In humans, two forms of diacylglycerol lipase, DAGLα and DAGLβ, generate the endocannabinoid 2-arachidonoyl glycerol by attacking DAG at the sn-1 position. KT109 is a selective inhibitor of DAGLβ with an IC50 value of 42 nM. It demonstrates ~60-fold selectivity for DAGLβ over DAGLα, and negligible activity against other key enzymes involved in endocannabinoid signaling, including FAAH, MAGL, and ABHD11. KT109 has been shown to disrupt the lipid network involved in macrophage inflammatory responses, lowering 2-AG, as well as arachidonic acid and eicosanoids, in mouse peritoneal macrophages.
Citations
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Product Documents
Purity:>98.00%Appearance:A solid
Chemical Properties
CAS No.
1402612-55-8
SMILES
O=C(N1N=NC(C2=CC=C(C3=CC=CC=C3)C=C2)=C1)N4C(CC5=CC=CC=C5)CCCC4
Molecular Formula
C27H26N4O
Molecular Weight
422.5
Solubility
DMF: 10 mg/ml,DMSO: 10 mg/ml
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.
CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility
g/mol
Reviews
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