Pentagastrin | CAS 5534-95-2 | CCK-B Receptor Agonist (Research Use Only) | Knowlux

Product Description

Pentagastrin, CAS 5534-95-2, is a synthetic pentapeptide analogue of the C-terminal active fragment of gastrin, supplied by Knowlux for laboratory research use. The sequence is Boc-beta-Ala-Trp-Met-Asp-Phe-NH2, with a tert-butoxycarbonyl (Boc) protecting group on the N-terminal beta-alanine and an amidated C-terminal phenylalanine. The molecular formula is C37H49N7O9S and the molecular weight is 767.89 g/mol. Each lot is released with a lot-specific COA, MSDS and analytical traceability.

Molecular Formula Verification Note: The formula C37H49N7O9S and molecular weight 767.89 are confirmed by ChemicalBook, Sigma-Aldrich, MedChemExpress, NCATS Inxight, HMDB, and PeptideDB. Several supplier listings (Santa Cruz Biotechnology, Biorbyt) show the formula as C37H50N7O9S with a molecular weight of 768.79. This discrepancy arises from a hydrogen count difference (H49 versus H50) and likely reflects a salt form or a rounding convention rather than the free peptide. The C37H49N7O9S / 767.89 value is adopted throughout this specification as the consensus free-peptide assignment. Buyers should verify the formula on the lot-specific COA against the declared salt basis.

Structural Note: The Boc group on the N-terminal beta-alanine protects the peptide from aminopeptidase degradation and is a defining feature relative to the endogenous gastrin fragment. The C-terminal phenylalaninamide is amidated, blocking carboxypeptidase attack. Pentagastrin contains a methionine residue (Met3), introducing a thioether side chain susceptible to oxidation. Unlike the cyclic, disulfide-constrained peptides in the Linaclotide and Eptifibatide families, Pentagastrin is linear and unprotected at the C-terminus aside from the amide.

Product Parameters

Item	Specification
Product Name	Pentagastrin
Synonyms	ICI-50123; AY-6608; Peptavlon; Boc-beta-Ala-Trp-Met-Asp-Phe-NH2
CAS No.	5534-95-2
Related CAS	57448-84-7 (Pentagastrin meglumine)
Molecular Formula	C37H49N7O9S
Molecular Weight	767.89 g/mol
Sequence (3-letter)	Boc-beta-Ala-Trp-Met-Asp-Phe-NH2
Sequence Length	5 residues, linear
Key Structural Features	Boc-protected N-terminal beta-alanine; Met3 thioether; C-terminal Phe-NH2
Appearance	White to off-white powder or colorless needles
Solubility	Insoluble in water; soluble in 5M ammonia and DMF; slightly soluble in ethanol; DMSO >=34 mg/mL
Purity	>=95.0% (HPLC); >=98.0% / >=99.0% available on request
Identity	Confirmed by LC-MS
Grade	Research grade
Counter-ion	Not applicable (free peptide); meglumine salt available under CAS 57448-84-7
Peptide Content	>=75.0% to >=80.0% (supplier-dependent)
Water Content	<=8.0% (Karl Fischer)
Storage	-20C, desiccated, protected from light; short-term 2C to 8C acceptable
Packaging	1 mg / 5 mg / 10 mg / 50 mg / 100 mg vial; bulk on request
Application	Laboratory research use only
Origin	China

Product Details

1. Overview

Pentagastrin is a synthetic pentapeptide that reproduces the biological actions of gastrin at the C-terminal pentapeptide region, the minimal sequence required for full gastrin-like activity. It acts as a potent and selective agonist at the cholecystokinin type B (CCK-B) receptor, with an EC50 of approximately 11 nM. Selectivity for CCK-B over CCK-A exceeds 1000-fold, making Pentagastrin a standard pharmacological tool for discriminating between these receptor subtypes in binding and functional assays. In clinical diagnostics, Pentagastrin has been used as a stimulant in gastric acid secretion testing and carcinoid provocation protocols. The material supplied under this specification is research-grade and is not intended for human administration. Knowlux supplies this compound strictly for laboratory investigation of CCK-B receptor pharmacology, gastric mucosal biology, and neuroendocrine signaling.

