COR170
COR170 (11u) is a selective CB2 inverse-agonist which is a 4-quinolone-3-carboxylic acid derivative with a Ki value of 3.8 nM for CB2 receptor. COR170 can be used for the research of inflammation and neuroprotection.
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- CAS No.: 1048039-15-1
- Formule: C31H36N2O2
- Masse moléculaire:468.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Protocole
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
In Vitro
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Mice with formalin (1.25%, 30 μL) injections[3]
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Dosage:1.5, 3 and 6 mg/kg
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Administration:Intraperitoneal injection; 1.5, 3 and 6 mg/kg for once
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Result:Reduced the late phase nociceptive behaviour induced by formalin with a 6 mg/kg dose and 10 min before formalin and abolished the analgesic effect from GW405833 which is a CB2 receptor partial agonist.
Chemical Information
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CAS No. 1048039-15-1
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Masse moléculaire 468.63
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Formule C31H36N2O2
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SMILES
O=C(C1=CN(CCCCC)C2=CC=C(C3=CC=CC=C3)C=C2C1=O)NC45C[C@H](C6)C[C@H](C[C@H]6C5)C4
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocole
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Research Protocol for Inflammation-related Diseases
The NLRP3 inflammasome is a cytosolic innate immune signaling platform that integrates priming signals and danger-signal activation to promote caspase-1 activation, maturation of IL-1β and IL-18, and gasdermin D-mediated pyroptotic cell death. The core experimental logic is to determine whether inflammatory disease phenotypes are driven by increased NLRP3 expression, ASC-containing inflammasome assembly, caspase-1 cleavage, GSDMD cleavage, and extracellular release of IL-1β/IL-18 rather than by nonspecific cell injury alone. The pathway is strongly linked to inflammation-related disease phenotypes because monosodium urate crystals activate NALP3/NLRP3 inflammasome signaling in gout-like crystal inflammation, cholesterol crystals activate NLRP3 inflammasomes in atherogenesis models, and DSS-induced intestinal inflammation has been reported to involve NLRP3 inflammasome activity. However, experimental colitis studies also show context-dependent protective effects of NLRP3 inflammasome co
Pureté et documentation
Références
[1]. Contartese A, et al. A novel CB2 agonist, COR167, potently protects rat brain cortical slices against OGD and reperfusion injury. Pharmacol Res. 2012 Dec;66(6):555-63. [Content Brief]
[2]. Pasquini S, et al. Investigations on the 4-quinolone-3-carboxylic acid motif. 2. Synthesis and structure-activity relationship of potent and selective cannabinoid-2 receptor agonists endowed with analgesic activity in vivo. J Med Chem. 2008 Aug 28;51(16): [Content Brief]
[3]. Cascio MG, et al. In vitro and in vivo pharmacological characterization of two novel selective cannabinoid CB(2) receptor inverse agonists. Pharmacol Res. 2010 Apr;61(4):349-54. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
COR170 Related Classifications
HY-103331 Related Classifications
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