WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 206123
Description: Polmacoxib, also known as CG100649, is a first-in-class NSAID drug candidate that is a dual inhibitor of COX-2 and carbonic anhydrase (CA). CG100649's interaction with CA in red blood cells provides it with a novel 'tissue-specific' transport mechanism that is designed to deliver sustained levels of drug to inflamed tissues, while maintaining low systemic exposure. Its unique dual COX-2 and CA binding properties are designed to provide potentially superior safety to cardiovascular, renal, and gastrointestinal tissues compared to traditional NSAIDs or COX-2 inhibitor drugs. CG100649 inhibits premalignant and malignant colorectal lesions in mouse models, partly through inhibiting tumor cell proliferation.
MedKoo Cat#: 206123
Chemical Formula: C18H16FNO4S
Exact Mass: 361.07841
Molecular Weight: 361.38734
Elemental Analysis: C, 59.82; H, 4.46; F, 5.26; N, 3.88; O, 17.71; S, 8.87
Synonym: CG100649; CG-100649; CG 100649; polmacoxib
IUPAC/Chemical Name: 4-(3-(3-fluorophenyl)-5,5-dimethyl-4-oxo-4,5-dihydrofuran-2-yl)benzenesulfonamide
InChi Key: IJWPAFMIFNSIGD-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H16FNO4S/c1-18(2)17(21)15(12-4-3-5-13(19)10-12)16(24-18)11-6-8-14(9-7-11)25(20,22)23/h3-10H,1-2H3,(H2,20,22,23)
SMILES Code: O=S(C1=CC=C(C(OC2(C)C)=C(C3=CC=CC(F)=C3)C2=O)C=C1)(N)=O
1: Kim SH, Margalit O, Katoh H, Wang D, Wu H, Xia D, Holla VR, Yang P, DuBois RN. CG100649, a novel COX-2 inhibitor, inhibits colorectal adenoma and carcinoma growth in mouse models. Invest New Drugs. 2014 Aug 3. [Epub ahead of print] PubMed PMID: 25085205.
2: Youn Choi H, Jin SJ, Jung JA, Kim UJ, Ko YJ, Noh YH, Bae KS, Lim HS. Effects of ketoconazole on the pharmacokinetic properties of CG100649, a novel NSAID: a randomized, open-label crossover study in healthy Korean male volunteers. Clin Ther. 2014 Jan 1;36(1):115-25. doi: 10.1016/j.clinthera.2013.12.004. PubMed PMID: 24417786.
3: Skarke C, Alamuddin N, Lawson JA, Cen L, Propert KJ, Fitzgerald GA. Comparative impact on prostanoid biosynthesis of celecoxib and the novel nonsteroidal anti-inflammatory drug CG100649. Clin Pharmacol Ther. 2012 Jun;91(6):986-93. doi: 10.1038/clpt.2012.3. Epub 2012 Jan 25. PubMed PMID: 22278334; PubMed Central PMCID: PMC3740579.