Gastrin-1, rat CAS NO.81123-06-0

Gastrin-1, rat (CAS NO. 81123-06-0) is an 18-amino-acid neuropeptide with the molecular formula C₉₄H₁₂₈N₂₂O₃₁S₂ and molecular weight 2126.32 g/mol. As a species-specific regulator of gastrointestinal function in rats, it is widely used to study gastric acid secretion, gastrin receptor pharmacology, and preclinical drug development.

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TECHNICAL SPECIFICATIONS

Item	Specification
Product Name	Gastrin-1, rat
CAS NO.	81123-06-0
Appearance	White to off-white lyophilized powder
Molecular Formula	C₉₄H₁₂₈N₂₂O₃₁S₂
Molecular Weight	2126.32 g/mol
Purity (RP-HPLC)	≥ 98.0%
Solubility	Soluble in water (pH 4.0–7.0) or 0.1 M acetic acid; slightly soluble in DMSO (≤5 mg/mL)
Endotoxin	< 1.0 EU/mg
Biological Activity	Binds to cholecystokinin-2 (CCK₂) receptor with high affinity (rat CCK₂ receptor Ki: ~0.1–1 nM), stimulating gastric acid secretion, gastrin release, and growth of gastric mucosa. Species-specific for rat models, critical for studying gastrointestinal physiology and drug development.
Storage Conditions	Lyophilized powder: Store at -20°C in a desiccated, light-protected container; avoid repeated freeze-thaw cycles. After reconstitution, aliquot and store at -80°C (stable for 6 months) or 2–8°C (stable for 1 week).
Stock Location	Stock in USA
MOQ	1g

1.MECHANISM OF ACTION

CCK₂ Receptor Activation: Binds to the cholecystokinin-2 (CCK₂) receptor (rat-specific, Ki: 0.1–1 nM), triggering Gq/11 protein-coupled signaling cascades.

Gastric Acid Secretion: Stimulates enterochromaffin-like (ECL) cells in the stomach to release histamine, which induces gastrin secretion from G cells, ultimately increasing gastric acid production.

Mucosal Growth: Promotes proliferation of gastric mucosal cells via CCK₂ receptor-mediated MAPK/ERK pathway activation, supporting tissue repair and regeneration.

2.PRODUCT INDICATIONS

Gastrointestinal Research: Studying gastric acid regulation, peptic ulcer disease, and gastroesophageal reflux disorder (GERD) in rat models.

Pharmacology Studies: Evaluating CCK₂ receptor antagonists (e.g., proton pump inhibitors, H₂ blockers) and agonists for acid suppression or mucosal protection.

Preclinical Drug Development: Testing the efficacy and safety of anti-ulcer drugs, gastric stimulants, or CCK₂-targeted therapies in rat models.

3.CLINICAL EFFICACY OF PRODUCT

Preclinical Validation:

Increases gastric acid output by 50–70% in pylorus-ligated rat models (ED₅₀: 0.3 nM).

Stimulates gastrin release from isolated rat G cells by 4–6x (concentration: 1 nM).

Promotes gastric mucosal cell proliferation (2–3x increase in BrdU incorporation) in rat explant cultures.

Therapeutic Relevance: CCK₂ receptor antagonists derived from Gastrin-1, rat are in clinical trials for acid-related disorders, with this peptide serving as a key reference standard.

4.DELIVERY & SHIPPING

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