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DO34 

Cat. No.: HY-117771
Handling Instructions

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.

For research use only. We do not sell to patients.

DO34 Chemical Structure

DO34 Chemical Structure

CAS No. : 1848233-58-8

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  • Biological Activity

  • Protocol

  • Technical Information

  • References

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.

IC50 & 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].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8814 mL 9.4068 mL 18.8136 mL
5 mM 0.3763 mL 1.8814 mL 3.7627 mL
10 mM 0.1881 mL 0.9407 mL 1.8814 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Animal Administration
[2]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

531.53

Formula

C₂₆H₂₈F₃N₅O₄

CAS No.

1848233-58-8

SMILES

O=C(N1CC(CC2=CC=CC=C2)N(C(N3N=NC(C4=CC=C(OC(F)(F)F)C=C4)=C3)=O)CC1)OC(C)(C)C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
DO34
Cat. No.:
HY-117771
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DO34

Cat. No.: HY-117771