| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Somatostatin receptors (SSTR1-5), a family of G-protein-coupled receptors with five subtypes (SSTR1, SSTR2, SSTR3, SSTR4, SSTR5). The peptide acts as a ligand for these receptors, mimicking the actions of the native somatostatin-14 hormone, which inhibits the release of various hormones (growth hormone, insulin, glucagon, gastrin) and neurotransmitters.
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| ln Vitro |
This peptide fragment exhibits somatostatin receptor binding affinity, although typically with somewhat reduced potency compared to the full-length somatostatin-14 due to the absence of the N-terminal Ala-Gly residues, which contribute to receptor subtype selectivity. It is used in competition binding assays to study receptor-ligand interactions. In functional cell-based assays, it may inhibit hormone secretion (e.g., growth hormone from pituitary cells) similar to the full-length peptide, with potency dependent on receptor subtype expression.
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| ln Vivo |
In vivo, somatostatin analogs (including this fragment) are used to study the physiological roles of somatostatin receptors, including suppression of hormone secretion, modulation of gastrointestinal motility, and inhibition of cell proliferation. This specific fragment may be used in animal models to study somatostatin receptor-mediated effects, though its shorter half-life limits its utility compared to more stable synthetic analogs (e.g., octreotide).
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| Enzyme Assay |
Competitive radioligand binding assay: Membranes from cells expressing specific somatostatin receptor subtypes (SSTR1-5) are incubated with a radiolabeled somatostatin analog (e.g., [¹2⁵I]Tyr¹¹-somatostatin-14, 0.05-0.2 nM) and varying concentrations of the peptide (0.01-10,000 nM) in binding buffer (50 mM HEPES pH 7.4, 5 mM MgCl2, 0.5% BSA, 0.1 mM PMSF) for 2 hours at 25degC. Bound radioactivity is separated by filtration through GF/C filters and quantified by gamma counting. IC50 and Ki values are calculated using nonlinear regression.
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| Cell Assay |
Inhibition of hormone secretion assay: Cells that secrete hormones regulated by somatostatin (e.g., GH-secreting pituitary cells, insulin-secreting pancreatic beta cells) are seeded in 24-well plates and treated with the peptide (0.01-10,000 nM) for 30-60 minutes, with or without a secretagogue (e.g., GHRH for GH secretion, glucose for insulin secretion). Supernatants are collected and hormone levels are measured by ELISA or RIA. Inhibition of stimulated hormone release is quantified and EC50 values for inhibition are calculated.
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| Animal Protocol |
Somatostatin analog studies in rodents: Animal models (e.g., rats with GH-secreting tumors or normal mice) are administered the peptide via intravenous or subcutaneous injection. Blood samples are collected at multiple time points for measurement of growth hormone, insulin, or glucagon levels by ELISA. Models of acromegaly or neuroendocrine tumors may be used to assess efficacy and receptor-mediated effects.
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| ADME/Pharmacokinetics |
As a peptide, pharmacokinetics are characterized by rapid clearance and degradation in vivo (half-life typically 1-3 minutes in circulation). Not orally bioavailable; requires parenteral administration. The disulfide bridge provides some conformational stability but does not prevent rapid proteolytic cleavage.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for this fragment. Somatostatin and its analogs are generally well-tolerated but can cause gastrointestinal effects (diarrhea, steatorrhea, abdominal pain), gallbladder stasis, and gallstones with chronic use due to inhibition of gallbladder contraction.
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| Additional Infomation |
This is a research peptide, not an approved drug. It is used as a tool to study somatostatin receptor function, receptor subtype selectivity, and in peptide screening assays for drug discovery. The full sequence is H-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Thr-Ser-Cys-OH with a disulfide bridge between Cys1 and Cys12. It is also referred to as somatostatin-14 (3-14) or somatostatin fragment 3-14.
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| Molecular Formula |
C73H99F3N16O19S2
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|---|---|
| Molecular Weight |
1625.78818535805
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| Exact Mass |
1624.666
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| CAS # |
54518-51-3
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| PubChem CID |
145707569
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
27
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| Rotatable Bond Count |
46
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| Heavy Atom Count |
113
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| Complexity |
2960
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| Defined Atom Stereocenter Count |
14
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| SMILES |
C[C@H]([C@@H](C(=O)N[C@@H](CC1=CC=CC=C1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CO)C(=O)N[C@@H](CS)C(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CC2=CNC3=CC=CC=C32)NC(=O)[C@H](CC4=CC=CC=C4)NC(=O)[C@H](CC5=CC=CC=C5)NC(=O)[C@H](CC(=O)N)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CS)N)O.C(=O)(C(F)(F)F)O
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| InChi Key |
ZJWIEPXPIRDHLF-ASWYRLASSA-N
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| InChi Code |
InChI=1S/C71H98N16O17S2.C2HF3O2/c1-39(89)58(69(101)83-52(32-43-22-10-5-11-23-43)67(99)87-59(40(2)90)70(102)84-55(36-88)68(100)85-56(38-106)71(103)104)86-62(94)49(27-15-17-29-73)78-65(97)53(33-44-35-76-47-25-13-12-24-45(44)47)81-64(96)51(31-42-20-8-4-9-21-42)79-63(95)50(30-41-18-6-3-7-19-41)80-66(98)54(34-57(75)91)82-61(93)48(26-14-16-28-72)77-60(92)46(74)37-105;3-2(4,5)1(6)7/h3-13,18-25,35,39-40,46,48-56,58-59,76,88-90,105-106H,14-17,26-34,36-38,72-74H2,1-2H3,(H2,75,91)(H,77,92)(H,78,97)(H,79,95)(H,80,98)(H,81,96)(H,82,93)(H,83,101)(H,84,102)(H,85,100)(H,86,94)(H,87,99)(H,103,104);(H,6,7)/t39-,40-,46+,48+,49+,50+,51+,52+,53+,54+,55+,56+,58+,59+;/m1./s1
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| Chemical Name |
(2R)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-2-[[(2S,3R)-2-[[(2S)-6-amino-2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[(2S)-4-amino-2-[[(2S)-6-amino-2-[[(2R)-2-amino-3-sulfanylpropanoyl]amino]hexanoyl]amino]-4-oxobutanoyl]amino]-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]hexanoyl]amino]-3-hydroxybutanoyl]amino]-3-phenylpropanoyl]amino]-3-hydroxybutanoyl]amino]-3-hydroxypropanoyl]amino]-3-sulfanylpropanoic acid;2,2,2-trifluoroacetic 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 : ~100 mg/mL (~66.24 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 | 0.6151 mL | 3.0754 mL | 6.1509 mL | |
| 5 mM | 0.1230 mL | 0.6151 mL | 1.2302 mL | |
| 10 mM | 0.0615 mL | 0.3075 mL | 0.6151 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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