| Bioactivity | Zaltoprofen (CN100), a non-steroidal anti-inflammatory drug (NSAID), is a preferential and orally active COX-2 inhibitor, with IC50s of 1.3 and 0.34 μM for COX-1 and COX-2, respectively. Zaltoprofen exhibits powerful anti-inflammatory effects as well as an analgesic action on inflammatory pain[1][2][3]. | ||||||||||||
| Invitro | Zaltoprofen (0.1-10 μM; 15 min) inhibits thromboxane B2 production in human platelets in a dose-dependent manner[1].Zaltoprofen (0.01-1 μM; 30 min) inhibits prostaglandin E2 production by interleukin-1β-stimulated synovial cells[1].Zaltoprofen (0.1-1 μM; 5 min) inhibits the bradykinin-induced increase of [Ca2+]i in DRG cells[2]. | ||||||||||||
| In Vivo | Zaltoprofen (5-20 mg/kg; a single p.o.) inhibits bradykinin-induced nociceptive responses in rats[2].Zaltoprofen (3-30 mg/kg; a single p.o.) inhibits the acetic acid-induced writhing response of mice in a dose-dependent manner[2]. Animal Model: | ||||||||||||
| Name | Zaltoprofen | ||||||||||||
| CAS | 74711-43-6 | ||||||||||||
| Formula | C17H14O3S | ||||||||||||
| Molar Mass | 298.36 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Kawai S, et, al. Comparison of cyclooxygenase-1 and -2 inhibitory activities of various nonsteroidal anti-inflammatory drugs using human platelets and synovial cells. Eur J Pharmacol. 1998 Apr 17;347(1):87-94. [2]. Hirate K, et, al. Zaltoprofen, a non-steroidal anti-inflammatory drug, inhibits bradykinin-induced pain responses without blocking bradykinin receptors. Neurosci Res. 2006 Apr;54(4):288-94. [3]. Kameyama T, et, al. Analgesic and antiinflammatory effects of 2-(10,11-dihydro-10-oxo-dibenzo[b,f]thiepin-2-yl)propionic acid in rat and mouse. Arzneimittelforschung. 1987 Jan;37(1):19-26. |