COX-2-IN-67
COX-2-IN-67 is an orally active, blood-brain barrier permeable multi-target inhibitor that potently targets COX-2 (IC50=0.07 μM), hCA IX (Ki=62.7 nM) and hBuChE (IC50=0.47 μM). COX-2-IN-67 alleviates oxidative stress and liver stress, improves glucose homeostasis and insulin sensitivity, and optimizes lipid profiles. Meanwhile, COX-2-IN-67 effectively reduces the levels of neuroinflammatory markers and improves hippocampus-dependent cognitive function in a high-fat diet-induced rat model. COX-2-IN-67 can be used for the research of metabolic dysfunction-associated mild cognitive impairment.
For research use only. We do not sell to patients.
- Formula: C40H35ClF3N9O4S
- Molecular Weight:830.28
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Storage:
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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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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hCOX-2 0.07 μM (IC50) |
hCA IX 62.7 nM (Ki) |
BuChE 0.47 μM (IC50) |
COX-2-IN-67 (compound 10b) shows reduced neurotoxicity against human SH-SY5Y neuroblastoma cells with an IC50 of 48.54 μM[1].
COX-2-IN-67 (5 min) binds moderately to human serum albumin with a KD of 10.2 μM, resulting in ~98.5% bound fraction at physiological conditions[1].
COX-2-IN-67 (20 μM; 4 h) demonstrates stability in human plasma when incubated at 37 °C, with no significant degradation detected[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:non-obese prediabetic strain[1]
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Dosage:20 mg/kg (oral); 1.2 mg/kg (intranasal nanoformulated)
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Administration:p.o.; daily; 2 weeks; i.n.; daily; 2 weeks
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Result:Significantly improved the composite hippocampal z-score compared to untreated high-fat diet-fed rats, with effects comparable to donepezil and greater than celecoxib or acetazolamide; the intranasal nanoformulation produced modestly greater cognitive improvement than the oral formulation.
Reversed high-fat diet-induced increases in fasting blood glucose, fasting serum insulin, total serum cholesterol, and serum triglycerides, restoring levels to extents comparable to reference drugs.
Reduced high-fat diet-induced elevated serum aspartate aminotransferase (AST) levels toward normal control values (oral formulation).
Reduced hippocampal malondialdehyde (MDA) levels to a degree comparable to donepezil (oral formulation); produced a further decrease in MDA (intranasal nanoformulated).
Increased hippocampal reduced glutathione (GSH) levels more than donepezil, achieving the highest GSH levels among all treatment groups (intranasal nanoformulated).
Reduced hippocampal interleukin-1β (IL-1β) and interleukin-6 (IL-6) levels more effectively than reference drugs, with the intranasal nanoformulation showing the greatest efficacy.
Chemical Information
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Molecular Weight 830.28
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Formula C40H35ClF3N9O4S
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SMILES
COC1=CC(/C=N/NC2=C3CCCCC3=NC4=CC=CC=C42)=CC=C1OCC5=CN(N=N5)C6=CC=C(C=C6)C7=CC(C(F)(F)F)=NN7C8=CC=C(C=C8)S(N)(=O)=O.Cl
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
COX-2-IN-67 Related Classifications
HY-184292 Related Classifications
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- COX-2-IN-67
- COX
- Carbonic Anhydrase
- Cholinesterase (ChE)
- human carbonic anhydrase IX
- human plasma
- hippocampus-dependent cognitive performance
- metabolic dysfunction-associated mild cognitive impairment
- high-fat diet-induced rat models
- human serum albumin
- neuronal cells
- human butyrylcholinesterase
- cyclooxygenase-2
- human SH-SY5Y neuroblastoma cells
- Inhibitor
- inhibitor
- inhibit