An inhibitor of ABHD6 (IC50 = 0.21 nM in Neuro2A cells); inhibits ABHD6 in a 2-AG hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells); selective for ABHD6 over DAGLβ at 1 µM but inhibits LYPLA1 and LYPLA2 at 10 µM; inhibits ABHD6 activity in mouse liver and brain in vivo at 5-10 and ~40 mg/kg

KT185 – 5 mg

Brand:
Cayman
CAS:
1472640-86-0
Storage:
-20
UN-No:
Non-Hazardous - /

KT185 is an orally bioavailable inhibitor of α/β-hydrolase domain-containing protein 6 (ABHD6) with an IC50 value of 0.21 nM in a competitive activity-based protein profiling assay using Neuro2A membranes.{24855} It inhibits ABHD6 in a 2-arachidonoyl glycerol (2-AG; Item No. 62160) 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. It inhibits ABHD6 activity in mouse liver and brain in vivo when administered at doses of 5-10 and approximately 40 mg/kg, respectively, without inhibiting fatty acid amide hydrolase (FAAH) in the brain. KT185 inhibits increases in the frequency of spontaneous inhibitory post-synaptic currents (sIPSCs) induced by nicotine (Item No. 29138) in the rat ventral tegmental area (VTA) but does not reduce nicotine self-administration in rats when administered intracerebroventricularly at a dose of 200 µg.{51209} It has been used as a negative control for the off-target effect of the DAGL inhibitor KT172 (Item No. 19112) on ABHD6.  

 

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Description

An inhibitor of ABHD6 (IC50 = 0.21 nM in Neuro2A cells); inhibits ABHD6 in a 2-AG hydrolysis assay (IC50 = 13.6 nM for the mouse recombinant enzyme expressed in HEK293T cells); selective for ABHD6 over DAGLβ at 1 µM but inhibits LYPLA1 and LYPLA2 at 10 µM; inhibits ABHD6 activity in mouse liver and brain in vivo at 5-10 and ~40 mg/kg, respectively; inhibits nicotine-induced increases in sIPSC frequency in the rat VTA but does not reduce nicotine self-administration in rats at 200 µg; has been used as a negative control for the off-target effect of KT172 on ABHD6

Formal name: [4′-[1-[(2-phenyl-1-piperidinyl)carbonyl]-1H-1,2,3-triazol-4-yl][1,1′-biphenyl]-3-yl]-1-piperidinyl-methanone

Synonyms: 

Molecular weight: 519.6

CAS: 1472640-86-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Small Molecule Inhibitors|Glycerolipid Lipases||Research Area|Lipid Biochemistry|Glycerolipids|Lipases||Research Area|Neuroscience|Behavioral Neuroscience|Addiction Research||Research Area|Neuroscience|Cannabinoid Research|Endocannabinoids

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