COX-2-IN-6

SKU: orb1687977

Description

COX-2-IN-6 is a potent, selective, and orally bioavailable COX-2 inhibitor, demonstrating activity in both enzymatic (IC₅₀=0.84 µM, Kᵢ=69 nM) and cellular PGE₂ synthesis (IC₅₀=0.60 µM) assays. Its research applications include the study of inflammation and the chemoprevention of colorectal cancer in experimental models.

Research Area

Immunology & Inflammation, Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 2756347-91-6
• MW: 409.5
• Purity: 99.69% (May vary between batches)
• Formula: C₂₀H₂₇NO₆S
• SMILES: O(CC(C)(C)O)C1=C(C=C(CO)C(OCCC)=N1)C2=CC=C(S(C)(=O)=O)C=C2
• Target: Prostaglandin Receptor,COX
• Solubility: DMSO:60 mg/mL (146.52 mM)

Bioactivity

• Target IC50:
  COX-2:0.84 μM
• In Vivo:
  COX-2-IN-6 (Compound 10) (30, 100, 300 mg/kg; oral; single dose; APCmin/mouse model) inhibits adenoma progression and extends survival in the APCmin/+ mouse model. COX-2-IN-6 (10 mg/kg; oral; single dose; APCmin/+ mouse model) exhibits high colonic exposure (>4300 ng/g) and low systemic exposure (<6 ng/mL), C/P distribution ratio > 1200 in 4 hours.
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• In Vitro:
  COX-2-IN-6 (Compound 10) inhibits human COX-2/COX-1 enzyme and COX-2/COX-1-driven PGE2 synthesis in HEK293 cells, with IC50 of 0.84 μM、>50 μM、0.60 μM and, >50 μM, respectively. COX-2-IN-6 exhibits stability in human or mouse liver microsomes and hepatocytes in vitro. The T1/2 value of human hepatocytes is 3.1 min, and the T1/2 value of mouse hepatocytes is 3.0 min.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

COX-2, ProstaglandinReceptor, Prostaglandin Receptor, PGE2

Compound Identifiers

PubChem CID

156587566