Gastrin I (human)
(Synonyms: 胃膜素) 目录号 : GC15133
Gastrin I (human) 是存在于胃内的内源性肽，作用于缩胆囊素受体2，促进胃酸分泌。
Cas No.:10047-33-3
Sample solution is provided at 25 µL, 10mM.
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Gastrin I (human) is an endogenous peptide present in the stomach, which acts on cholecystokinin 2 receptor to promote gastric acid secretion[1]. Gastrin I (human) plays important role in stimulating the initiation and development of many gastrointestinal diseases[2]. Gastrin I (human) induces parathyroid hormone-like hormone expression in gastric parietal cells[3].
Gastrin I (human) (25μM; 15, 30, 45min) stimulates trypsin and chymotrypsin secretion from yellowtail pyloric caeca/pancreatic cell[4]. Gastrin I (human) (10 or 100nmol/l; 48h) enhances transcription of genes involved in islet cell function and identity in donors with higher HbA1c (>42 mmol/mol)[5].
Gastrin I (human) (20μg/kg; i.p. ; 24h and 40min) improved renal function and alleviates pathological damage after renal ischemic/reperfusion injury of mice model[6]. Gastrin I (human) (15nmol/kg; i.v. ; 20min) and Cholecystokinin-8S (CCK-8S (15nmol/kg; i.v. ; 20min)) significantly increased the release of NO breakdown products into the rat gastric lumen[7].
References:
[1] NOBLE F, WANK S A, CRAWLEY J N, et al. International Union of Pharmacology. XXI. Structure, distribution, and functions of cholecystokinin receptors [J]. Pharmacological reviews, 1999, 51(4): 745-81.
[2] YANG K, JIN H, GAO X, et al. Elucidating the molecular determinants in the process of gastrin C-terminal pentapeptide amide end activating cholecystokinin 2 receptor by Gaussian accelerated molecular dynamics simulations [J]. Front Pharmacol, 2022, 13(1054575.
[3] AL MENHALI A, KEELEY T M, DEMITRACK E S, et al. Gastrin induces parathyroid hormone-like hormone expression in gastric parietal cells [J]. Am J Physiol Gastrointest Liver Physiol, 2017, 312(6): G649-G57.
[4] KOFUJI P Y, MURASHITA K, HOSOKAWA H, et al. Effects of exogenous cholecystokinin and gastrin on the secretion of trypsin and chymotrypsin from yellowtail (Seriola quinqueradiata) isolated pyloric caeca [J]. Comp Biochem Physiol A Mol Integr Physiol, 2007, 146(1): 124-30.
[5] IRWIN N, LENZ A, LENZ G, et al. Islets from human donors with higher but not lower hemoglobin A1c levels respond to gastrin treatment in vitro [J]. Plos One, 2019, 14(8):
[6] LIU C, CHEN K, WANG H, et al. Gastrin Attenuates Renal Ischemia/Reperfusion Injury by a PI3K/Akt/Bad-Mediated Anti-apoptosis Signaling [J]. Front Pharmacol, 2020, 11(540479.
[7] BLANDIZZI C, LAZZERI G, COLUCCI R, et al. CCK1 and CCK2 receptors regulate gastric pepsinogen secretion [J]. Eur J Pharmacol, 1999, 373(1): 71-84.
Gastrin I (human) 是存在于胃内的内源性肽，作用于缩胆囊素受体2，促进胃酸分泌[1]。Gastrin I (human) 在刺激许多胃肠道疾病的发生和进展中起着重要作用[2]。Gastrin I (human) 诱导胃壁细胞中甲状旁腺激素样激素表达[3]。
Gastrin I (human)（25μM; 15, 30, 45min）刺激黄尾鱼幽门盲肠/胰腺细胞胰蛋白酶和凝乳胰蛋白酶的分泌[4]。Gastrin I (human)（10 or 100nmol; 48h）在HbA1c（>42 mmol/mol）较高浓度的胰岛供体中增强与胰岛细胞功能和身份相关的基因转录[5]。
使用Gastrin I (human)（20μg/kg; i.p. ; 24h and 40min）处理小鼠肾缺血/再灌注模型，Gastrin I (human)可减轻小鼠的肾病理损伤[6]。使用Gastrin I (human)（15nmol/kg; i.v. ; 20min）和CCK-8S（Cholecystokinin-8S，胆囊收缩素8S (15nmol/kg; i.v. ; 20min)）处理大鼠，Gastrin I (human) 显著增加了大鼠胃腔内NO代谢产物的释放[7]。
| Cell experiment [1]: | |
Cell lines | Human islets cells |
Preparation Method | The study was done on human islets approved for research use by the City of Hope Institutional Review Board and with the written informed consent from each organ donor family. Donor characteristics were categorized by the donor’s HbA1c level as either higher HbA1c (>42mmol/mol (6.0%)). |
Reaction Conditions | 10 or 100nmol/l; 48h |
Applications | Gastrin I (human) enhances transcription of genes involved in islet cell function and identity in donors with higher HbA1c. |
| Animal experiment [2]: | |
Animal models | Adult male C57/BL6 mice |
Preparation Method | Mice were anesthetized via intraperitoneal injection of sodium pentobarbital (60mg/kg) and placed on a heating pad to maintain body temperature at 37℃ during surgery. After clean of the surgical area, a midline laparotomy incision was performed and the right kidney was exposed. Then the right ureter, right renal artery and vein were all ligated before right nephrectomy. The left kidney was used for ischemia and reperfusion, the left renal artery was clamped by an artery clip for 40min. Gastrin I (human) (25μg/kg) was administrated via intraperitoneal injection to the left kidney before ischemia. |
Dosage form | 25μg/kg; 4 day; i.p. |
Applications | Gastrin I (human) improved renal function and alleviates pathological damage after renal ischemic/reperfusion injury of mice model. |
References: | |
| Cas No. | 10047-33-3 | SDF | |
| 别名 | 胃膜素 | ||
| 化学名 | (3S,4Z,6S,7Z,9S,10Z,13Z,15S,16Z,18S,19Z,21S,22Z,24S,25Z,27S,28Z,30S,31Z,33S)-9-((1H-indol-3-yl)methyl)-21,24,27,30-tetrakis(2-carboxyethyl)-5,8,11,14,17,20,23,26,29,32-decahydroxy-3-((Z)-hydroxy(((S)-1-hydroxy-1-imino-3-phenylpropan-2-yl)imino)methyl)-33- | ||
| Canonical SMILES | CC(C[C@@](/N=C(O)/[C@](/N=C(O)/[C@]1([H])CCCN1C(C/N=C(O)/[C@]2([H])CCC(O)=N2)=O)([H])CC3=CNC4=CC=CC=C34)([H])/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/C/C(O)=N/[C@@](/C(O)=N/[C@@](/C(O)=N/[C@ | ||
| 分子式 | C97H124N20O31S | 分子量 | 2098.22 |
| 溶解度 | 1% NH3 (Aqueous): 1 mg/ml,Formic Acid: 1 mg/ml | 储存条件 | -20°C, protect from light |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 0.4766 mL | 2.383 mL | 4.7659 mL |
| 5 mM | 0.0953 mL | 0.4766 mL | 0.9532 mL |
| 10 mM | 0.0477 mL | 0.2383 mL | 0.4766 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Quality Control & SDS
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- Purity: >99.50%
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