BAY-390 (C09-1113-680)

BAY-390 is a selective, across species active and brain penetrating TRPA1 inhibitor. BAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC 50 s of 16, 82, 63 and 35 nM, respectively. BAY-390 can be used for the research of inflammationIn VitroBAY-390 inhibits hTRPA1 FLIPR, hTRPA1 Ephys, rTRPA1 FLIPR and rDRG Ephys with IC 50 s of 16, 82, 63 and 35 nM, respectively. BAY-390 inhibits mTRPA1, gpTRPA1, dogTRPA1 and monkeyTRPA1 with IC 50 s of 73, 68, 81 and 19 nM, respectively. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoBAY-390 (30 and 90 mg/kg; p.o.; BID for 10 days) effects the neuropathic pain in vivo . BAY-390 reduces visceral pain in rat cyclophosphamide induced cystitis models . BAY-390 shows efficacy in inflammatory pain and neurogenic inflammation models . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Nrodent animals with neuropathic pain Dosage: 30 and 90 mg/kg Administration: Oral gavage; 30 and 90 mg/kg; twice daily for 10 days Result: Effectively reduced the neuropathic pain in rodent neuropathic pain model.Form:OilIC50& Target:IC50: 16 nM (hTRPA1 FLIPR), 82 nM (hTRPA1 Ephys), 63 nM (rTRPA1 FLIPR), 35 nM (rDRG Ephys), 73 nM (mTRPA1), 68 nM (gpTRPA1), 81 nM (dogTRPA1)m, 19 nM (monkeyTRPA1). Molecular Formula: C13H15F4NO Molecular Weight: 277.26