exhibits minimal cross-reactivity toward other central and peripheral serine hydrolases, including no detectable activity against FAAH.
体内研究：
KML29 enhibits antinociceptive activity without cannabimimetic side effects.KML29 (20 mg/kg) has a significant but modest protective effectagainst LPS-induced fever.Animal Model:C57Bl/6 mice.
Dosage:1-40 mg/kg.
Administration:P.O. single dose.
Result:Selectively inhibited MAGL in mice.
Animal Model:Wistar albino male rats.
Dosage:20 mg/kg (+LPS E. coli O111:B4 (250 μg/kg, sc)).
Administration:SC.
Result:Administration of KML29 simultaneously with LPS E. coli O111:B4 significantly decreased ?T (with 5% type 1 error, 1.7 fold) compared to saline+LPS E. coli O111:B4. Administration of KML29 simultaneously with LPS E. coli O111:B4 resulted in decreased plateau phase of fever compared to LPS E. E. coli O111:B4+saline administration.
体外研究：
KML29 dose-dependently elevates brain 2-AG level up to10-fold without alteration in brain levels of anandamide, palmitoylethanolamide, and oleoylethanolamide.KML29 is a potent inhibitor of 2-AG hydrolysis, but did not affect AEA hydrolysis at any concentration tested.
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