DO34 |
カタログ番号GC31446
One-Click Copy Product Info
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DO34 は、SAG から 2-AG への DAGLα 変換の IC50 が 6 nM で、DAGLβ の IC50 が 6 nM である、非常に強力で選択的かつ中枢活性なジアシルグリセロール リパーゼ (DAGL) 阻害剤です。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1848233-58-8
Sample solution is provided at 25 µL, 10mM.
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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.
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].
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].
[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.
Animal experiment: | 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: [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. | |
| Cas No. | 1848233-58-8 | SDF | |
| Canonical 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 | ||
| Formula | C26H28F3N5O4 | M.Wt | 531.53 |
| 溶解度 | DMSO : ≥ 100 mg/mL (188.14 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8814 mL | 9.4068 mL | 18.8136 mL |
| 5 mM | 376.3 μL | 1.8814 mL | 3.7627 mL |
| 10 mM | 188.1 μL | 940.7 μL | 1.8814 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)