2. Receptor Pharmacology

Pentagastrin binds CCK-B receptors with high selectivity. In GH3 pituitary cell membranes, competition curves yielded an IC50 of 25 nM for Pentagastrin, compared with 2.4 nM for the non-selective agonist CCK-8s. Functional studies in the same cell line reported an IC50 of 45 nM for Pentagastrin-stimulated polyphosphoinositide turnover. MedChemExpress lists an EC50 of 11 nM for CCK-B receptor activation. These values are assay- and system-dependent and are provided for scientific reference only. Pentagastrin also stimulates gastric mucosal DNA synthesis and enhances gastric mucosal defense mechanisms against acid-induced injury in preclinical models.

3. Research Applications

Published pharmacological characterizations describe the following research applications:

• CCK-B receptor binding and functional assays (selectivity discrimination versus CCK-A)

• Gastric acid secretion and parietal cell function studies

• Gastric mucosal defense and cytoprotection research models

• Neuroendocrine tumor (carcinoid, gastrinoma) provocation and signaling studies

• Reference standard development for HPLC and LC-MS analytical methods

These descriptions are derived from published research and are provided for scientific reference only. They do not constitute clinical guidance or dosing recommendations.

Quality Control

Test Item	Method	Acceptance Criteria
Purity	RP-HPLC	>=95.0% (>=98.0% / >=99.0% available)
Identity & Molecular Mass	LC-MS (deconvoluted)	Consistent with structure
Single Impurity	RP-HPLC	<=1.0% to <=2.0% (grade-dependent)
Peptide Content	Amino Acid Analysis or Nitrogen	>=75.0% to >=80.0%
Water Content	Karl Fischer	<=8.0%
Appearance	Visual	White to off-white powder
Specific Rotation	Polarimetry, DMF	-25 to -30 degrees (20C, 0.5-2.0 mg/mL)

Supplier specifications for Pentagastrin vary by grade and supplier. Aladdin lists >=95% HPLC purity. A Watson Biotechnology COA reports peptide purity of 98.1%, total impurities of 1.9%, largest single impurity of 0.7%, and water content of 7.3%. ChemScene lists 99.97% purity for its catalog item, and Adamas reports 98.98% purity for a tested lot. Peptide content specifications range from >=75.0% to >=80.0% depending on the supplier. The British Pharmacopoeia reference standard specification includes a specific rotation acceptance range of -25 to -30 degrees (20C, DMF), providing an orthogonal identity check beyond HPLC and MS. Buyers should request lot-specific HPLC chromatograms, mass spectra, and specific rotation data where chiral integrity is critical. Full COA, MSDS, and lot-specific chromatograms are issued with each shipment.

Solubility and Handling

Solubility: Pentagastrin is practically insoluble in water, a property that distinguishes it from the hydrophilic peptides in the Semax and Epitalon families. It is soluble in 5M ammonia and in dimethylformamide (DMF), and slightly soluble in ethanol (96%). Merck and Krackeler list DMF solubility of 20 mg/mL, yielding a clear, colorless to faint yellow or tan solution. InvivoChem reports DMSO solubility of >=34 mg/mL (approximately 44.28 mM) and water solubility of <0.1 mg/mL. For in vivo formulation studies, InvivoChem describes a vehicle of 10% DMSO + 40% PEG300 + 5% Tween80 + 45% saline achieving >=2.08 mg/mL (2.71 mM) with a clear solution. Given the low aqueous solubility, DMSO or DMF stock solutions are recommended, with dilution into aqueous buffer immediately before use. Prepare solutions fresh and aliquot to avoid repeated freeze-thaw cycles.

