[Leu15]-Gastrin I (human) CAS NO.39024-57-2

[Leu15]-Gastrin I (human) is a synthetic analog of the human gastrin hormone, specifically characterized by the substitution of methionine at position 15 with leucine. This peptide is a 17-amino acid variant corresponding to the biologically active C-terminal fragment of gastrin. The methionine-to-leucine substitution enhances chemical stability by removing the oxidation-prone sulfur-containing amino acid, making it a more robust tool for experimental applications.

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TECHNICAL SPECIFICATIONS

Item	Specification
Product Name	[Leu¹⁵]-Gastrin I (human)
CAS NO.	39024-57-2
Appearance	White to off-white lyophilized powder
Molecular Formula	C98H126N20O31
Molecular Weight	2080.19g/mol
Purity (RP-HPLC)	≥ 95.0%
Solubility	Soluble in water (≥ 5 mg/mL), dilute acetic acid, and DMSO; forms a clear solution at 1 mg/mL in wate
Endotoxin	< 1.0 EU/mg
Biological Activity	Potent stimulator of gastric acid secretion, comparable to native gastrin I EC₅₀ ≤ 5 nM in parietal cell functional assays Resists degradation by serum enzymes longer than native gastrin.
Storage Conditions	Store at -20°C to -80°C in a desiccated, inert atmosphere Avoid repeated freeze-thaw cycles; aliquot into single-use portions
Stock Location	Stock in USA
MOQ	1g

1.MECHANISM OF ACTION

[Leu15]-Gastrin I functions as a potent agonist for the cholecystokinin B/gastrin receptor (CCK₂R). The peptide binds specifically to this G protein-coupled receptor located predominantly on gastric parietal cells and enterochromaffin-like (ECL) cells. Receptor activation triggers the Gq/11 signaling pathway, leading to phospholipase C (PLC) activation. This results in the production of inositol trisphosphate (IP₃) and diacylglycerol (DAG), which subsequently increase intracellular calcium levels and activate protein kinase C (PKC).

2.PRODUCT INDICATIONS

Gastrointestinal Physiology Studies: Investigating the mechanisms of gastric acid secretion, parietal cell function, and gastrin signaling pathways.

Receptor Pharmacology: Serving as a stable reference agonist in CCK₂ receptor binding assays, signal transduction studies, and drug screening.

Method Development: Utilized in the development and validation of in vitroassays for gastric function due to its enhanced chemical stability compared to native gastrin.

Comparative Studies: Comparing the biological activity and stability of modified versus native gastrin peptides.

Trophic Effect Research: Studying the role of gastrin in the growth and maintenance of gastrointestinal mucosa and certain tumor cells.

3.CLINICAL EFFICACY OF PRODUCT

Research Validation: In vitroand animal studies confirm that this analog retains the acid-stimulating potency of native human gastrin-I, making it a validated tool for physiological research.

Stability Advantage: The primary advantage over native gastrin is its resistance to oxidation, which improves reproducibility in long-term experiments and assay protocols.

Diagnostic/Therapeutic Gap: While the gastrin/CCK₂R pathway is clinically relevant (e.g., in diagnosing gastrinoma), this specific analog is not used in clinical diagnostics or therapy. Its role is confined to preclinical research.

Translational Relevance: Research using this stable analog contributes to the broader understanding of gastrin biology, which indirectly informs the development of clinical diagnostic tests (e.g., for Zollinger-Ellison syndrome) and therapeutic strategies targeting acid-related disorders.

4.DELIVERY & SHIPPING

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