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Purity: ≥98%
| Targets |
Target: Cortistatin-14 targets all five cloned somatostatin receptors (sst1-sst5) and the ghrelin receptor. It exhibits binding affinity with IC50 values for somatostatin receptor binding: sst2 0.09 nM, sst4 0.2 nM, sst3 0.3 nM, sst5 0.3 nM, sst1 5 nM. The compound prevents somatostatin-14 binding at these receptors. It also binds to the ghrelin receptor to exert its biological activities.
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| ln Vitro |
In Vitro Activity: Cortistatin-14 displays potency at all five somatostatin receptors with IC50 values ranging from 0.09 to 5 nM. It binds to the ghrelin receptor to exert its biological activities. The neuropeptide demonstrates neuronal depressant activity. CST-14 and BDNF mRNA are decreased in hippocampus and cortex once mice are exposed to stress. Detailed in vitro activity data are available from the primary literature.
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| ln Vivo |
In Vivo Activity: Centrally administered Cortistatin-14 induces antidepressant-like effects in mice via mediating ghrelin and GABAA receptor signaling pathways. Intracerebroventricular (i.c.v.) or intranasal administration of CST-14 produces rapid antidepressant effects. NIR fluorescence imaging detected brain uptake and distribution after intranasal CST-14. Antidepressant effects of CST-14 are related to ghrelin and GABAA system. Co-injection of CST-14 and NPS produces antidepressant effects without impairing memory. In depression models, CST-14 produced antidepressant-like effects without altering locomotor activity levels.
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| Enzyme Assay |
In Vitro Enzyme/Receptor Binding Protocol: Somatostatin receptor binding assays typically use membrane preparations from cells expressing specific SSTR subtypes. Radioligand binding with [125I]somatostatin-14 or similar ligands is performed with varying concentrations of Cortistatin-14 to determine IC50 values. Ghrelin receptor binding assays may also be performed using appropriate radioligands.
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| Cell Assay |
In Vitro Cell-Based Assay Protocol: Cells expressing somatostatin receptors or ghrelin receptors are treated with Cortistatin-14 at various concentrations. Receptor activation and downstream signaling are measured using standard assays such as cAMP accumulation or calcium mobilization. Neuronal activity may be assessed using electrophysiological techniques. Gene expression changes including BDNF mRNA can be measured by qPCR.
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| Animal Protocol |
In Vivo Animal Assay Protocol: Mouse models of depression are used to evaluate antidepressant-like effects. Cortistatin-14 is administered centrally (i.c.v.) or intranasally. Behavioral tests such as forced swim test, tail suspension test, or open field test are performed. NIR fluorescence imaging is used to detect brain uptake and distribution after intranasal administration. Stress-induced depression models may also be employed.
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| ADME/Pharmacokinetics |
Pharmacokinetics: Cortistatin-14 has molecular formula C81H113N19O19S2 and molecular weight 1721.01. As a cyclic peptide, it is expected to have limited oral bioavailability and is typically administered parenterally (i.c.v. or intranasal). NIR fluorescence imaging has been used to detect brain uptake and distribution after intranasal administration.
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| Toxicity/Toxicokinetics |
Toxicity: No detailed toxicity data are publicly available for Cortistatin-14. As an endogenous neuropeptide, it is expected to have a favorable safety profile. In animal studies, CST-14 produced antidepressant-like effects without altering locomotor activity levels. Standard toxicological evaluation would be required for therapeutic development. The compound is for research use only.
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| References |
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| Additional Infomation |
Additional Information: Cortistatin-14 has CAS number 193829-96-8. It is also known as CST-14, CST14, and CST 14. The neuropeptide is mainly expressed in the cortex and hippocampus and coexists with GABA. It has structural and functional similarities to somatostatin-14. CST-14 has potential applications in depression, sleep disorders, and neurological conditions. The peptide sequence is Pro-Cys-Lys-Asn-Phe-Phe-Trp-Lys-Thr-Phe-Ser-Ser-Cys-Lys. For research use only, not for human therapy.
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| Molecular Formula |
C81H113N19O19S2
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|---|---|
| Molecular Weight |
1721.00983595848
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| Exact Mass |
1719.79
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| CAS # |
193829-96-8
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| PubChem CID |
16133803
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| Appearance |
White to off-white solid powder
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| LogP |
-2.7
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| Hydrogen Bond Donor Count |
23
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| Hydrogen Bond Acceptor Count |
25
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| Rotatable Bond Count |
30
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| Heavy Atom Count |
121
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| Complexity |
3400
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| Defined Atom Stereocenter Count |
15
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| SMILES |
S1C[C@@H](C(N[C@H](C(N[C@@H](CC(N)=O)C(N[C@@H](CC2C=CC=CC=2)C(N[C@@H](CC2C=CC=CC=2)C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@H](C(N[C@@H](CO)C(N[C@@H](CO)C(N[C@H](C(N[C@H](C(=O)O)CCCCN)=O)CS1)=O)=O)=O)CC1C=CC=CC=1)=O)[C@@H](C)O)=O)CCCCN)=O)CC1=CNC2C=CC=CC1=2)=O)=O)=O)=O)CCCCN)=O)NC([C@@H]1CCCN1)=O
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| InChi Key |
DDRPLNQJNRBRNY-WYYADCIBSA-N
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| InChi Code |
InChI=1S/C81H113N19O19S2/c1-46(103)67-80(117)95-59(38-49-24-9-4-10-25-49)73(110)96-62(42-101)76(113)97-63(43-102)77(114)99-65(79(116)90-56(81(118)119)30-15-18-34-84)45-121-120-44-64(98-68(105)53-31-19-35-86-53)78(115)89-54(28-13-16-32-82)69(106)94-61(40-66(85)104)75(112)92-57(36-47-20-5-2-6-21-47)71(108)91-58(37-48-22-7-3-8-23-48)72(109)93-60(39-50-41-87-52-27-12-11-26-51(50)52)74(111)88-55(70(107)100-67)29-14-17-33-83/h2-12,20-27,41,46,53-65,67,86-87,101-103H,13-19,28-40,42-45,82-84H2,1H3,(H2,85,104)(H,88,111)(H,89,115)(H,90,116)(H,91,108)(H,92,112)(H,93,109)(H,94,106)(H,95,117)(H,96,110)(H,97,113)(H,98,105)(H,99,114)(H,100,107)(H,118,119)/t46-,53+,54+,55+,56+,57+,58+,59+,60+,61+,62+,63+,64+,65+,67+/m1/s1
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| Chemical Name |
(2S)-6-amino-2-[[(4R,7S,10S,13S,16S,19S,22S,25S,28S,31S,34S,37R)-19,34-bis(4-aminobutyl)-31-(2-amino-2-oxoethyl)-13,25,28-tribenzyl-16-[(1R)-1-hydroxyethyl]-7,10-bis(hydroxymethyl)-22-(1H-indol-3-ylmethyl)-6,9,12,15,18,21,24,27,30,33,36-undecaoxo-37-[[(2S)-pyrrolidine-2-carbonyl]amino]-1,2-dithia-5,8,11,14,17,20,23,26,29,32,35-undecazacyclooctatriacontane-4-carbonyl]amino]hexanoic acid
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| Synonyms |
CST-14; CST14; CST 14
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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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 0.5811 mL | 2.9053 mL | 5.8105 mL | |
| 5 mM | 0.1162 mL | 0.5811 mL | 1.1621 mL | |
| 10 mM | 0.0581 mL | 0.2905 mL | 0.5811 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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