[CAS NO. 1848233-58-8] DO34
PRODUCTS SPECIFICATIONS [1848233-58-8]
DESCRIPTION [1848233-58-8]
Overview
| MDL | - |
|---|---|
| Molecular Weight | 531.53 |
| Molecular Formula | C26H28F3N5O4 |
| 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 |
2 Publications Citing Use of MCE
Summary
DO34 is a highly potent, selective and centrally active diacylglycerol lipase (DAGL) inhibitor, with an IC 50 of 6 nM for DAGLα conversion of SAG to 2-AG, and an IC 50 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 IC 50 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 IC 50 of 3-8 nM [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
DO34 (compound 39) prevents fasting-induced refeeding of mice, which is typical cannabinoid CB 1 -receptor mediated behavior. DO34 (comound 39) reduces brain 2-AG levels in dose- and time dependent manner [2] . DO34 could block the tonic CB 1 activation. AM251 significantly increases basal PF-EPSCs in MAGL-TKO mice, and the effect of AM251 is blocked by the DAGL inhibitor DO34 [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 100 mg/mL ( 188.14 mM )
* "≥" means soluble, but saturation unknown.
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 |
References
- [1] Ogasawara D, et al. Rapid and profound rewiring of brain lipid signaling networks by acute diacylglycerol lipase inhibition. Proc Natl Acad Sci U S A. 2016 Jan 5;113(1):26-33.
- [2] Deng H, et al. Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding. J Med Chem. 2017 Jan 12;60(1):428-440.
- [3] Liu X, et al. Coordinated regulation of endocannabinoid-mediated retrograde synaptic suppression in the cerebellum by neuronal and astrocytic monoacylglycerol lipase. Sci Rep. 2016 Oct 24;6:35829.