Pentagastrin (ICI-50123) 是胆囊收缩素 B (CCKB) 受体的选择性激动剂,IC50 为 11 nM。可增强胃粘膜对酸的防御机制,并保护胃粘膜免受损伤。
Pentagastrin Chemical Structure
CAS No. : 5534-95-2
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是否有货
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10 mM * 1 mL in DMSO
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生物活性
Pentagastrin (ICI-50123) is a selective agonist of Cholecystokinin B (CCKB) receptor with an IC50 of 11 nM[1]. Pentagastrin enhances gastric mucosal defence mechanisms against acid and protects the gastric mucosa from experimental injury[2].
IC50 & Target
IC50: 11 nM (CCKB receptor)[1]
体外研究 (In Vitro)
Cholecystokinin receptors on GH3 rat anterior pituitary cells have been characterised using radioligand binding and Ca2+ mobilisation. Competition curve with Pentagastrin (IC50 of 25 nM) is consistent with a population predominantly of CCKB receptors. The selective CCKB receptor agonist, Pentagastrin, (0.1 nM-100 μM) dose dependently increased intracellular Ca2+ with a maximal increase of 2.77-fold. Binding of 50 pM [125I]BHCCK to GH 3 cells is dose dependently inhibited by Pentagastrin IC50 of 45 nM. Response to a submaximal dose of the CCKB receptor agonist Pentagastrin (100 nM) was dose dependently blocked by the CCKB receptor antagonist L-365,260[1].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究 (In Vivo)
Pentagastrin (80 µg/kg/h; intravenous injection; male Sprague-Dawley rats) treatment protects rat gastric mucosa from acidified aspirin injury. Pentagastrin induces a hyperaemic response to luminal acid challenge, increases mucus gel thickness, and elevates intracellular pH (pHi) during acid challenge[2].
上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
Male Sprague-Dawley rats (approximately 200 g)[2]
Dosage:
80 µg/kg/h
Administration:
Intravenous injection
Result:
Protected rat gastric mucosa from acidified aspirin injury. Induced a hyperaemic response to luminal acid challenge, increased mucus gel thickness, and elevated pHi during acid challenge.
分子量
767.89
Formula
C37H49N7O9S
CAS 号
5534-95-2
中文名称
五肽胃泌素;五肽胃必素;五肽促胃液素
运输条件
Room temperature in continental US; may vary elsewhere.
[1]. Smith AJ, et al. Characterisation of CCKB receptors on GH3 pituitary cells: receptor activation is linked to Ca2+ mobilisation. Eur J Pharmacol. 1994 Apr 15;267(2):215-23.
[2]. Tanaka S, et al. Pentagastrin gastroprotection against acid is related to H2 receptor activation but not acid secretion. Gut. 1998 Sep;43(3):334-41.