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Polmacoxib

Name: Polmacoxib
Brand: TargetMol
SKU: T21294
Price: 39 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T21294Cas No. 301692-76-2

Alias CG-100649, CG100649, CG 100649

Polmacoxib (CG 100649) is a first-in-class NSAID drug candidate, is a dual inhibitor of carbonic anhydrase (CA) and COX-2. Polmacoxib inhibits premalignant and malignant colorectal lesions in mouse models, partly through inhibiting tumor cell proliferation.

Polmacoxib

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Purity: 97.88%

Catalog No. T21294Alias CG-100649, CG100649, CG 100649Cas No. 301692-76-2

Pack Size	Price	USA Warehouse	Global Warehouse
2 mg	$39	In Stock	In Stock
5 mg	$64	In Stock	In Stock
10 mg	$109	In Stock	In Stock
25 mg	$183	In Stock	In Stock
50 mg	$272	In Stock	In Stock
100 mg	$397	In Stock	In Stock
200 mg	$593	-	In Stock
1 mL x 10 mM (in DMSO)	$70	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:97.88%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Polmacoxib AI Summary

Polmacoxib exhibits potent in vitro inhibitory activity against prostaglandin G/H synthase 2 (COX-2) with an IC50 of 0.003 μg/mL and prostaglandin G/H synthase 1 (COX-1) with an IC50 of 0.3 μg/mL. It shows high selectivity for COX-2 over COX-1 with a selectivity ratio of 100.0. In vivo, Polmacoxib effectively inhibits carrageenan-induced rat foot edema by 47.0% when administered at 3 mg/kg orally and shows significant anti-inflammatory activity in adjuvant-induced arthritis in rats, with ED50 values ranging from 0.01 to 0.1 mg/kg/day. Additionally, the compound displays analgesic properties by reducing thermal stimuli-induced nociceptive responses by 92.0% at a dose of 1 mg/kg in carrageenan-stimulated Sprague-Dawley rats and diminishes the number of abdominal constrictions in ICR mice with an ED50 of 12.3 mg/kg. However, at a dose of 5 mg/kg, Polmacoxib exhibits gastric ulcerogenicity with an activity value of 1.5..

Note: Summary generated by AI. Data source: ChEMBL

Bioactivity

Description	Polmacoxib (CG 100649) is a first-in-class NSAID drug candidate, is a dual inhibitor of carbonic anhydrase (CA) and COX-2. Polmacoxib inhibits premalignant and malignant colorectal lesions in mouse models, partly through inhibiting tumor cell proliferation.
Targets&IC50	COX-2:0.1 μg/mL (IC50)
Synonyms	CG-100649, CG100649, CG 100649

Chemical Properties

Molecular Weight	361.39
Formula	C₁₈H₁₆FNO₄S
Cas No.	301692-76-2
Smiles	CC1(C)OC(=C(C1=O)c1cccc(F)c1)c1ccc(cc1)S(N)(=O)=O
Relative Density.	1.361 g/cm3 (Predicted)

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

H2O: Insoluble

DMSO: 55 mg/mL (152.19 mM), Sonication is recommended.

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	2.7671 mL	13.8355 mL	27.6709 mL	138.3547 mL
5 mM	0.5534 mL	2.7671 mL	5.5342 mL	27.6709 mL
10 mM	0.2767 mL	1.3835 mL	2.7671 mL	13.8355 mL
20 mM	0.1384 mL	0.6918 mL	1.3835 mL	6.9177 mL
50 mM	0.0553 mL	0.2767 mL	0.5534 mL	2.7671 mL
100 mM	0.0277 mL	0.1384 mL	0.2767 mL	1.3835 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc