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DO34

Cat. No. M14690
DO34 Structure
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Biological Activity

DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC50 for DAGLβ.

Chemical Information
Molecular Weight 531.53
CAS Number 1848233-58-8
Solubility (25°C) DMSO ≥ 90 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Prabhuanand Selvaraj, et al. The Novel Monoacylglycerol Lipase Inhibitor MJN110 Suppresses Neuroinflammation, Normalizes Synaptic Composition and Improves Behavioral Performance in the Repetitive Traumatic Brain Injury Mouse Model

[2] William Fyke, et al. Pharmacological inhibition of the primary endocannabinoid producing enzyme, DGL-α, induces autism spectrum disorder-like and co-morbid phenotypes in adult C57BL/J mice

[3] Lesley D Schurman, et al. Diacylglycerol Lipase-Alpha Regulates Hippocampal-Dependent Learning and Memory Processes in Mice

[4] Victoria S Cavener, et al. Inhibition of Diacylglycerol Lipase Impairs Fear Extinction in Mice

[5] Jenny L Wilkerson, et al. Investigation of Diacylglycerol Lipase Alpha Inhibition in the Mouse Lipopolysaccharide Inflammatory Pain Model

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