| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| Other Sizes |
| Targets |
Tyr-Somatostatin-14 primarily targets the somatostatin receptors (SSTRs). These receptors are G-protein-coupled transmembrane receptors, and five subtypes (SSTR1-SSTR5) have been identified. By binding to SSTRs, the peptide analog modulates endocrine and nervous system functions. The additional tyrosine residue enables radiolabeling for imaging and receptor binding studies. Tyr-Somatostatin-14 has potential therapeutic applications as a drug candidate for various diseases.
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| ln Vitro |
In vitro, Tyr-Somatostatin-14 binds to somatostatin receptors (SSTRs) and modulates receptor-mediated signaling. The peptide analog mimics the structure and activity of naturally occurring somatostatin. It is used in receptor binding studies to investigate SSTR subtype specificity and function. The additional tyrosine residue enables radiolabeling for detection and quantification in binding assays. Its activity has been characterized in various cell-based systems expressing SSTRs.
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| ln Vivo |
In vivo, Tyr-Somatostatin-14 has potential therapeutic applications as a drug candidate for various diseases. As a somatostatin receptor ligand, it modulates endocrine and nervous system functions. The peptide analog is used in preclinical research to study SSTR-mediated signaling and potential therapeutic interventions. Its radiolabeled form can be used for imaging applications. Further in vivo studies are ongoing to fully characterize its pharmacokinetic and pharmacodynamic properties.
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| Enzyme Assay |
Tyr-Somatostatin-14 receptor binding assays involve measuring affinity for somatostatin receptors (SSTRs). Radioligand binding displacement studies are performed using membranes from cells expressing recombinant SSTR subtypes. The compound's binding affinity (Ki) is determined through competitive binding assays with radiolabeled somatostatin. Functional activity is assessed by measuring inhibition of cAMP production or other SSTR-mediated signaling pathways. Assays are performed in appropriate buffer systems with positive controls such as native somatostatin-14. IC50 or Ki values are calculated from dose-response curves.
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| Cell Assay |
Tyr-Somatostatin-14 cell-based assays are conducted in cells expressing somatostatin receptors (SSTRs). Cells are cultured in appropriate media at 37°C with 5% CO2 and treated with the peptide at varying concentrations. Receptor activation is assessed by measuring inhibition of forskolin-stimulated cAMP production using ELISA or HTRF-based methods. Receptor internalization may be assessed by immunofluorescence. Cell viability is assessed by standard assays. Experiments are performed in triplicate with appropriate positive (e.g., somatostatin-14) and negative (vehicle) controls.
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| Animal Protocol |
Tyr-Somatostatin-14 in vivo studies are conducted in animal models for pharmacokinetic and pharmacodynamic evaluation. Animals are administered the peptide via intravenous, subcutaneous, or intraperitoneal injection. For imaging studies, radiolabeled Tyr-Somatostatin-14 is used for PET or SPECT imaging to assess receptor expression in tissues. For therapeutic studies, animal models of neuroendocrine tumors or other SSTR-expressing diseases may be used. Blood samples are collected for pharmacokinetic analysis. Animals are monitored for clinical signs. Tissues are collected for histopathological and biomarker analysis at study endpoints. Studies are conducted in accordance with institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Tyr-Somatostatin-14 (MW 1801.05 g/mol, C85H113N19O21S2) is a synthetic peptide. The peptide sequence is Tyr-Ala-Gly-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys with a disulfide bond between the cysteine residues. It is supplied as a lyophilized powder and should be stored at -20°C. The compound is soluble in appropriate aqueous buffers. Pharmacokinetic parameters such as half-life, bioavailability, and tissue distribution would be determined in species-specific studies. The peptide is used in endocrine and neuroendocrine research.
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| Toxicity/Toxicokinetics |
Tyr-Somatostatin-14 is generally well-tolerated in preclinical studies at therapeutic doses. The compound is a synthetic peptide analog of somatostatin with established safety profiles. No significant adverse effects have been reported in the available literature at research-use concentrations. The compound is intended for research use only. Standard safety precautions should be followed when handling. Comprehensive toxicological evaluation would be required for therapeutic development.
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| Additional Infomation |
Tyr-Somatostatin-14 is a synthetic peptide analog that plays a crucial role in regulating endocrine and nervous system functions. It is a modified peptide incorporating an additional Tyrosine amino acid into the structure of Somatostatin-14. The peptide primarily targets somatostatin receptors (SSTRs). It has potential therapeutic applications as a drug candidate for various diseases. Its molecular formula is C85H113N19O21S2 with a molecular weight of 1801.05 g/mol. All applications are limited to non-human research use.
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| Molecular Formula |
C85H113N19O21S2
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|---|---|
| Molecular Weight |
1801.05000
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| Exact Mass |
1799.78
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| CAS # |
58100-03-1
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| PubChem CID |
74339064
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
3.11
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| Hydrogen Bond Donor Count |
24
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| Hydrogen Bond Acceptor Count |
26
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| Rotatable Bond Count |
30
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| Heavy Atom Count |
127
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| Complexity |
3630
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C[C@H](NC([C@@H](N)CC1=CC=C(O)C=C1)=O)C(NCC(N[C@H]2CSSC[C@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC([C@@H](NC2=O)CCCCN)=O)CC(N)=O)=O)CC3=CC=CC=C3)=O)CC4=CC=CC=C4)=O)CC5=CNC6=CC=CC=C56)=O)CCCCN)=O)[C@H](O)C)=O)CC7=CC=CC=C7)=O)[C@H](O)C)=O)CO)=O)C(O)=O)=O)=O
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| InChi Key |
WIKMYZSTFRZVMC-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C85H113N19O21S2/c1-46(92-73(112)56(88)35-52-29-31-54(108)32-30-52)72(111)91-42-69(110)93-66-44-126-127-45-67(85(124)125)102-81(120)65(43-105)101-84(123)71(48(3)107)104-80(119)62(38-51-23-11-6-12-24-51)100-83(122)70(47(2)106)103-75(114)59(28-16-18-34-87)94-78(117)63(39-53-41-90-57-26-14-13-25-55(53)57)98-77(116)61(37-50-21-9-5-10-22-50)96-76(115)60(36-49-19-7-4-8-20-49)97-79(118)64(40-68(89)109)99-74(113)58(95-82(66)121)27-15-17-33-86/h4-14,19-26,29-32,41,46-48,56,58-67,70-71,90,105-108H,15-18,27-28,33-40,42-45,86-88H2,1-3H3,(H2,89,109)(H,91,111)(H,92,112)(H,93,110)(H,94,117)(H,95,121)(H,96,115)(H,97,118)(H,98,116)(H,99,113)(H,100,122)(H,101,123)(H,102,120)(H,103,114)(H,104,119)(H,124,125)
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| Chemical Name |
19,34-bis(4-aminobutyl)-37-[[2-[2-[[2-amino-3-(4-hydroxyphenyl)propanoyl]amino]propanoylamino]acetyl]amino]-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-10,16-bis(1-hydroxyethyl)-7-(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carboxylic 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. |
| 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 : ~100 mg/mL (~55.52 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 | 0.5552 mL | 2.7762 mL | 5.5523 mL | |
| 5 mM | 0.1110 mL | 0.5552 mL | 1.1105 mL | |
| 10 mM | 0.0555 mL | 0.2776 mL | 0.5552 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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