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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
Mini Gastrin I targets the cholecystokinin-B (CCK-B)/gastrin receptor, a G protein-coupled receptor found primarily in the stomach and central nervous system. By binding to this receptor, it mimics the activity of the full-length hormone. The sequence is Leu-Glu-Glu-Glu-Glu-Glu-Ala-Tyr-Gly-Trp-Met-Asp-Phe-NH2.
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| ln Vitro |
As a truncated but potent gastrin analog, Mini Gastrin I is used to stimulate gastric acid secretion. It binds with high affinity to the cholecystokinin-B (CCK-B)/gastrin receptor, initiating a signaling cascade that activates H+/K+ ATPase in parietal cells. It is also used to target CCK-B/gastrin receptor-expressing tumors.
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| ln Vivo |
Not available. The primary in vivo use of Mini Gastrin I is in nuclear medicine, where it is radiolabeled to image tumors. Specific in vivo activity data on its metabolic or proliferative effects is not provided. It is known to be useful for targeting tumors that express its receptor.
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| Enzyme Assay |
Standard binding assays for assessing the affinity of Mini Gastrin I involve using radiolabeled gastrin or a gastrin analog. The assay is performed on membranes prepared from cells overexpressing the CCK-B/gastrin receptor. The membrane preparation is incubated with a fixed concentration of the radioligand and varying concentrations of Mini Gastrin I. After incubation, bound and free ligands are separated by vacuum filtration, and the radioactivity on the filters is counted to calculate binding affinity.
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| Cell Assay |
Standard cellular assays for studying gastrin-mediated signaling involve culturing receptor-expressing cells, such as A431-B (transfected with CCK-B receptor) or AR42J rat pancreatic acinar cells. After serum starvation, cells are treated with varying concentrations of Mini Gastrin I. The signaling response, such as intracellular calcium mobilization, is measured using a calcium-sensitive dye (e.g., Fluo-4). Alternatively, the activation of downstream kinases like ERK1/2 or PKC can be assessed by Western blotting of cell lysates.
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| Animal Protocol |
For in vivo studies, the peptide is typically radiolabeled with a diagnostic isotope like Indium-111 or Gallium-68 and administered intravenously to animal models or patients. The distribution of the radiotracer is then monitored by Single Photon Emission Computed Tomography (SPECT) or Positron Emission Tomography (PET) imaging to visualize CCK-B/gastrin receptor-expressing tissues, such as certain neuroendocrine tumors.
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| ADME/Pharmacokinetics |
As a peptide, Mini Gastrin I TFA is expected to have a very short plasma half-life due to rapid proteolytic degradation if administered systemically without protection. This is why it is primarily used for diagnostic imaging after being radiolabeled, as the imaging is completed before significant degradation occurs. Its rapid clearance helps to provide a high tumor-to-background ratio.
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| Toxicity/Toxicokinetics |
Peptides like this are generally considered safe for diagnostic use at low concentrations, as they are rapidly broken down into constituent amino acids. Toxicity associated with gastrin mimics would typically be related to unwanted stimulation of gastric acid secretion. For radiolabeled versions, the primary risk is the radiation dose, which is managed within safety guidelines.
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| References | |
| Additional Infomation |
Mini Gastrin I, human TFA is a research-grade peptide used to study gastric acid secretion, the biology of the CCK-B/gastrin receptor, and neuroendocrine cancers. It is not a drug and has not been approved by the FDA for any therapeutic indication. It is strictly intended for laboratory research use, often in the context of developing new diagnostic imaging agents or targeted radionuclide therapies for cancer.
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| Molecular Formula |
C76H100F3N15O28S
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| Molecular Weight |
1760.75
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| Related CAS # |
Mini Gastrin I, human;54405-27-5
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| Appearance |
White to yellow solid powder
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5679 mL | 2.8397 mL | 5.6794 mL | |
| 5 mM | 0.1136 mL | 0.5679 mL | 1.1359 mL | |
| 10 mM | 0.0568 mL | 0.2840 mL | 0.5679 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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