COX-2/5-LOX-IN-8
COX-2/5-LOX-IN-8 is an orally active dual COX-2/5-LOX inhibitor, with an IC50 of 6.30 μM against sheep-derived COX-2 and an IC50 of 8.09 μM against 5-LOX. COX-2/5-LOX-IN-8 acts as a membrane stabilizer that stabilizes erythrocyte membranes against hypotonicity-induced hemolysis. COX-2/5-LOX-IN-8 functions as a protein stabilizer that inhibits heat-induced denaturation of bovine serum albumin. COX-2/5-LOX-IN-8 reduces paw swelling, improves hind limb weight-bearing function, decreases serum levels of pro-inflammatory cytokines (TNF-α, IL-1β, IL-6, CRP), and lowers serum levels of cartilage degradation biomarkers (COMP, MMP-3, CTX-II). COX-2/5-LOX-IN-8 can be used in the research of osteoarthritis.
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- Formule: C20H16N6O5S2
- Masse moléculaire:484.51
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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]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
Description
IC50 & Target
[1]|
Ovine COX-2 6.3 μM (IC50) |
5-LOX 8.09 μM (IC50) |
TNF-α |
IL-1β |
IL-6 |
MMP-3 |
In Vitro
COX-2/5-LOX-IN-8 (Compound 9) potently stabilizes rat erythrocyte membranes and resists hypotonicity-induced hemolysis, with an IC50 of 51.60 μM[1].
COX-2/5-LOX-IN-8 (31.25-500 μg/mL; 20 min (37 °C); 3 min (60 °C)) effectively inhibits heat-induced bovine serum albumin (BSA) denaturation[1].
COX-2/5-LOX-IN-8 (0.5-1000 μg/mL; 10 min) potently and selectively inhibits ovine COX-2, with an IC50 of 6.30 μM[1].
COX-2/5-LOX-IN-8 (0.5-1000 μg/mL; 10-15 min) potently inhibits 5-LOX with an IC50 value of 8.09 μM[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar (male; osteoarthritis induced by intra-articular injection of 50 μL of 80 mg/mL mono-iodoacetate into the right ankle joint)[1]
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Dosage:150 mg/kg
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Administration:p.o.; daily; 7 consecutive days
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Result:Reduced paw edema volume to 0.08 cm3, corresponding to 98% inhibition relative to the MIA-induced control group.
Restored hind-limb weight-bearing ratio to 1.00, matching the normal control group.
Caused 80-85% reductions in serum levels of pro-inflammatory markers TNF-α, IL-1β, and CRP, bringing levels comparable to the normal control group.
Caused 70-85% reductions in cartilage degradation markers COMP, MMP-3, and CTX-II.
Chemical Information
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Masse moléculaire 484.51
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Formule C20H16N6O5S2
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SMILES
O=C(C(S1)=NNC21C(NC3=C2C=CC=C3)=O)NC4=CC=C(S(=O)(NC5=NOC(C)=C5)=O)C=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.
Pureté et documentation
Références
[1]. El-Saghier AM, et al. Design, synthesis, and biological evaluation of novel Spirosulfamethoxazole-1,3,4-thiadiazole-2-carboxamide derivatives as dual COX-2/5-LOX inhibitors with promising anti-inflammatory and anti-osteoarthritic potential. Bioorg Chem. Published online May 12, 2026. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
COX-2/5-LOX-IN-8 Related Classifications
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