DO34 analog
Based on 1 Customer Validation
DO34 analog is a structural analog of DO34 (HY-117771). DO34 is a selective DAGL inhibitor, with an IC50 of 6 nM for DAGLα conversion of SAG to 2-AG. DO34 blocks de novo 2-AG synthesis, and suppresses tonic CB1 receptor activation. DO34 blocks depolarization-induced suppression of excitation and inhibition in the cerebellum and hippocampus. DO34 regulates feeding behavior and locomotor activity in mice. DO34 abolishes AM251-mediated enhancement of parallel fiber-evoked excitatory postsynaptic currents in cerebellar slices from MAGL global knockout mice. DO34 can be used for the research of energy balance disorder and neuroinflammation.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 98.42%
- CAS. Nr.: 2098969-71-0
- Formel: C26H28F3N5O4
- Molecular Weight:531.53
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Biologische Aktivität
Beschreibung
IC50 & Target
[1]|
DAGLα 6 nM (IC50) |
DAGLβ |
In Vitro
Chemical Information
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CAS. Nr. 2098969-71-0
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Appearance Solid
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Molecular Weight 531.53
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Formel C26H28F3N5O4
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Color Light yellow to yellow
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SMILES
O=C(N1C(CC2=CC=CC=C2)CN(C(OC(C)(C)C)=O)CC1)N3N=CC(C4=CC=C(OC(F)(F)F)C=C4)=N3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : ≥ 105 mg/mL (197.54 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
* "≥" means soluble, but saturation unknown.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Protokoll
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Gene Editing
Gene editing modify specific sites within the genome through gene deletions, insertions or conversions to study functionally unknown genes or conduct gene therapy. It is also used to change the biological traits of organisms to establish new varieties. Gene editing techniques include zinc finger nuclease (ZFN), transcription activator-like effector nuclease (TALEN), and clustered regularly interspaced short palindromic repeats (CRISPR)/CRISPR-associated protein 9 (Cas 9) (CRISPR/Cas9).
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Protocol for Open Field Test (OF)
The Open Field Test is a rodent behavioral assay that measures spontaneous locomotion, exploratory behavior, and anxiety-like behavior when an animal is placed in a novel open arena. The main readouts are total distance traveled, movement time, velocity, center-zone entries, center-zone time, peripheral-zone time, and thigmotaxis. The assay is based on the conflict between exploration of a novel environment and avoidance of exposed open areas; higher center exploration is commonly interpreted as lower anxiety-like behavior, whereas increased wall-following or peripheral occupancy is interpreted as higher anxiety-like behavior.
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Research Protocol for Neurological Diseases
PINK1/Parkin-mediated mitophagy pathway is a mitochondrial quality-control signaling axis in which mitochondrial depolarization stabilizes PINK1 on damaged mitochondria, activates Parkin recruitment and E3 ubiquitin ligase activity, promotes ubiquitination of outer mitochondrial membrane proteins, recruits selective autophagy adaptors, and drives lysosomal degradation of damaged mitochondria. In neurological disease research, this pathway is experimentally important because neurons, especially dopaminergic neurons, are highly dependent on mitochondrial integrity, and defective mitochondrial turnover can lead to mitochondrial dysfunction, oxidative stress, impaired neuronal survival, α-synuclein accumulation, and neuroinflammatory damage-associated signals. The genetic disease link is strongest in Parkinson’s disease because mutations in PRKN/parkin cause autosomal recessive juvenile parkinsonism, mutations in PINK1 cause hereditary early-onset Parkinson’s disease, and Drosophila studie
Reinheit & Dokumentation
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Data Sheet (273 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
Verweise
[1]. Deng H, et al. Triazole Ureas Act as Diacylglycerol Lipase Inhibitors and Prevent Fasting-Induced Refeeding. J Med Chem. 2017;60(1):428-440. [Content Brief]
[2]. Liu X, et al. Coordinated regulation of endocannabinoid-mediated retrograde synaptic suppression in the cerebellum by neuronal and astrocytic monoacylglycerol lipase. Sci Rep. 2016;6:35829. Published 2016 Oct 24. [Content Brief]
[3]. 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;113(1):26-33. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.8814 mL | 9.4068 mL | 18.8136 mL | 47.0340 mL |
| 5 mM | 0.3763 mL | 1.8814 mL | 3.7627 mL | 9.4068 mL | |
| 10 mM | 0.1881 mL | 0.9407 mL | 1.8814 mL | 4.7034 mL | |
| 15 mM | 0.1254 mL | 0.6271 mL | 1.2542 mL | 3.1356 mL | |
| 20 mM | 0.0941 mL | 0.4703 mL | 0.9407 mL | 2.3517 mL | |
| 25 mM | 0.0753 mL | 0.3763 mL | 0.7525 mL | 1.8814 mL | |
| 30 mM | 0.0627 mL | 0.3136 mL | 0.6271 mL | 1.5678 mL | |
| 40 mM | 0.0470 mL | 0.2352 mL | 0.4703 mL | 1.1759 mL | |
| 50 mM | 0.0376 mL | 0.1881 mL | 0.3763 mL | 0.9407 mL | |
| 60 mM | 0.0314 mL | 0.1568 mL | 0.3136 mL | 0.7839 mL | |
| 80 mM | 0.0235 mL | 0.1176 mL | 0.2352 mL | 0.5879 mL | |
| 100 mM | 0.0188 mL | 0.0941 mL | 0.1881 mL | 0.4703 mL |