| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Tetragastrin targets the Cholecystokinin (CCK) receptor, specifically the CCK-4 subtype. It is an agonist at this receptor. By binding to and activating the CCK receptor, it stimulates gastric acid secretion. It also has a role as a human metabolite and can have anxiogenic effects.
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| ln Vitro |
Since cimetidine is an antagonist of histamine H2 receptors, it prevents histamine from stimulating cells in vitro and causes tetragastrin to stimulate adenylyl cyclase activity. In the stomach mucosa of rats, adenylyl cyclase is activated by histamine and tetragastrin via distinct receptors [4].
Tetragastrin stimulates the secretion of gastric acid and pepsinogen in vitro. This is its primary pharmacological activity, confirming its role as a gastrin receptor agonist. Its activity is comparable to that of the full-length gastrin hormone, as it is the smallest fragment with full activity. |
| ln Vivo |
The study found that inbred Wistar rats treated with N-methyl-N'-nitro-N-nitrosoguanidine, tetragastrin (sc; 1 mg/kg; every other day), and number had a much lower incidence of adenocarcinoma. Additionally, the labeling index in the gastric antral mucosa was significantly lower [1]. Tetragastrin may improve the protective effects of the gastric mucosa in rats by promoting mucus production and/or secretion at the mucosal surface. The superficial mucosal layer and mucus gel showed a substantial increase in mucin concentration. Tetragastrin treatment causes an increase in mucin in the surface mucosa and mucus gel [3].
Tetragastrin has been shown to have in vivo activity, stimulating gastric secretion. It is known for its gastric mucosal protective effects and is used to improve symptoms of hypochlorhydria or gastric atony, as well as in the treatment of atrophic gastritis. This confirms its clinical utility. |
| Enzyme Assay |
The in vitro activity of Tetragastrin is assessed by measuring its ability to stimulate acid secretion in isolated gastric glands or parietal cells. The compound is applied to these cells, and the production of acid is measured. This confirms its agonistic activity at the CCK receptor.
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| Cell Assay |
Tetragastrin's activity is also evaluated in cell-based assays using cells expressing the CCK receptor. Its ability to activate downstream signaling pathways, such as calcium mobilization, can be measured. This provides a functional readout of its receptor agonism.
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| Animal Protocol |
Animal/Disease Models: Sevenweeks old male Wistar rats, each weighing approximately 160 g[3]
Doses: 12, 120 or 400 μg/kg Route of Administration: subcutaneous injection; followed by gastric mucosal injury caused by 50% ethanol Experimental Results: It caused a significant increase in mucosal body mucin content and prevented gastric mucosal damage caused by 50% ethanol in a dose-dependent manner. Tetragastrin has been used in various animal models to study gastric function. In these studies, the compound is typically administered intravenously or subcutaneously, and its effects on gastric acid secretion, gastric emptying, and other gastrointestinal parameters are measured. It has also been used in clinical studies. |
| ADME/Pharmacokinetics |
Tetragastrin has a molecular weight of 596.7 and a molecular formula of C29H36N6O6S. Its sequence is WMDF-NH2. It is a tetrapeptide. It is the C-terminal tetrapeptide of gastrin and the smallest fragment with full gastrin activity. It is a synthetic peptide hormone.
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| Toxicity/Toxicokinetics |
Tetragastrin is a peptide hormone and its toxicity profile is not detailed in the provided sources. As a gastrin analog, it can stimulate acid secretion, and its use would be contraindicated in conditions where increased acid is harmful. Its anxiogenic effects are also noted. It is generally used in controlled settings for diagnostic or research purposes.
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| References |
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| Additional Infomation |
Tetragastrin-gastrin is a Tetragastrin composed of L-tryptophan, L-methionine, L-aspartic acid, and L-phenylalanine residues linked in sequence. It has anxiolytic effects and is a human metabolite. It is both a Tetragastrin and a peptide amide. Tetragastrin-gastrin has been reported to exist in bovine animals (Bos taurus), and relevant data are available. L-Tryptophanyl-L-methionyl-L-aspartic-L-phenylalanine is the C-terminal Tetragastrin of gastrin and also the smallest peptide fragment of gastrin, possessing the same physiological and pharmacological activities as gastrin.
Tetragastrin (CAS#: 1947-37-1) is a synthetic tetrapeptide that is the C-terminal fragment of gastrin, with the sequence WMDF-NH2. It acts as a Cholecystokinin (CCK-4) receptor agonist and stimulates gastric acid and pepsinogen secretion. It is the smallest peptide fragment of gastrin with full physiological activity. Tetragastrin is used in research and has clinical applications in gastrointestinal function testing. |
| Molecular Formula |
C29H36N6O6S
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|---|---|
| Molecular Weight |
596.7
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| Exact Mass |
730.278
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| CAS # |
1947-37-1
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| PubChem CID |
446569
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| Appearance |
White to off-white solid powder
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| Density |
1.341g/cm3
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| Boiling Point |
1159.2ºC at 760mmHg
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| Flash Point |
654.8ºC
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| Vapour Pressure |
0mmHg at 25°C
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| Index of Refraction |
1.643
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| LogP |
4.679
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
16
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| Heavy Atom Count |
42
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| Complexity |
948
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| Defined Atom Stereocenter Count |
4
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| SMILES |
CSCC[C@@H](C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N)NC(=O)[C@H](CC2=CNC3=CC=CC=C32)N
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| InChi Key |
RGYLYUZOGHTBRF-BIHRQFPBSA-N
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| InChi Code |
InChI=1S/C29H36N6O6S/c1-42-12-11-22(33-27(39)20(30)14-18-16-32-21-10-6-5-9-19(18)21)28(40)35-24(15-25(36)37)29(41)34-23(26(31)38)13-17-7-3-2-4-8-17/h2-10,16,20,22-24,32H,11-15,30H2,1H3,(H2,31,38)(H,33,39)(H,34,41)(H,35,40)(H,36,37)/t20-,22-,23-,24-/m0/s1
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| Chemical Name |
(3S)-3-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]-4-methylsulfanylbutanoyl]amino]-4-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-4-oxobutanoic acid
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| Synonyms |
Cholecystokinin tetrapeptide; Gastrin tetrapeptide; Tetragastrin
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~8.33 mg/mL (~13.96 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.19 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.19 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.19 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6759 mL | 8.3794 mL | 16.7588 mL | |
| 5 mM | 0.3352 mL | 1.6759 mL | 3.3518 mL | |
| 10 mM | 0.1676 mL | 0.8379 mL | 1.6759 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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