产品
编 号：F274291
分子式：C22H30ClNO4S
分子量：440
分子式：C22H30ClNO4S
分子量：440
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CAS No: 216158-34-8
产品详情
生物活性：
ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer.
体内研究：
ONO-8711 (400 or 800 p.p.m.; p.o.; for 20 weeks) suppresses cancer incidence and delays occurrence of breast tumors.Animal Model:Female Sprague-Dawley rats (induced breast cancer by gavage of 85 mg/kg PhIP (HY-118716) 4 times for 2 weeks)
Dosage:400 or 800 p.p.m.
Administration:p.o.; for 20 weeks
Result:Did not induce any symptoms of toxicity at 800 p.p.m..Delayed occurrence of breast tumors for 2 or 4 weeks at 400 or 800 p.p.m., respectively.Significantly suppressed cancer incidence compared with the control diet group at 800 p.p.m. (56% versus 79%, P < 0.05).
体外研究：
ONO-8711 (10 and 30 μM; 30 min) blocks the contractions induced by sulprostone in human pulmonary veins in a non-competitive manner.ONO-8711 inhibits PGE2-induced increase in cytosolic Ca2+ concentration with IC50s of 0.21 μM, 0.05 μM, and 0.22 μM for the mouse, human, and rat receptors, respectively.
ONO-8711 is a potent and selective competitive antagonist of EP1 receptor (Ki = 0.6 and 1.7 nM for human and mouse EP1 respectively). ONO-8711 effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oral cancer.
体内研究：
ONO-8711 (400 or 800 p.p.m.; p.o.; for 20 weeks) suppresses cancer incidence and delays occurrence of breast tumors.Animal Model:Female Sprague-Dawley rats (induced breast cancer by gavage of 85 mg/kg PhIP (HY-118716) 4 times for 2 weeks)
Dosage:400 or 800 p.p.m.
Administration:p.o.; for 20 weeks
Result:Did not induce any symptoms of toxicity at 800 p.p.m..Delayed occurrence of breast tumors for 2 or 4 weeks at 400 or 800 p.p.m., respectively.Significantly suppressed cancer incidence compared with the control diet group at 800 p.p.m. (56% versus 79%, P < 0.05).
体外研究：
ONO-8711 (10 and 30 μM; 30 min) blocks the contractions induced by sulprostone in human pulmonary veins in a non-competitive manner.ONO-8711 inhibits PGE2-induced increase in cytosolic Ca2+ concentration with IC50s of 0.21 μM, 0.05 μM, and 0.22 μM for the mouse, human, and rat receptors, respectively.
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