DO34
Names
[ CAS No. ]:
1848233-58-8
[ Name ]:
DO34
Biological Activity
[Description]:
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.
[Related Catalog]:
[Target]
IC50: 6 nM (DAGLα), 3-8 nM (DAGLβ)[1].
[In Vitro]
DO34 is a highly potent, selective and centrally active DAGL inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG, as determined using a real-time, fluorescence-based natural substrate assay with membrane lysates from HEK293T cells expressing recombinant human DAGLα. It is also confirmed that and DO34 is a potent inhibitor of DAGLβ with IC50 of 3-8 nM[1].
[In Vivo]
DO34 (compound 39) prevents fasting-induced refeeding of mice, which is typical cannabinoid CB1-receptor mediated behavior. DO34 (comound 39) reduces brain 2-AG levels in dose- and time dependent manner[2]. DO34 could block the tonic CB1 activation. AM251 significantly increases basal PF-EPSCs in MAGL-TKO mice, and the effect of AM251 is blocked by the DAGL inhibitor DO34[3].
[Animal admin]
Mice[2] 12-week-old male C57Bl/6J mice are single housed in metabolic cages with a regular 12:12h light/dark cycle (6 a.m.-6 p.m.) and free access to food and water unless noted otherwise. After 3 days of acclimatization, mice are fasted for 18h starting at midnight followed by an intraperitoneal injection with 38 (50 mg/kg), DO34 (compound 39: 50 mg/kg), 40 (50 mg/kg) or vehicle 30 min prior to refeeding[2].
[References]
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Chemical & Physical Properties
[ Molecular Formula ]:
C26H28F3N5O4
[ Molecular Weight ]:
531.53
[ Storage condition ]:
2-8℃