| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| 1g | |||
| Other Sizes |
| Targets |
The primary target of gastrin I is the cholecystokinin B receptor (CCKBR), also known as the gastrin receptor. Gastrin stimulates gastric acid secretion by binding to CCKBR on enterochromaffin-like (ECL) cells and parietal cells. The (1-14) fragment retains biological activity, with an EC₅₀ of 6.2 pM for gastrin receptor binding and 0.014 nM for histamine release from ECL cells.
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|---|---|
| ln Vitro |
In vitro, gastrin I (1-14), human binds to the gastrin receptor with an EC₅₀ of 6.2 pM. It stimulates histamine release from ECL cells with an EC₅₀ of 0.014 nM. The fragment is a cost-effective, validated alternative to full-length gastrin without compromising experimental sensitivity. Its activity has been characterized in various cell-based and receptor binding assays.
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| ln Vivo |
In vivo, gastrin I is the major hormonal regulator of gastric acid secretion. The (1-14) fragment retains the biological activity of full-length gastrin and can be used in animal studies to stimulate gastric acid secretion. The compound's effects on gastric physiology have been extensively studied in animal models.
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| Enzyme Assay |
For in vitro receptor binding assays, gastrin I (1-14), human is evaluated for its ability to bind to the cholecystokinin B receptor (CCKBR). Radiolabeled gastrin (e.g., ¹²⁵I-gastrin) is incubated with membrane preparations containing CCKBR and varying concentrations of the fragment. Bound and free ligand are separated by filtration. Binding affinity (Ki) is calculated from competition binding curves.
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| Cell Assay |
For in vitro cell-based assays, gastrin I (1-14), human is tested on ECL cells or other cells expressing CCKBR. Cells are treated with the fragment at various concentrations (typically 0.001 nM-1 µM). Histamine release is measured by ELISA or radioimmunoassay. Calcium mobilization or MAPK activation can be measured as additional readouts of receptor activation. EC₅₀ values are determined from dose-response curves.
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| Animal Protocol |
For in vivo animal experiments, gastrin I (1-14), human is typically administered intravenously or subcutaneously to rodents. The compound is given at doses ranging from 0.1-100 µg/kg. Gastric acid secretion is measured by gastric lavage or using a gastric fistula. Blood samples are collected to measure gastrin levels and other hormones. The compound's effects on gastric mucosal proliferation and histology can also be assessed.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for gastrin I (1-14), human are limited. As a peptide with a molecular weight of 1705.73 g/mol and formula C₇₉H₁₀₀N₁₆O₂₇, it is expected to have a short half-life due to rapid proteolytic degradation. The compound is typically administered via injection. Its pharmacokinetic profile is similar to other peptide hormones.
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| Toxicity/Toxicokinetics |
Toxicological data for gastrin I (1-14), human are limited. As a peptide fragment of an endogenous hormone, it is generally considered to have low toxicity at pharmacological doses. However, chronic administration of gastrin can lead to gastric mucosal hyperplasia or carcinoid tumors in animal models. The compound is classified as a research-grade reagent and is not for human therapeutic use.
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| References | |
| Additional Infomation |
Gastrin I (1-14), human is a research-use only compound and has not been approved for clinical applications. It is the 1-14 fragment of human gastrin I peptide. Its molecular weight is 1705.73, and its formula is C₇₉H₁₀₀N₁₆O₂₇. The compound is used in research on gastric acid secretion, gastrointestinal physiology, and the role of gastrin in health and disease. It is available from various research chemical suppliers.
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| Molecular Formula |
C79H100N16O27
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|---|---|
| Exact Mass |
1704.694
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| CAS # |
100940-57-6
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| Related CAS # |
Gastrin I (1-14), human TFA
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| PubChem CID |
146156206
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| Sequence |
{Glp}-Gly-Pro-Trp-Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp{Glp}-GPWLEEEEEAYGW
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| SequenceShortening |
{Glp}-GPWLEEEEEAYGW
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| Appearance |
White to off-white solid
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
2164.2±65.0 °C at 760 mmHg
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| Flash Point |
1262.7±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.625
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| LogP |
-1.8
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| Hydrogen Bond Donor Count |
22
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| Hydrogen Bond Acceptor Count |
27
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| Rotatable Bond Count |
49
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| Heavy Atom Count |
122
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| Complexity |
3790
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(C1CCCN1C(CNC(C1CCC(N1)=O)=O)=O)NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(C(NC(C)C(NC(C(NCC(NC(C(=O)O)CC1=CNC2C=CC=CC1=2)=O)=O)CC1C=CC(=CC=1)O)=O)=O)CCC(=O)O)=O)CCC(=O)O)=O)CCC(=O)O)=O)CCC(=O)O)=O)CCC(=O)O)=O)CC(C)C)=O)CC1=CNC2C=CC=CC1=2
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| InChi Key |
WRJJBRDFCLLYQF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C79H100N16O27/c1-39(2)31-55(93-77(119)57(33-42-35-80-47-11-6-4-9-45(42)47)94-78(120)59-13-8-30-95(59)62(99)38-83-69(111)49-18-24-60(97)85-49)76(118)91-54(23-29-67(108)109)75(117)90-53(22-28-66(106)107)74(116)89-52(21-27-65(104)105)73(115)88-51(20-26-64(102)103)72(114)87-50(19-25-63(100)101)71(113)84-40(3)68(110)92-56(32-41-14-16-44(96)17-15-41)70(112)82-37-61(98)86-58(79(121)122)34-43-36-81-48-12-7-5-10-46(43)48/h4-7,9-12,14-17,35-36,39-40,49-59,80-81,96H,8,13,18-34,37-38H2,1-3H3,(H,82,112)(H,83,111)(H,84,113)(H,85,97)(H,86,98)(H,87,114)(H,88,115)(H,89,116)(H,90,117)(H,91,118)(H,92,110)(H,93,119)(H,94,120)(H,100,101)(H,102,103)(H,104,105)(H,106,107)(H,108,109)(H,121,122)
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| Chemical Name |
4-[[4-carboxy-2-[[4-carboxy-2-[[4-carboxy-2-[[4-carboxy-2-[[2-[[3-(1H-indol-3-yl)-2-[[1-[2-[(5-oxopyrrolidine-2-carbonyl)amino]acetyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]-4-methylpentanoyl]amino]butanoyl]amino]butanoyl]amino]butanoyl]amino]butanoyl]amino]-5-[[1-[[1-[[2-[[1-carboxy-2-(1H-indol-3-yl)ethyl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-5-oxopentanoic acid
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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) |
H2O: ~14.3 mg/mL (~8.4 mM; with ultrasonication and adjustment of pH to 6 with NH3·H2O)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (1.17 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), Clear solution; with ultrasonication and warming and heat to 60°C.
(Please use freshly prepared in vivo formulations for optimal results.) |
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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