COX-2-IN-30
COX-2-IN-30 is a benzenesulfonamide derivative, as well as an orally active and dual inhibitor of COX (IC50=49 nM for COX-2, 10.4 μM for COX-1) and 5-LOX (IC50=2.4 μM). COX-2-IN-30 also inhibits transmembrane hCA IX and hCA XII isoform with nanomolar calss Ki values. COX-2-IN-30 exhibits analgesic, anti-inflammatory, and ulcerogenic activities, and does not show acute gastric effect.
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- No. CAS: 1160498-08-7
- Fòrmula: C17H16N6O3S
- Peso molecular:384.41
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
COX-2 49 nM (IC50) |
COX-1 10.4 μM (IC50) |
hCA I 183.4 nM (Ki) |
hCA II 81.4 nM (Ki) |
hCA IX 38.4 nM (Ki) |
hCA XII 21.6 nM (Ki) |
5-LOX 2.4 μM (IC50) |
In Vitro
COX-2-IN-30 (compound 7a) binds to hCA isoforms with Ki values of 183.4 nM (hCA I), 81.4 nM (hCA II), 38.4 nM (hCA IX), 21.6 nM (hCA XII), respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
COX-2-IN-30 (10 mg/kg; po; single dose) results a significant reduction of paw height in Carrageenan (HY-125474)-induced rat paw edema assay. And COX-2-IN-30 siginificantly decreases the levels of TNF-α and IL-1β[1].
COX-2-IN-30 (10 mg/kg; po; single dose)shows safety profile on the gastric tissues, in male albino rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Albino mice (25-30 g)[1]
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Dosage:10 mg/kg
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Administration:PO; single dose; after one hour, 0.1 mL of 1 percent acetic acid in a volume of 0.1 mL/10 g body weight was used to produce writhing.
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Result:Decreased the number of writhing responses of mouse conpared with control group.
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Animal Model:Paw edema rat induced by Carrageenan (HY-125474)[1]
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Dosage:10 mg/kg
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Administration:PO; single dose; after one hour, 0.1 mL of 1% carrageenan solution was injected in the left hind paw; measure inflammation height at 0, 1, 2, and 3 h
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Result:Showed a significant reduction of paw height compared to control after 3 h.
Chemical Information
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No. CAS 1160498-08-7
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Peso molecular 384.41
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Fòrmula C17H16N6O3S
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SMILES
O=C(C1=C(N(N=C1)C2=CC=C(C=C2)S(N)(=O)=O)N)N/N=C/C3=CC=CC=C3
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
[1]. Ragab MA, et al. 4-(5-Amino-pyrazol-1-yl)benzenesulfonamide derivatives as novel multi-target anti-inflammatory agents endowed with inhibitory activity against COX-2, 5-LOX and carbonic anhydrase: Design, synthesis, and biological assessments. Eur J Med Chem. 2023 Mar 15;250:115180. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
COX-2-IN-30 Related Classifications
HY-149269 Related Classifications
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