| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Somatostatin receptors (SSTR1, SSTR2, SSTR3, SSTR4, SSTR5). Cyclosomatostatin is a non-selective somatostatin receptor antagonist. It can inhibit somatostatin receptor type 1 (SSTR1) signaling and decreases cell proliferation, ALDH+ cell population size, and sphere-formation in colorectal cancer (CRC) cells.
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| ln Vitro |
Cyclosomatostatin inhibits somatostatin receptor type 1 (SSTR1) signaling. It decreases cell proliferation, ALDH+ cell population size, and sphere-formation in colorectal cancer (CRC) cells, suggesting a role for SSTR1 in cancer stem cell maintenance. It blocks the effects of CRF-induced suppression of gastric emptying and somatostatin effects on airway beta-adrenergic function. It also prevents growth hormone, insulin, glucagon release, and modulation of ACh release.
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| ln Vivo |
In vivo, cyclosomatostatin blocks somatostatin-mediated effects including CRF-induced suppression of gastric emptying and somatostatin effects on airway beta-adrenergic function. It also prevents growth hormone, insulin, and glucagon release, demonstrating broad antagonism of somatostatin physiology. It is used to study the physiological roles of endogenous somatostatin in various organ systems.
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| Enzyme Assay |
Cell-free radioligand binding assays for somatostatin receptors: Membranes from CHO-K1 cells expressing human SSTR1, SSTR2, SSTR3, SSTR4, or SSTR5 are incubated with [125I]-Tyr11-SRIF-14 (0.1 nM) and increasing concentrations of cyclosomatostatin (0.01-10,000 nM) in binding buffer (50 mM HEPES, pH 7.4, 5 mM MgCl2, 0.5% BSA) for 60-90 min at 25degC. Bound radioactivity is separated by GF/B filtration. IC50 values are determined by nonlinear regression. Cyclosomatostatin shows non-selective antagonism across all five SSTR subtypes.
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| Cell Assay |
SSTR1-expressing CHO-K1 cells are seeded and pre-incubated with cyclosomatostatin (0.1-10,000 nM) for 15-30 min, then stimulated with somatostatin-14 (1-100 nM). Functional readouts include inhibition of forskolin-stimulated cAMP accumulation (measured by HTRF cAMP kit) or changes in intracellular calcium. Cyclosomatostatin is also tested for its ability to reduce ALDH+ cell population size and sphere-formation in colorectal cancer (CRC) cell lines, indicating its effect on cancer stem cell properties.
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| Animal Protocol |
In vivo studies are conducted in rats to assess gastric emptying. Cyclosomatostatin is administered intravenously (1-10 mg/kg) or intraperitoneally prior to CRF administration. Gastric emptying of a liquid or solid meal is measured by phenol red method or by quantifying the amount of food remaining in the stomach after a set time. For endocrine studies, cyclosomatostatin is administered prior to somatostatin or GH-releasing hormone to assess GH suppression reversal. For airway studies, cyclosomatostatin is used to block somatostatin-induced modulation of beta-adrenergic bronchodilation.
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| ADME/Pharmacokinetics |
No specific PK data are reported for cyclosomatostatin. As a cyclic peptide (C44H57N7O6, molecular weight 779.98), cyclosomatostatin is not orally bioavailable and is typically administered intravenously or intraperitoneally for in vivo studies. The half-life is expected to be short (minutes to hours) due to peptide degradation by proteases. It is soluble in DMSO (10-25 mg/mL). Storage: -20degC, protect from light.
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| Toxicity/Toxicokinetics |
No specific toxicity data are reported for cyclosomatostatin. As a somatostatin receptor antagonist, potential toxicities may include disruption of normal somatostatin-mediated regulatory functions (e.g., dysregulated GH, insulin, glucagon secretion leading to metabolic disturbances). At pharmacological doses used in research (1-10 mg/kg), no overt toxicity has been reported. No clinical trials have been conducted.
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| References | |
| Additional Infomation |
Other information: Cyclosomatostatin is a non-selective somatostatin receptor antagonist. CAS number: 84211-54-1. The peptide sequence is cyclo(7-aminoheptanoyl-Phe-D-Trp-Lys-Thr[Bzl]). It is available as the acetate salt for research purposes. Cyclosomatostatin is a key pharmacological tool for dissecting the physiological roles of endogenous somatostatin and its five receptor subtypes. It is not FDA-approved and is for research use only. Synonyms include c[Ahe-cyclo(7-aminoheptanoyl-Phe-D-Trp-Lys-Thr)].
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| Molecular Formula |
C44H57N7O6
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|---|---|
| Molecular Weight |
779.97
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| Exact Mass |
779.437
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| CAS # |
84211-54-1
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| Related CAS # |
Cyclosomatostatin TFA
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| PubChem CID |
4195535
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| Appearance |
White to off-white solid powder
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| Density |
1.147g/cm3
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| Boiling Point |
1118.4ºC at 760 mmHg
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| Flash Point |
630.2ºC
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| Index of Refraction |
1.558
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| LogP |
6.051
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
57
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| Complexity |
1270
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CC(C1C(=O)NCCCCCCC(=O)NC(C(=O)NC(C(=O)NC(C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)OCC5=CC=CC=C5
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| InChi Key |
YHVHQZYJGWGAKN-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C44H57N7O6/c1-30(57-29-32-18-8-5-9-19-32)40-44(56)46-25-15-3-2-10-23-39(52)48-37(26-31-16-6-4-7-17-31)42(54)50-38(27-33-28-47-35-21-12-11-20-34(33)35)43(55)49-36(41(53)51-40)22-13-14-24-45/h4-9,11-12,16-21,28,30,36-38,40,47H,2-3,10,13-15,22-27,29,45H2,1H3,(H,46,56)(H,48,52)(H,49,55)(H,50,54)(H,51,53)
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| Chemical Name |
6-(4-aminobutyl)-12-benzyl-9-(1H-indol-3-ylmethyl)-3-(1-phenylmethoxyethyl)-1,4,7,10,13-pentazacycloicosane-2,5,8,11,14-pentone
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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: 10 mg/mL (12.82 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 | 1.2821 mL | 6.4105 mL | 12.8210 mL | |
| 5 mM | 0.2564 mL | 1.2821 mL | 2.5642 mL | |
| 10 mM | 0.1282 mL | 0.6411 mL | 1.2821 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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