ONO-8711

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ONO-8711

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

216158-34-8

ONO-8711 是一种有效且选择性的EP1 受体竞争性拮抗剂(对人和小鼠 EP1 的K_i分别为 0.6 和 1.7 nM)。ONO-8711 有效降低结肠癌、乳腺癌和口腔癌小鼠模型中的肿瘤发生率和多样性。

生物活性

ONO-8711 is a potent and selective competitive antagonist ofEP1 receptor(K_i= 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 oralcancer^[1].

IC₅₀& Target

体外研究
(In Vitro)

ONO-8711 (10 and 30 μM; 30 min) blocks the contractions induced by sulprostone in human pulmonary veins in a non-competitive manner^[2].
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^[3].

体内研究
(In Vivo)

ONO-8711 (400 or 800 p.p.m.; p.o.; for 20 weeks) suppresses cancer incidence and delays occurrence of breast tumors^[3].

Animal Model:	Female Sprague-Dawley rats (induced breast cancer by gavage of 85 mg/kgPhIP(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).

分子量

440.00

Formula

C₂₂H₃₀ClNO₄S

CAS 号

216158-34-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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