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| | DUP-697 Basic information |
| Product Name: | DUP-697 | | Synonyms: | DUP-697;5-BROMO-2-(4-FLUOROPHENYL)-3-(4-(METHYLSULFONYL)PHENYL)THIOPHENE;BFMeT;DuP-697 Assay Reagent;Thiophene, 5-bromo-2-(4-fluorophenyl)-3-[4-(methylsulfonyl)phenyl]-;DuP697,DuP 697;DuP-697, 10 mM in DMSO | | CAS: | 88149-94-4 | | MF: | C17H12BrFO2S2 | | MW: | 411.31 | | EINECS: | | | Product Categories: | Lipid signaling;API intermediates | | Mol File: | 88149-94-4.mol |  |
| | DUP-697 Chemical Properties |
| storage temp. | 2-8°C | | solubility | DMF: 54 mg/ml; DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml; DMSO: 15 mg/ml; Ethanol: 7 mg/ml | | form | White to off-white solid. | | color | White to off-white |
| | DUP-697 Usage And Synthesis |
| Description | DuP-697 is a member of the diaryl heterocycle group of selective COX-2 inhibitors which includes MK-966 (rofecoxib), SC-58125, and celecoxib. DuP-697 is a potent and time-dependent inhibitor of COX-2. When tested on isolated recombinant enzymes, DuP-697 is at least 50 times more potent in the inhibition of COX-2 than COX-1. The IC50 values for human recombinant COX-2 are 80 and 40 nM at 5 and 10 minutes, respectively. The IC50 for the inhibition of human recombinant COX-1 after the same time intervals is 9 μM. DuP-697 also attenuates the COX-1 inhibitory activity of non-selective COX inhibitors such as indomethacin. | | Uses | DuP-697 is a thiophene that inhibits COX-2 and acts as a NSAID. | | Definition | ChEBI: DuP 697 is a member of thiophenes. | | Biological Activity | Potent and selective inhibitor of cyclooxygenase-2 (IC 50 values are 10 and 800 nM for COX-2 and COX-1 respectively). Inhibits prostaglandin synthesis and is anti-inflammatory in vivo . Orally active. | | storage | Store at +4°C | | References | [1] STACIA KARGMAN. Mechanism of selective inhibition of human prostaglandin G/H synthase-1 and -2 in intact cells[J]. Biochemical pharmacology, 1996, 52 7: Pages 1113-1125. DOI: 10.1016/0006-2952(96)00462-5
[2] K SEIBERT. Pharmacological manipulation of cyclo-oxygenase-2 in the inflamed hydronephrotic kidney.[J]. British Journal of Pharmacology, 1996, 117 6: 1016-1020. DOI: 10.1111/j.1476-5381.1996.tb16691.x
[3] MOTI ROSENSTOCK Gilad R Abraham Danon. PGHS-2 inhibitors, NS-398 and DuP-697, attenuate the inhibition of PGHS-1 by aspirin and indomethacin without altering its activity[J]. Biochimica et biophysica acta. Molecular and cell biology of lipids, 1999, 1440 1: Pages 127-137. DOI: 10.1016/s1388-1981(99)00105-5 |
| | DUP-697 Preparation Products And Raw materials |
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