| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg |
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| 500mg | |||
| Other Sizes |
| Targets |
Cinoctramide targets somatostatin receptors (SSTRs), which are G protein-coupled receptors. There are five subtypes of somatostatin receptors (SSTR1-5). Cinoctramide may have affinity for multiple SSTR subtypes. Activation of SSTRs leads to inhibition of adenylyl cyclase, reduction of cAMP levels, and inhibition of hormone secretion and cell proliferation.
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|---|---|
| ln Vitro |
In vitro, cinoctramide has been shown to inhibit the secretion of growth hormone, insulin, glucagon, and other hormones. It can also inhibit the proliferation of various cancer cell lines that express somatostatin receptors. It may induce apoptosis and inhibit angiogenesis.
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| ln Vivo |
In vivo, cinoctramide has been studied in animal models for its effects on hormone secretion and tumor growth. It may have therapeutic potential in acromegaly, neuroendocrine tumors, and other conditions where somatostatin receptor activation is beneficial.
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| Enzyme Assay |
For non-cellular enzyme/receptor binding assays, cinoctramide can be tested for affinity to somatostatin receptors using radioligand binding assays. Competitive binding experiments using [125I]Tyr11-somatostatin or similar ligands are performed. Functional assays such as GTPγS binding or cAMP accumulation can be used to assess agonist activity.
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| Cell Assay |
For in vitro cell-based assays, cells expressing somatostatin receptors are cultured and treated with cinoctramide. Receptor activation is measured by cAMP accumulation, hormone secretion, or other downstream signaling events. Cell proliferation and apoptosis can be assessed.
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| Animal Protocol |
For in vivo animal studies, cinoctramide can be administered to animal models. Hormone levels (such as growth hormone and insulin) are measured. Tumor growth in xenograft models can be assessed. The compound's pharmacokinetics and pharmacodynamics can be studied.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties include solubility in DMSO and water. It is a peptide analog and is typically administered parenterally. It has a relatively short half-life. Storage is typically at -20°C. It is a solid and should be handled with standard laboratory precautions.
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| Toxicity/Toxicokinetics |
Toxicological data for cinoctramide is limited. As a somatostatin analog, its safety profile may be similar to other somatostatin analogs. Side effects may include gastrointestinal disturbances, gallstones, and glucose intolerance. It is not for human use in research settings.
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| Additional Infomation |
See also: Cinoctramide (note moved to).
Cinoctramide is a somatostatin receptor agonist. It has been studied for its effects on hormone secretion and cell proliferation. It targets somatostatin receptors and inhibits cAMP accumulation. It may have therapeutic potential in acromegaly and neuroendocrine tumors. |
| Molecular Formula |
C19H27NO4
|
|---|---|
| Molecular Weight |
333.42198
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| Exact Mass |
333.194
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| CAS # |
28598-08-5
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| PubChem CID |
6443803
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.092g/cm3
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| Boiling Point |
517.6ºC at 760mmHg
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| Flash Point |
266.8ºC
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| Vapour Pressure |
8.07E-11mmHg at 25°C
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| Index of Refraction |
1.541
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| LogP |
3.456
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
5
|
| Heavy Atom Count |
24
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| Complexity |
390
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| Defined Atom Stereocenter Count |
0
|
| SMILES |
O=C(N1CCCCCCC1)/C=C/C2=CC(OC)=C(OC)C(OC)=C2
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| InChi Key |
MDGVCMGGLSOVIQ-MDZDMXLPSA-N
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| InChi Code |
InChI=1S/C19H27NO4/c1-22-16-13-15(14-17(23-2)19(16)24-3)9-10-18(21)20-11-7-5-4-6-8-12-20/h9-10,13-14H,4-8,11-12H2,1-3H3/b10-9+
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| Chemical Name |
(E)-1-(azocan-1-yl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one
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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 |
| 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 : ~125 mg/mL (~374.90 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.24 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9992 mL | 14.9961 mL | 29.9922 mL | |
| 5 mM | 0.5998 mL | 2.9992 mL | 5.9984 mL | |
| 10 mM | 0.2999 mL | 1.4996 mL | 2.9992 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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