Handling Precautions: Use powder-handling containment (glove box or fume hood with particulate control). Avoid inhalation of fine powder. ChemicalBook assigns GHS07 (warning, H302+H312+H332), indicating harmful if swallowed, in contact with skin, or if inhaled. Wear nitrile gloves, lab coat, and eye protection. The methionine thioether is susceptible to oxidation; handle under inert atmosphere where practical. Follow institutional chemical hygiene plans for research peptides.

Storage and Stability

Format	Temperature	Shelf Life
Lyophilized Powder	-20C, sealed, desiccated, protected from light	3 years
Lyophilized Powder	4C, sealed, desiccated	2 years
Lyophilized Powder	2C to 8C, sealed, desiccated	Acceptable short-term (one supplier lists 4C, 3-year validity)
Reconstituted Solution	-80C, aliquoted	6 months
Reconstituted Solution	-20C, aliquoted	1 month

Storage guidance varies by supplier: InvivoChem specifies 3 years at -20C and 2 years at 4C for powder, with 6 months at -80C or 1 month at -20C for solutions. One Chinese supplier lists 2C to 8C storage with a 3-year validity when kept at 4C. Aladdin specifies -20C with protection from light. Shipping is typically at ambient temperature, as InvivoChem notes the product is stable at ambient for a few days during ordinary shipping. The lyophilized powder is hygroscopic; equilibrate vials to room temperature before opening to prevent condensation. Protect from light and moisture.

Documentation Support

Per lot: COA, MSDS, certificate of origin, HPLC chromatogram, and mass spectrometry data. Specific rotation data and sequence verification available on request. Custom specifications and third-party inspection can be arranged on a project basis.

About Knowlux

Knowlux Biotechnology is a GMP-oriented manufacturer and supplier of peptides, APIs and fine-chemical research compounds, operating from Hubei, China. We serve research groups, CDMOs and distributors in more than 40 countries, and support contract synthesis, custom packaging and technical documentation requests.

Compliance Statement

FOR RESEARCH USE ONLY. NOT FOR HUMAN USE. NOT FOR DIAGNOSTIC OR THERAPEUTIC USE.

This product is supplied for laboratory research use only. It is not for human or animal administration, not for diagnostic or therapeutic use, not for retail sale, and not for personal use. Pentagastrin has been used historically as a diagnostic agent in certain jurisdictions; however, the material offered under this specification is research-grade and is not intended for clinical use. The purchaser is responsible for verifying product specifications against their specific research requirements and for compliance with all applicable institutional, local, and national regulations governing research chemical acquisition, storage, and use. Research context statements are for scientific reference only and do not constitute medical advice, promotional claims, or dosing guidance.

Data Verification Notes: The molecular formula C37H49N7O9S and molecular weight 767.89 g/mol are confirmed by ChemicalBook, Sigma-Aldrich, MedChemExpress, NCATS Inxight, HMDB, and PeptideDB. Santa Cruz Biotechnology and Biorbyt list C37H50N7O9S with MW 768.79; this hydrogen-count discrepancy is noted and the C37H49N7O9S / 767.89 assignment is adopted as the consensus free-peptide value. The sequence Boc-beta-Ala-Trp-Met-Asp-Phe-NH2 is confirmed across ChemicalBook, Sigma-Aldrich, Santa Cruz, and InvivoChem. The CCK-B selectivity data (>1000-fold over CCK-A) and the IC50/EC50 values (25 nM, 45 nM, 11 nM) are from published pharmacological sources and are assay-dependent. Solubility values for water, ammonia, DMF, and DMSO are reported with their respective source conditions. One ChemicalBook listing describes Pentagastrin as soluble in dilute ammonia solution while also stating insoluble in water, which is consistent given the pH-dependent ionization behavior of the peptide.

Formatting Note: All formulas, sequences, and comparison operators use plain ASCII notation to prevent character corruption on the platform. Beta-alanine is rendered as "beta-Ala" rather than the Greek beta symbol to eliminate non-ASCII character risk. Section headings, table alignment, and spacing follow the approved product detail pattern. No trailing spaces or non-breaking characters are used; tables use consistent pipe alignment.