2. Immunology/Inflammation
  3. COX
  4. COX-2-IN-6

COX-2-IN-6 (compound 10) is an orally active, gut-restricted and selective cyclooxygenase-2 (COX-2) inhibitor for colorectal Chemoprevention of cancer. COX-2-IN-6 selectively targets COX-2 with an IC50 of 0.84 μM and a Ki of 69 nM. COX-2-IN-6 also inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM.

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COX-2-IN-6 Chemical Structure

COX-2-IN-6 Chemical Structure

CAS No. : 2756347-91-6

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Based on 1 publication(s) in Google Scholar

COX-2-IN-6 Related Antibodies

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COX COX-1 COX-2 COX-3

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Description

COX-2-IN-6 (compound 10) is an orally active, gut-restricted and selective cyclooxygenase-2 (COX-2) inhibitor for colorectal Chemoprevention of cancer. COX-2-IN-6 selectively targets COX-2 with an IC50 of 0.84 μM and a Ki of 69 nM. COX-2-IN-6 also inhibits COX-2-driven PGE2 synthesis with an IC50 of 0.60 μM[1].

IC50 & Target

COX-2

 

In Vitro

COX-2-IN-6 (compound 10) inhibits human COX-2/COX-1 enzymes, and COX-2/COX-1-driven PGE2 synthesis in HEK293 cells with IC50s of 0.84 μM, >50 μM, 0.60 μM, and >50 μM, respectively[1].
COX-2-IN-6 shows liver microsomal and hepatocyte stability in vitro of human or mouse. And the T1/2 values are 3.1 min for human hepatocyte and 3.0 min for mouse hepatocyte[1].

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

COX-2-IN-6 Related Antibodies
In Vivo

COX-2-IN-6 (compound 10) (30-300 mg/kg; po; single dose) inhibits adenoma progression and enhances survival extension in an APCmin/+ mouse model[1].
COX-2-IN-6 (10 mg/kg; po; single dose) displays high colonic exposures (>4300 ng/g) and a low systemic exposure (<6 ng/mL) with a distribution ratio of C/P >1200 at 4 h[1].

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

Animal Model: APCmin/+ mouse model[1]
Dosage: 30 mg/kg, 100 mg/kg, 300 mg/kg
Administration: PO; daily in chow diet
Result: Significantly decreased [18F]-FDG uptake and polyp area.
Molecular Weight

409.50

Formula

C20H27NO6S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCOC1=NC(OCC(C)(O)C)=C(C=C1CO)C2=CC=C(C=C2)S(C)(=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (244.20 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.4420 mL 12.2100 mL 24.4200 mL
5 mM 0.4884 mL 2.4420 mL 4.8840 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.4420 mL 12.2100 mL 24.4200 mL 61.0501 mL
5 mM 0.4884 mL 2.4420 mL 4.8840 mL 12.2100 mL
10 mM 0.2442 mL 1.2210 mL 2.4420 mL 6.1050 mL
15 mM 0.1628 mL 0.8140 mL 1.6280 mL 4.0700 mL
20 mM 0.1221 mL 0.6105 mL 1.2210 mL 3.0525 mL
25 mM 0.0977 mL 0.4884 mL 0.9768 mL 2.4420 mL
30 mM 0.0814 mL 0.4070 mL 0.8140 mL 2.0350 mL
40 mM 0.0611 mL 0.3053 mL 0.6105 mL 1.5263 mL
50 mM 0.0488 mL 0.2442 mL 0.4884 mL 1.2210 mL
60 mM 0.0407 mL 0.2035 mL 0.4070 mL 1.0175 mL
80 mM 0.0305 mL 0.1526 mL 0.3053 mL 0.7631 mL
100 mM 0.0244 mL 0.1221 mL 0.2442 mL 0.6105 mL
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COX-2-IN-6 Related Classifications

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-62756347-91-6COXCyclooxygenaseInhibitorinhibitorinhibit

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