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首页-小分子抑制剂&激动剂-Metabolic Enzyme/Protease-Phospholipase-KT185
KT185

Chemical Structure : KT185

CAS No.: 1472640-86-0

KT185 (KT-185)

货号: PC-20131Not For Human Use, Lab Use Only.

KT185 (KT-185) is a potent, selective, irreversible and orally-active α/β-hydrolase domain 6 (ABHD6) inhibitor with IC50 of 0.21 nM.

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5 mg ¥1480 In stock
10 mg ¥2180 In stock
25 mg ¥3780 In stock
50 mg ¥5880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

KT185 (KT-185) is a potent, selective, irreversible and orally-active α/β-hydrolase domain 6 (ABHD6) inhibitor with IC50 of 0.21 nM.
KT185 inhibits ABHD6 in a 2-arachidonoyl glycerol (2-AG) hydrolysis assay (IC50=13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells).
KT185 is selective for ABHD6 over diacylglycerol lipase β (DAGLβ) at 1 µM, but inhibits lysophospholipase 1 (LYPLA1) and LYPLA2 at 10 µM.
KT185 (5-10 mg/kg) inhibits ABHD6 activity in mouse liver and brain in vivo.
KT185 inhibits increases in the frequency of spontaneous inhibitory post-synaptic currents (sIPSCs) induced by nicotine in the rat ventral tegmental area (VTA) but does not reduce nicotine self-administration in rats.

物理化学性质&存储条件

分子量 519.65
分子式 C32H33N5O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

[4'-[1-[(2-Phenyl-1-piperidinyl)carbonyl]-1H-1,2,3-triazol-4-yl][1,1'-biphenyl]-3-yl]-1-piperidinylmethanone

参考文献

1. Ku-Lung Hsu, et al. J Med Chem. 2013 Nov 14;56(21):8270-9.

2. Matthew W Buczynski, et al. Proc Natl Acad Sci U S A. 2016 Jan 26;113(4):1086-91.

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