Name: KT109
Rating: 5 (10 reviews)

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HIT ID:HIT212000176
Cas No:1402612-55-8
常用名:KT109
别名:KT-109, KT 109
IUPAC:2-benzyl-1-(4-{[1,1'-biphenyl]-4-yl}-1H-1,2,3-triazole-1-carbonyl)piperidine
IUPAC:2-benzyl-1-(4-{[1,1'-biphenyl]-4-yl}-1H-1,2,3-triazole-1-carbonyl)piperidine
InChI key:JKJMWHULJIOKPJ-UHFFFAOYSA-N

分子式:C27H26N4O
分子量:422.532
氢键供体数 (HBD):0
氢键受体数 (HBA):3
LogP:5.933738
SMILES:O=C(N1CCCCC1Cc1ccccc1)n1cc(nn1)-c1ccc(cc1)-c1ccccc1
SMILES:O=C(N1CCCCC1Cc1ccccc1)n1cc(nn1)-c1ccc(cc1)-c1ccccc1

KT109 is a selective inhibitor of DAGLβ (IC50 = 42 nM). KT109-treated wild-type mice displayed reductions in LPS-induced allodyni as well as in DAGL-β (-/-) micea. Repeated KT109 administration prevented the expression of LPS-induced allodynia, without evidence of tolerance. Intraplantar injection of KT109 into the LPS-treated paw, but not the contralateral paw, reversed the allodynic responses. KT109 also reversed allodynia in the CCI and CINP models and lacked discernible side effects (e.g. anxiogenic behaviour, gross motor deficits or gastric ulcers).

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