2. Immunology/Inflammation Metabolic Enzyme/Protease Apoptosis
  3. COX Lipoxygenase TNF Receptor Interleukin Related MMP
  4. 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.

For research use only. We do not sell to patients.

COX-2/5-LOX-IN-8

COX-2/5-LOX-IN-8 Chemical Structure

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COX-2/5-LOX-IN-8 Related Antibodies

Top Publications Citing Use of Products

View All COX Isoform Specific Products:

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COX COX-1 COX-2 COX-3

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5-LOX 12-LOX 15-LOX

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TNFRSF1A/CD120a TNFRSF3/CD18 TNFRSF4 TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF7/CD27 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF10B/DR5/CD262 TNFRSF12A/TWEAK TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

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IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22 IL-18

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MMP-1 MMP-2 MMP-3 MMP-8 MMP-9 MMP-13 MMP-14 MMP-17 ADAM10 ADAM17 MMP-7 MMP-12 MMP-10 MMP ADAM8 MMP-19

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Description

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[1].

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.

COX-2/5-LOX-IN-8 Related Antibodies
In Vivo

COX-2/5-LOX-IN-8 (150 mg/kg; p.o.; once daily; for 7 consecutive days) exerts a 98% inhibitory effect on monoiodoacetate (MIA)-induced paw edema in male Wistar rats, restores their hindlimb weight-bearing function, and significantly reduces serum markers of inflammation and cartilage degradation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 150 mg/kg
Administration: p.o.; daily; 7 consecutive days
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.
Molecular Weight

484.51

Formula

C20H16N6O5S2
SMILES

O=C(C(S1)=NNC21C(NC3=C2C=CC=C3)=O)NC4=CC=C(S(=O)(NC5=NOC(C)=C5)=O)C=C4
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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COX-2/5-LOX-IN-8 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

COX-2/5-LOX-IN-8COXLipoxygenaseTNF ReceptorInterleukin RelatedMMPCyclooxygenaseLOXTumor Necrosis Factor ReceptorTNFRILMatrix metalloproteinasesCOX-2IL-1βTNF-αleukotrieneprostaglandinbovine serum albuminosteoarthritiserythrocyte membranesrats5-LOXInhibitorinhibitorinhibit

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