货号:A459112
同义名:
ICI-50123; AY 6608
Pentagastrin是选择性胆囊收缩素B(CCKB)受体拮抗剂,IC50为11 nM。Pentagastrin是一种合成的多肽,在给药后可引起与胃泌素类似的效应,能够促进唾液蛋白的分泌和合成。
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描述 | Pentagastrin (ICI-50123) is identified as a potent, selective antagonist of the Cholecystokinin B (CCKB) receptor, with IC50 values of 11 nM for CCKB and 1100 nM for CCKA receptors. It plays a significant role in enhancing gastric mucosal defense mechanisms against acid and provides protection to the gastric mucosa from experimental damage[1].[2]. |
体内研究 | In vivo experiments with male Sprague-Dawley rats demonstrate that Pentagastrin (administered intravenously at 80 µg/kg/h) effectively protects gastric mucosa from injuries caused by acidified aspirin[2]. |
体外研究 | In vitro studies involving GH3 cells have shown that Pentagastrin increases intracellular calcium levels in a dose-dependent manner, with the maximum increase observed being approximately 2.77-fold at concentrations ranging from 0.1 to 100 μM[1]. Additionally, Pentagastrin demonstrates dose-dependent binding to GH3 cells within the same concentration range[1]. |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT01699113 | Hypergastrinaemia | Phase 1 | Completed | - | United Kingdom ... 展开 >> Hammersmith Medicines Research London, United Kingdom 收起 << |
NCT00625495 | Gastroesophageal Reflux Diseas... 展开 >>e 收起 << | Phase 4 | Completed | - | - |
NCT00001229 | - | Completed | - | United States, Maryland ... 展开 >> National Heart, Lung and Blood Institute (NHLBI) Bethesda, Maryland, United States, 20892 收起 << | |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
1.30mL 0.26mL 0.13mL |
6.51mL 1.30mL 0.65mL |
13.02mL 2.60mL 1.30mL |
CAS号 | 5534-95-2 |
分子式 | C37H49N7O9S |
分子量 | 767.89 |
SMILES Code | O=C(N[C@@H](CCSC)C(N[C@@H](CC(O)=O)C(N[C@H](C(N)=O)CC1=CC=CC=C1)=O)=O)[C@@H](NC(CCNC(OC(C)(C)C)=O)=O)CC2=CNC3=C2C=CC=C3 |
MDL No. | MFCD00076515 |
别名 | ICI-50123; AY 6608; Petogasrin; Peptavlon; Pentagastrinum; ICI-50123 |
运输 | 蓝冰 |
存储条件 |
In solvent -20°C:3-6个月-80°C:12个月 Pure form Keep in dark place, sealed in dry, store in freezer, under -20°C |
溶解方案 |
DMSO: 35 mg/mL(45.58 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂: ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
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