Naproxcinod
Naproxcinod (Nitronaproxen) is the first in class of cyclooxygenase (COX)-inhibiting nitric oxide donators (CINODs). Naproxcinod shows analgesic and anti-inflammatory effects, it can be used for the research of osteoarthritis and inflammation.
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- CAS No.: 163133-43-5
- Formule: C18H21NO6
- Masse moléculaire:347.36
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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
Activité biologique
Description
In Vitro
Naproxcinod (1-30 μM; 15 min) concentration-dependently increases cGMP level up to 27-fold over basal level[1]. Naproxcinod (1-100 μM; 8 h) concentration-dependently increases HO-1 mRNA in endothelial cells[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:Endothelial and gastric mucosal cell lines
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Concentration:30-1000 μM
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Incubation Time:8 and 24 hours
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Result:Increased HO-1 protein levels in endothelial and gastric mucosal cells and increased HO-1mRNA levels in endothelial cells.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/10 mice with Duchenne muscular dystrophy (DMD)[3]
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Dosage:0, 10, 21 and 41 mg/kg
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Administration:Oral gavage; 0-41 mg/kg once daily for 42 weeks
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Result:Significantly improved fraction shortening and ejection fraction, and reduced inflammation in vivo.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 163133-43-5
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Masse moléculaire 347.36
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Formule C18H21NO6
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SMILES
C[C@@H](C1=CC=C2C=C(OC)C=CC2=C1)C(OCCCCO[N+]([O-])=O)=O
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Synonyms
AZD 3582; HCT 3012; Nitronaproxen
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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]. Berndt G, et al. A common pathway of nitric oxide release from AZD3582 and glyceryl trinitrate. Eur J Pharm Sci. 2004 Feb;21(2-3):331-5. [Content Brief]
[2]. Berndt G, et al. AZD3582 increases heme oxygenase-1 expression and antioxidant activity in vascular endothelial and gastric mucosal cells. Eur J Pharm Sci. 2005 Jun;25(2-3):229-35. [Content Brief]
[3]. Uaesoontrachoon K, et al. Long-term treatment with naproxcinod significantly improves skeletal and cardiac disease phenotype in the mdx mouse model of dystrophy. Hum Mol Genet. 2014 Jun 15;23(12):3239-49. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Naproxcinod Related Classifications
HY-14931 Related Classifications
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