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.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- CAS. Nr.: 163133-43-5
- Formel: C18H21NO6
- Molecular Weight:347.36
-
Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Biologische Aktivität
-
Chemical Information
- Protokoll
- Reinheit & Dokumentation
- Verweise
-
Help & FAQs
Biologische Aktivität
Beschreibung
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.
-
Cell Line:Endothelial and gastric mucosal cell lines
-
Concentration:30-1000 μM
-
Incubation Time:8 and 24 hours
-
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.
-
Animal Model:C57BL/10 mice with Duchenne muscular dystrophy (DMD)[3]
-
Dosage:0, 10, 21 and 41 mg/kg
-
Administration:Oral gavage; 0-41 mg/kg once daily for 42 weeks
-
Result:Significantly improved fraction shortening and ejection fraction, and reduced inflammation in vivo.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS. Nr. 163133-43-5
-
Molecular Weight 347.36
-
Formel C18H21NO6
-
SMILES
C[C@@H](C1=CC=C2C=C(OC)C=CC2=C1)C(OCCCCO[N+]([O-])=O)=O
-
Synonyms
AZD 3582; HCT 3012; Nitronaproxen
-
Versand
Room temperature in continental US; may vary elsewhere.
-
Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
-
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
Reinheit & Dokumentation
Verweise
[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
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Naproxcinod Related Classifications
HY-14931 Related Classifications
Powered by Bioz