2. Immunology/Inflammation Metabolic Enzyme/Protease Neuronal Signaling
  3. COX Carbonic Anhydrase Cholinesterase (ChE)
  4. 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.

COX-2-IN-67

COX-2-IN-67 Chemical Structure

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COX-2-IN-67 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

View All Carbonic Anhydrase Isoform Specific Products:

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CA CA I CA Ⅱ CA IX CA XII CA VII CA VI CA VA CA VB CA XIII CA XIV

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AChE BChE

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Description

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[1].

IC50 & Target[1]

hCOX-2

0.07 μM (IC50)

hCA IX

62.7 nM (Ki)

BuChE

0.47 μM (IC50)

In Vitro

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.

COX-2-IN-67 Related Antibodies
In Vivo

COX-2-IN-67 (compound 10b) (1.2-20 mg/kg; p.o., i.n.; daily; 2 weeks) significantly improves hippocampal-dependent cognitive performance, normalizes metabolic parameters, reduces hepatic stress, and attenuates hippocampal oxidative stress and neuroinflammation in rats with high-fat diet-induced metabolic dysfunction-associated mild cognitive impairment[1].

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

Animal Model: non-obese prediabetic strain[1]
Dosage: 20 mg/kg (oral); 1.2 mg/kg (intranasal nanoformulated)
Administration: p.o.; daily; 2 weeks; i.n.; daily; 2 weeks
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.
Molecular Weight

830.28

Formula

C40H35ClF3N9O4S
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
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-IN-67 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-IN-67COXCarbonic AnhydraseCholinesterase (ChE)CyclooxygenaseCarbonate dehydratasehuman carbonic anhydrase IXhuman plasmahippocampus-dependent cognitive performancemetabolic dysfunction-associated mild cognitive impairmenthigh-fat diet-induced rat modelshuman serum albuminneuronal cellshuman butyrylcholinesterasecyclooxygenase-2human SH-SY5Y neuroblastoma cellsInhibitorinhibitorinhibit

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