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CI-988
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。
CI-988图片
CAS NO:130332-27-3
包装与价格:
包装价格(元)
100mg电议
250mg电议
500mg电议

产品名称
PD134308
产品介绍
CI-988 (PD134308) 是一种有效、选择性和具有口服活性的CCK2R(胆囊收缩素 2 受体)拮抗剂,对小鼠皮质 CCK2 的IC50为 1.7 nM。CI-988 对 CCK2 的选择性超过 CCK1 受体的 1600 倍。CI-988 具有抗焦虑和抗肿瘤作用。
生物活性

CI-988 (PD134308) is a potent, selective and orally activeCCK2R (cholecystokinin 2 receptor)antagonist with anIC50of 1.7 nM for mouse cortex CCK2. CI-988 shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 has anxiolytic and anti-tumor effects[1][2][3].

IC50& Target

IC50: 1.7 nM (Mouse cortex CCK2); 2717 nM (Rat pancreas CCK1)[2]

体外研究
(In Vitro)

CI-988 inhibits specific125I-BH-CCK-8 binding to NCI-H727 cells with high affinity (Kiof 4.5 nM). The increase in ROS caused by CCK-8 addition to NCI-727 cells is blocked significantly by CI-988. CI-988 (3 μM) inhibits the basal growth of NCI-H727 cells or that stimulated by CCK-8. CI-988 inhibits the ability of CCK-8 to cause ERK phosphorylation and elevate cytosolic Ca2+[1].
CI-988 inhibits in a dose-dependent manner the ability of CCK-8 to cause EGFR transactivation in NCI-H727 cells. CI-988 at doses of 1 and 10 μM weakly and strongly, respectively, inhibits the ability of 0.1μM CCK-8 to increase EGFR tyrosine phosphorylation. CI-988 antagonizes the ability of CCK-8 to cause lung cancer EGFR or ERK tyrosine phosphorylation[1].

体内研究
(In Vivo)

CI-988 (10 mg/kg; p.o.; daily; for 20 days) inhibits the growth of colorectal cancer in xenografts model mice[3].

Animal Model:Nude mice injected with LoVo cells[3]
Dosage:10 mg/kg
Administration:p.o.; daily; for 20 days
Result:Inhibited the growth of xenografts by 53%.
分子量

614.73

Formula

C35H42N4O6

CAS 号

130332-27-3

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.