Gastrin I (human) (Synonyms: Gastrin I (1-17) (human), Gastrin Heptadecapeptide I (human)) |
| Katalog-Nr.GC15133 |
Selektiver CCK2-Rezeptor-Agonist
Products are for research use only. Not for human use. We do not sell to patients.
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.
| 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 | |
| Überlieferungen | Gastrin I (1-17) (human), Gastrin Heptadecapeptide I (human) | ||
| Chemical Name | (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@ | ||
| Formula | C97H124N20O31S | M.Wt | 2098.22 |
| Löslichkeit | 1% NH3 (Aqueous): 1 mg/ml,Formic Acid: 1 mg/ml | Storage | -20°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
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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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)
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