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Tetragastrin

Alias: Cholecystokinin tetrapeptide; Gastrin tetrapeptide; Tetragastrin
Cat No.:V14581 Purity: ≥98%
Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin, which can stimulate gastric juice secretion.
Tetragastrin
Tetragastrin Chemical Structure CAS No.: 1947-37-1
Product category: New1
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
Other Sizes
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Product Description
Tetragastrin (Cholecystokinin tetrapeptide; CCK-4) is the C-terminal tetrapeptide of gastrin, which can stimulate gastric juice secretion. Tetragastrin is a cholecystokinin (CCK-4) receptor agonist (activator). Tetragastrin has gastric mucosal protection.
Biological Activity I Assay Protocols (From Reference)
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].
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].
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.
References

[1]. Effect of 6-hydroxydopamine on gastric carcinogenesis and tetragastrin inhibition of gastric carcinogenesis induced by N-methyl-N'-nitro-N-nitrosoguanidine in Wistar rats. Cancer Res. 1989 Aug 1;49(15):4199-203.

[2]. Pulmonary and systemic nitric oxide measurements during CCK-5-induced panic attacks. Neuropsychopharmacology. 2003 Oct;28(10):1840-5.

[3]. Effects of tetragastrin on mucus glycoprotein in rat gastric mucosal protection. Gastroenterol Jpn. 1992 Oct;27(5):597-603.

[4]. Tetragastrin activation of rat gastric mucosa adenyl cyclase in vitro. Biull Eksp Biol Med. 1981 Apr;91(4):440-1.

Additional Infomation
Tetragastrin is a tetrapeptide composed of L-tryptophan, L-methione, L-aspartic acid and L-phenylalaninamide residues joined in sequence. It has a role as an anxiogenic and a human metabolite. It is a tetrapeptide and a peptidyl amide.
Tetragastrin has been reported in Bos taurus with data available.
L-Tryptophyl-L-methionyl-L-aspartyl-L-phenylalaninamide. The C-terminal tetrapeptide of gastrin. It is the smallest peptide fragment of gastrin which has the same physiological and pharmacological activity as gastrin.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C29H36N6O6S
Molecular Weight
596.7
Exact Mass
730.278
CAS #
1947-37-1
PubChem CID
446569
Appearance
White to off-white solid powder
Density
1.341g/cm3
Boiling Point
1159.2ºC at 760mmHg
Flash Point
654.8ºC
Vapour Pressure
0mmHg at 25°C
Index of Refraction
1.643
LogP
4.679
Hydrogen Bond Donor Count
7
Hydrogen Bond Acceptor Count
8
Rotatable Bond Count
16
Heavy Atom Count
42
Complexity
948
Defined Atom Stereocenter Count
4
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
InChi Key
RGYLYUZOGHTBRF-BIHRQFPBSA-N
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
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
Synonyms
Cholecystokinin tetrapeptide; Gastrin tetrapeptide; Tetragastrin
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
DMSO : ~8.33 mg/mL (~13.96 mM)
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.

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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.
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 corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
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.

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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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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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