2. GPCR/G Protein Neuronal Signaling
  3. Cholecystokinin Receptor
  4. CI-988 hemihydrate

CI-988 hemihydrate  (Synonyms: PD134308 hemihydrate)

目录号: HY-105226B
产品使用指南

摩尔计算器

CI-988 hemihydrate (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 hemihydrate 对 CCK2 的选择性超过 CCK1 受体的 1600 倍。CI-988 hemihydrate 具有抗焦虑和抗肿瘤作用。

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CI-988 hemihydrate Chemical Structure

CI-988 hemihydrate Chemical Structure

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Customer Review

Other Forms of CI-988 hemihydrate:

CI-988 hemihydrate 相关抗体

Top Publications Citing Use of Products

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CCKAR CCKBR

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CI-988 hemihydrate (PD134308) is a potent, selective and orally active CCK2R (cholecystokinin 2 receptor) antagonist with an IC50 of 1.7 nM for mouse cortex CCK2. CI-988 hemihydrate shows >1600-fold selectivity for CCK2 over CCK1 receptor. CI-988 hemihydrate has anxiolytic and anti-tumor effects[1][2][3].

体外研究
(In Vitro)

CI-988 inhibits specific 125I-BH-CCK-8 binding to NCI-H727 cells with high affinity (Ki of 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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

CI-988 hemihydrate 相关抗体:
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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

623.74

Formula

C35H42N4O6.1/2H2O
性状

固体

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
细胞实验： 

DMSO 中的溶解度 : ≥ 62.374 mg/mL (100.00 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.6032 mL 8.0162 mL 16.0323 mL
5 mM 0.3206 mL 1.6032 mL 3.2065 mL
查看完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

CI-988 hemihydrate 相关分类

完整储备液配制表

* 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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.6032 mL 8.0162 mL 16.0323 mL 40.0808 mL
5 mM 0.3206 mL 1.6032 mL 3.2065 mL 8.0162 mL
10 mM 0.1603 mL 0.8016 mL 1.6032 mL 4.0081 mL
15 mM 0.1069 mL 0.5344 mL 1.0688 mL 2.6721 mL
20 mM 0.0802 mL 0.4008 mL 0.8016 mL 2.0040 mL
25 mM 0.0641 mL 0.3206 mL 0.6413 mL 1.6032 mL
30 mM 0.0534 mL 0.2672 mL 0.5344 mL 1.3360 mL
40 mM 0.0401 mL 0.2004 mL 0.4008 mL 1.0020 mL
50 mM 0.0321 mL 0.1603 mL 0.3206 mL 0.8016 mL
60 mM 0.0267 mL 0.1336 mL 0.2672 mL 0.6680 mL
80 mM 0.0200 mL 0.1002 mL 0.2004 mL 0.5010 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

CI-988 hemihydratePD134308 hemihydrateCholecystokinin ReceptorCCK ReceptorCCK-8CCK2RERKEGFRphosphorylationCa2+anxiolyticanti-tumorInhibitorinhibitorinhibit

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