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MedChemExpress - Model Bromfenac - ...

MedChemExpress - Model Bromfenac - 91714-94-2

Bromfenac is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac can be used in ocular inflammation research[1].

Bromfenac

MCE China：Bromfenac

Brand：MedChemExpress (MCE)

Cat. No.HY-B1888

CAS：91714-94-2

Storage：Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping：Room temperature in continental US; may vary elsewhere.

Description：Bromfenac is a potent and orally active inhibitor of COX, with IC50s of 5.56 and 7.45 nM for COX-1 and COX-2, respectively. Bromfenac can be used in ocular inflammation research.

In Vitro：Bromfenac (0-80 μg/mL; 24 h) can inhibit transforming growth factor-β2-induced epithelial-mesenchymal transition in HLEC-B3 in a concentration-dependent manner[2]. Bromfenac (80 μg/mL; 48 h) inhibits transforming growth factor-β2-induced epithelial-mesenchymal transition in human anterior capsules[2].

In Vivo：Bromfenac (0.0032-3.16%; 100 or 200 μL; rubbed onto the backs) produces significant anti-inflammatory activity at concentrations as low as 0.1% (4 h pretreatment time) or 0.32% (18h pretreatment time) in rats[3]. Bromfenac (0.032-3.16%; 100 μL; rubbed onto the paws) produces dose-related anti-inflammatory activity in rats[3]. Bromfenac (0.032-1.0%; 50 μL) is 26 times more potent than indomethacin in blocking the erythema when applied directly onto the skin area exposed to UV light in guinea pigs[3]. Bromfenac (0.0032-0.1%; 50 μL; rubbed onto the uninjected paw for 4 h per day and 5 days per week) produces a dose and time dependent reduction in the paw volume of both hind limbs in rats[3]. Bromfenac (0.32%; 50 μL; rubbed onto the abdomen) produces significant blockade of abdominal constriction to ACh challenge in mice[3]. Bromfenac (eyedrop instillation; 1 μL (0.09%) per eye; twice-daily; 4 w) partially reduces corneal staining, and becomes so more slowly by the 4-week time point[4].

IC50 & Target：Human COX-1 5.56 nM (IC50) Human COX-2 7.45 nM (IC50)

References：

[1]. Tetsuo Kida, et al. Pharmacokinetics and efficacy of topically applied nonsteroidal anti-inflammatory drugs in retinochoroidal tissues in rabbits. PLoS One. 2014 May 5;9(5):e96481. [Content Brief]

[2]. Xiaobo Zhang, et al. Drug-eluting intraocular lens with sustained bromfenac release for conquering posterior capsular opacification. Bioact Mater. 2021 Jul 23;9:343-357. [Content Brief]

[3]. Nolan JC, et, al. The topical anti-inflammatory and analgesic properties of bromfenac in rodents. Agents Actions. 1988 Aug; 25(1-2): 77-85. [Content Brief]

[4]. Kaevalin Lekhanont, et al. Effects of topical anti-inflammatory agents in a botulinum toxin B-induced mouse model of keratoconjunctivitis sicca. J Ocul Pharmacol Ther. 2007 Feb;23(1):27-34. [Content Brief]

Brand introduction:
•   MCE (MedChemExpress) has a global exclusive compound library of more than 200 kinds, and we are committed to providing the most comprehensive range of high-quality small molecule active compounds for scientific research customers around the world；
•   More than 50,000 highly selective inhibitors and agonists are involved in various popular signaling pathways and disease areas；
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•   Provide virtual screening, ion channel screening, metabolomics analysis detection analysis, drug screening and other professional technical services；
•   It has a professional experimental center and strict quality control and verification system；
•   Provide LC/MS, NMR, HPLC, chiral analysis, elemental analysis and other quality inspection reports to ensure the high purity and high quality of products；
•   The biological activity of the products has been verified by the experiments of customers in various countries；
•   A variety of top journals such as Nature, Cell, Science and pharmaceutical patents have included the scientific research results of MCE customers；
•   Our professional team tracks the latest pharmaceutical and life science research and provides you with the latest active compounds in the world；
•   It has established long-term cooperation with the world's major pharmaceutical companies and well-known scientific research institutions。