ONO-8711 dicyclohexylamine

立即咨询

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。

ONO-8711 dicyclohexylamine 是一种有效的选择性竞争性EP1拮抗剂，对人和小鼠 EP1 的K_i值分别为 0.6 nM 和 1.7 nM。ONO-8711 dicyclohexylamine 有效降低结肠癌、乳腺癌和口腔癌小鼠模型的肿瘤发生率。

生物活性

ONO-8711 dicyclohexylamine is a selective and orally activeEP1competitive antagonist withK_ivalue of 0.6 nM and 1.7 nM for human and mouse EP1 respectively. ONO-8711 dicyclohexylamine effectively reduces tumor incidence and multiplicity in mouse models of colon, breast, and oralcancer^[1].

IC₅₀& Target

K_i: 0.6 nM (human EP1), 1.7 nM (mouse EP1)^[1]

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

621.31

性状

Solid

Formula

C₃₄H₅₃ClN₂O₄S

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 50 mg/mL(80.48 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	1.6095 mL	8.0475 mL	16.0950 mL
5 mM	0.3219 mL	1.6095 mL	3.2190 mL
10 mM	0.1610 mL	0.8048 mL	1.6095 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month (sealed storage, away from moisture)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。