2. Immunology/Inflammation Metabolic Enzyme/Protease
  3. COX Carbonic Anhydrase
  4. Polmacoxib

Polmacoxib  (Synonyms: CG100649)

Cat. No.: HY-16726 Purity: 99.70%
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Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models.

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

Polmacoxib Chemical Structure

Polmacoxib Chemical Structure

CAS No. : 301692-76-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 88 In-stock
Solution
10 mM * 1 mL in DMSO USD 88 In-stock
Solid
1 mg USD 32 In-stock
5 mg USD 80 In-stock
10 mg USD 135 In-stock
25 mg USD 280 In-stock
50 mg USD 445 In-stock
100 mg USD 680 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of Polmacoxib:

Polmacoxib Related Antibodies

Top Publications Citing Use of Products

View All COX Isoform Specific Products:

View All Isoforms
COX COX-1 COX-2 COX-3

View All Carbonic Anhydrase Isoform Specific Products:

View All Isoforms
CA CA I CA Ⅱ CA Ⅸ CA XII

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Polmacoxib (CG100649) is a first-in-class, orally active nonsteroidal anti-inflammatory agent (NSAID) which is a dual inhibitor of COX-2 (IC50 around 0.1 μg/ml) and carbonic anhydrase[1]. Polmacoxib inhibits colorectal adenoma and tumor growth in mouse models[2].

IC50 & Target[1]

COX-2

0.1 μg/mL (IC50)

carbonic anhydrase

 

In Vitro

Polmacoxib (CG100649) (0-1 μg/ml; 24 hours; HCA-7 and HT-29 cells) can inhibit COX-2 activity and PGE2 production in human colon cancer cells, at lower concentrations compared to Celecoxib[2].

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

Polmacoxib Related Antibodies
In Vivo

Polmacoxib (7 mg/kg; p.o.; daily for 8 weeks) suppresses intestinal polyp formation in ApcMin/+ mice[2].
Polmacoxib (7-15 mg/kg; p.o.; daily from day 27 post-injection to day 111; athymic nude mice; subcutaneous xenograft mouse model) reduces tumor volume and tumor weight by 58% and 48%, respectively, compared to a 48% and 36% reduction following treatment with Celecoxib[2].
Polmacoxib (7-15 mg/kg; p.o.; began on day 14 and continued for 8 weeks; athymic nu/nu mice; orthotopic xenograft mouse model) inhibits CRC growth in an orthotopic xenograft mouse model, reducing tumor weight by 70% using 7 mg/kg or by 83% using 15 mg/kg, compared to a similar 70% reduction following treatment with 500 mg/kg of Celecoxib[2].

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

361.39

Formula

C18H16FNO4S
CAS No.
Appearance

Solid

Color

Light yellow to green yellow

SMILES

O=S(C1=CC=C(C(OC2(C)C)=C(C3=CC=CC(F)=C3)C2=O)C=C1)(N)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (691.77 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 2.7671 mL 13.8355 mL 27.6709 mL
5 mM 0.5534 mL 2.7671 mL 5.5342 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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (5.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (5.76 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 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

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 2.7671 mL 13.8355 mL 27.6709 mL 69.1773 mL
5 mM 0.5534 mL 2.7671 mL 5.5342 mL 13.8355 mL
10 mM 0.2767 mL 1.3835 mL 2.7671 mL 6.9177 mL
15 mM 0.1845 mL 0.9224 mL 1.8447 mL 4.6118 mL
20 mM 0.1384 mL 0.6918 mL 1.3835 mL 3.4589 mL
25 mM 0.1107 mL 0.5534 mL 1.1068 mL 2.7671 mL
30 mM 0.0922 mL 0.4612 mL 0.9224 mL 2.3059 mL
40 mM 0.0692 mL 0.3459 mL 0.6918 mL 1.7294 mL
50 mM 0.0553 mL 0.2767 mL 0.5534 mL 1.3835 mL
60 mM 0.0461 mL 0.2306 mL 0.4612 mL 1.1530 mL
80 mM 0.0346 mL 0.1729 mL 0.3459 mL 0.8647 mL
100 mM 0.0277 mL 0.1384 mL 0.2767 mL 0.6918 mL
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Polmacoxib 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:

Polmacoxib301692-76-2CG100649CG 100649CG-100649COXCarbonic AnhydraseCyclooxygenaseCarbonate dehydratasecolorectaladenomatumorNSAIDinflammatorypolyporthotopicInhibitorinhibitorinhibit

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