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Polmacoxib

Cat. No. M21500
Polmacoxib Structure
Synonym:

CG100649

Size Price Availability Quantity
5mg USD 80  USD80 In stock
10mg USD 135  USD135 In stock
25mg USD 270  USD270 In stock
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Quality Control & Documentation
Biological Activity

Polmacoxib (CG100649) is a first-in-class, orally active non-steroidal anti-inflammatory compound (NSAID) that acts as a dual inhibitor. It inhibited COX-2 (IC50 ~ 0.1 μg/ml) and carbonic anhydrase. CG100649's interaction with CA in red blood cells provides a new "tissue-specific" transport mechanism designed to deliver sustained levels of the compound to inflamed tissues while maintaining low systemic exposure. Its unique dual COX-2 and CA-binding properties are designed to provide potentially higher safety for cardiovascular, renal and gastrointestinal tissues than conventional NSaids or COX-2 inhibitor drugs. In mouse models, CG100649 inhibited precancerous and malignant colorectal lesions, in part by inhibiting tumor cell proliferation.

Chemical Information
Molecular Weight 361.39
Formula C18H16FNO4S
CAS Number 301692-76-2
Solubility (25°C) DMSO ≥ 200 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Yong-Soon Cho, et al. Clin Ther. Population Pharmacokinetic and Pharmacodynamic Analysis of Polmacoxib in Healthy Volunteers and Patients With Osteoarthritis

[2] In-Gyu Song, et al. Ann Coloproctol. An Unusual Case of Colon Perforation With Multiple Transmural Ulcers After Use of Polmacoxib and Everolimus in a Metastatic Breast Cancer Patient

[3] Claudiu T Supuran. Expert Opin Drug Metab Toxicol. An update on drug interaction considerations in the therapeutic use of carbonic anhydrase inhibitors

[4] Myungchul Lee, et al. Clin Orthop Surg. A Randomized, Multicenter, Phase III Trial to Evaluate the Efficacy and Safety of Polmacoxib Compared with Celecoxib and Placebo for Patients with Osteoarthritis

[5] Hyun Tae Kim, et al. Biochem Biophys Res Commun. Structural insight into the inhibition of carbonic anhydrase by the COX-2-selective inhibitor polmacoxib (CG100649)

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Keywords: Polmacoxib, CG100649 supplier, COX, inhibitors, activators


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