iNOS/COX-2-IN-1
iNOS/COX-2-IN-1 (Compound 12e) is an inhibitor of cyclooxygenase-2 (COX-2) and inducible nitric oxide synthase (iNOS). iNOS/COX-2-IN-1 inhibits the NF-κB and MAPKs signaling pathways and thus exerts anti-inflammatory effects.
Nos produits utilisent uniquement pour la recherche. Nous ne vendons pas aux patients.
- Formule: C31H38FN3O2S
- Masse moléculaire:535.72
-
Stockage:
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]
-
Activité biologique
-
Chemical Information
- Pureté et documentation
- Références
-
Help & FAQs
Activité biologique
|
COX-2 |
iNOS |
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| RAW264.7 | IC50 |
2.34 μM
Compound: 12e
|
Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production measured after 24 hrs incubation by Griess assay
Anti-inflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS-induced NO production measured after 24 hrs incubation by Griess assay
|
[PMID: 38704943] |
iNOS/COX-2-IN-1 (0.625-40 μM; 24 h) has no significant cytotoxicity against RAW 264.7 cells at a concentration of 5 μM[1].
iNOS/COX-2-IN-1 (2.5-10 μM; 1 h) significantly inhibits LPS-induced NO production, with a NO inhibition rate of 45.38% (5 μM). Concentration-dependently inhibits the expression of TNF-α and COX-2. Effectively inhibits mRNA expression of pro-inflammatory cytokines. Exerts its anti-inflammatory effect by inhibiting the activation of NF-κB signaling pathway [1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:RAW 264.7cells
-
Concentration:0.625, 1.25, 2.5, 5, 10, 20, 40 μM
-
Incubation Time:24 h
-
Result:The survival rate of RAW 264.7 cells was 97.44% at a concentration of 5 μM, indicating low cytotoxicity.
-
Cell Line:RAW 264.7cells
-
Concentration:2.5, 5, 10 μM
-
Incubation Time:1 h
-
Result:Dose-dependent inhibited the expression of iNOS and COX-2 proteins.
Significantly inhibited LPS-induced phosphorylation of NF-κB p65 and degradation of IκBα, and reduced translocation of NF-κB p65 from the cytoplasm to the nucleus.
Significantly inhibited LPS-induced phosphorylation of ERK, JNK and p38 MAPK.
-
Cell Line:RAW 264.7cells
-
Concentration:2.5, 5, 10 μM
-
Incubation Time:24 h
-
Result:Significantly reduced mRNA expression levels of TNF-α, iNOS, IL-6 and COX-2.
Chemical Information
-
Masse moléculaire 535.72
-
Formule C31H38FN3O2S
-
SMILES
FC1=CC=CC(C2CC([C@H]3CC[C@@]4([H])[C@]5([H])CC=C6C[C@@H](O)CC[C@]6(C)[C@@]5([H])CC[C@@]43C)=NN2C(SC7)=NC7=O)=C1
-
Livraison
Room temperature in continental US; may vary elsewhere.
-
Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Cai X, et al. Design, synthesis and molecular modeling of novel D-ring substituted steroidal 4,5-dihydropyrazole thiazolinone derivatives as anti-inflammatory agents by inhibition of COX-2/iNOS production and down-regulation of NF-κB/MAPKs in LPS-induced RAW264.7 macrophage cells. Eur J Med Chem. 2024 Apr 27;272:116460. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
iNOS/COX-2-IN-1 Related Classifications
HY-161513 Related Classifications
Powered by Bioz