| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
Gastrin I (rat) targets the cholecystokinin-2 receptor (CCK2R), also known as the gastrin receptor, which is a G-protein coupled receptor expressed on gastric parietal cells. Activation of this receptor stimulates acid secretion from parietal cells via histamine release from enterochromaffin-like (ECL) cells.
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|---|---|
| ln Vitro |
Gastrin I (rat) potently stimulates gastric acid secretion in vitro. It activates the CCK2 receptor on parietal cells, leading to increased intracellular calcium and activation of the proton pump (H+/K+-ATPase). The peptide also promotes the growth and differentiation of gastric mucosal cells.
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| ln Vivo |
In vivo, Gastrin I (rat) stimulates gastric acid secretion when administered to animal models. It is used to determine the expression of histidine decarboxylase and histamine metabolism. The peptide plays a crucial role in maintaining gastric mucosal architecture and function.
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| Enzyme Assay |
Receptor binding assays for Gastrin I use membrane preparations from cells expressing the CCK2 receptor. Radiolabeled gastrin or CCK is incubated with varying concentrations of the test peptide, and binding affinity is determined by competition binding curves.
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| Cell Assay |
Cellular assays for Gastrin I typically use parietal cell cultures or cell lines expressing the CCK2 receptor. Cells are treated with the peptide, and acid secretion is measured by intracellular pH indicators or by assessing proton pump activation. Calcium mobilization and signaling pathways can also be evaluated.
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| Animal Protocol |
In vivo studies with Gastrin I (rat) are conducted in rodent models. The peptide is typically administered via subcutaneous or intravenous injection. Gastric acid secretion is measured by gastric aspiration or using pH probes. Effects on gastric mucosal histology and enzyme expression are also assessed.
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| ADME/Pharmacokinetics |
As a peptide hormone, Gastrin I (rat) is expected to have a short half-life due to proteolytic degradation. The compound should be stored as a lyophilized powder at -20degC. Standard peptide handling and storage procedures apply.
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| Toxicity/Toxicokinetics |
Toxicity data for Gastrin I (rat) are limited. Peptide hormones are generally well-tolerated at physiological concentrations. Chronic hypergastrinemia may be associated with gastric mucosal hyperplasia, but acute toxicity is unlikely. Standard safety precautions apply.
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| References | |
| Additional Infomation |
Gastrin I (rat) is a research-use peptide and is not approved for therapeutic applications. It is also known as Rat Gastrin-17. The peptide is used to study gastric acid secretion regulation, gastrointestinal physiology, and the role of gastrin in gastric mucosal maintenance. It is available from multiple research suppliers.
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| Molecular Formula |
C94H128N22O31S2
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|---|---|
| Molecular Weight |
2126.28092
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| Exact Mass |
2124.86
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| CAS # |
81123-06-0
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| PubChem CID |
57339541
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| Appearance |
White to off-white solid powder
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| LogP |
2.222
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| Hydrogen Bond Donor Count |
27
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| Hydrogen Bond Acceptor Count |
34
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| Rotatable Bond Count |
65
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| Heavy Atom Count |
149
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| Complexity |
4740
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| Defined Atom Stereocenter Count |
16
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| SMILES |
C[C@@H](C(=O)N[C@@H](CC1=CC=C(C=C1)O)C(=O)NCC(=O)N[C@@H](CC2=CNC3=CC=CC=C32)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](CC4=CC=CC=C4)C(=O)N)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCC(=O)O)NC(=O)[C@H](CCSC)NC(=O)[C@@H]5CCCN5C(=O)[C@@H]6CCCN6C(=O)[C@H](CCCNC(=N)N)NC(=O)[C@@H]7CCC(=O)N7
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| InChi Key |
FUTWNIPXZKAJHO-FKZYTOAASA-N
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| InChi Code |
InChI=1S/C94H128N22O31S2/c1-48(79(133)113-65(43-50-19-21-52(117)22-20-50)80(134)100-47-71(119)103-66(44-51-46-99-54-15-8-7-14-53(51)54)89(143)109-61(35-40-148-2)88(142)114-67(45-77(130)131)90(144)112-64(78(95)132)42-49-12-5-4-6-13-49)101-81(135)56(24-30-72(120)121)104-83(137)57(25-31-73(122)123)105-84(138)58(26-32-74(124)125)106-85(139)59(27-33-75(126)127)107-86(140)60(28-34-76(128)129)108-87(141)62(36-41-149-3)110-91(145)68-17-10-38-115(68)93(147)69-18-11-39-116(69)92(146)63(16-9-37-98-94(96)97)111-82(136)55-23-29-70(118)102-55/h4-8,12-15,19-22,46,48,55-69,99,117H,9-11,16-18,23-45,47H2,1-3H3,(H2,95,132)(H,100,134)(H,101,135)(H,102,118)(H,103,119)(H,104,137)(H,105,138)(H,106,139)(H,107,140)(H,108,141)(H,109,143)(H,110,145)(H,111,136)(H,112,144)(H,113,133)(H,114,142)(H,120,121)(H,122,123)(H,124,125)(H,126,127)(H,128,129)(H,130,131)(H4,96,97,98)/t48-,55-,56-,57-,58-,59-,60-,61-,62-,63-,64-,65-,66-,67-,68-,69-/m0/s1
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| Chemical Name |
(4S)-5-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-amino-1-oxo-3-phenylpropan-2-yl]amino]-3-carboxy-1-oxopropan-2-yl]amino]-4-methylsulfanyl-1-oxobutan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-(4-hydroxyphenyl)-1-oxopropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-1-[(2S)-1-[(2S)-5-carbamimidamido-2-[[(2S)-5-oxopyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]-4-methylsulfanylbutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]amino]-4-carboxybutanoyl]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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ≥ 27.5 mg/mL (~12.93 mM)
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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 | 0.4703 mL | 2.3515 mL | 4.7030 mL | |
| 5 mM | 0.0941 mL | 0.4703 mL | 0.9406 mL | |
| 10 mM | 0.0470 mL | 0.2352 mL | 0.4703 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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