1. Immunology/Inflammation
  2. COX
  3. COX-2-IN-2

COX-2-IN-2 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX-2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities.

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

COX-2-IN-2 Chemical Structure

COX-2-IN-2 Chemical Structure

CAS No. : 134729-13-8

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1 mg USD 1580 In-stock
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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

COX-2-IN-2 is a selective and inducible COX2 inhibitor with an IC50 of 0.24 μM. COX-2-IN-1 is an anti-inflammatory compound with anti-inflammatory and analgesic activities.

IC50 & Target[1]

COX-2

240 nM (IC50)

In Vitro

COX-2-IN-2 shows no COX-1 inhibition even at 100μM[1].

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

In Vivo

COX-2-IN-2 has oral ED50 values of 0.030 and 0.47mg/kg on adjuvant-induced arthritis and collagen-induced arthritis, respectively, and an ED30 value of 7.4mg/kg in the yeast-induced hyperalgesia (Randall-Selitto) assay. COX-2-IN-2 shows good analgesic activity and no ulcerogenicity[1].

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

Molecular Weight

341.36

Formula

C17H12FN3O2S

CAS No.
Unlabeled Cas

Appearance

Solid

Color

Off-white to light yellow

SMILES

N#CC1=NN(C2=CC=C(F)C=C2)C(C3=CC=C(S(=O)(C)=O)C=C3)=C1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (146.47 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 2.9295 mL 14.6473 mL 29.2946 mL
5 mM 0.5859 mL 2.9295 mL 5.8589 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.32 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Kinase Assay
[1]

hCOX1 or hCOX2 is preincubated with COX2-IN-2 in 0.1 M Tris-HCl buffer containing 2 μM hematin and 5 mM L-tryptophan at 30°C for 5 min, followed by a 5 min incubation with arachidonic acid. The enzyme reaction is stopped by the addition of 1 N HCl. The PGE2 formed is extracted with EtOAc and measured by RIA[1].

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

Animal Administration
[1]

Rats: Ten male Sprague Dawley rats are used per group. A suspension of 0.5% brewer's yeast in 0.5% methyl cellulose is injected into the right hind paw. The pain threshold us determined 3h after yeast injection. COX-2-IN-2 is given orally 2 h after yeast injection. The pain threshold in the treated rats are compared with that in the control rats[1].

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

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. 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 2.9295 mL 14.6473 mL 29.2946 mL 73.2365 mL
5 mM 0.5859 mL 2.9295 mL 5.8589 mL 14.6473 mL
10 mM 0.2929 mL 1.4647 mL 2.9295 mL 7.3236 mL
15 mM 0.1953 mL 0.9765 mL 1.9530 mL 4.8824 mL
20 mM 0.1465 mL 0.7324 mL 1.4647 mL 3.6618 mL
25 mM 0.1172 mL 0.5859 mL 1.1718 mL 2.9295 mL
30 mM 0.0976 mL 0.4882 mL 0.9765 mL 2.4412 mL
40 mM 0.0732 mL 0.3662 mL 0.7324 mL 1.8309 mL
50 mM 0.0586 mL 0.2929 mL 0.5859 mL 1.4647 mL
60 mM 0.0488 mL 0.2441 mL 0.4882 mL 1.2206 mL
80 mM 0.0366 mL 0.1831 mL 0.3662 mL 0.9155 mL
100 mM 0.0293 mL 0.1465 mL 0.2929 mL 0.7324 mL
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COX-2-IN-2 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.

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COX-2-IN-2
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