| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg | |||
| Other Sizes |
| Targets |
Cortistatin-14 targets somatostatin receptors (sst1 through sst5) as well as the ghrelin receptor. It binds to all five cloned somatostatin receptor subtypes (SSTR1-SSTR5) with IC50 values ranging from 0.5 to 18.2 nM for human receptors expressed in CCL39 cells. The compound also activates the ghrelin receptor and interacts with GABA(A/B) receptors. Through these receptor interactions, Cortistatin-14 modulates neuronal excitability, sleep patterns, and inflammatory responses in the central nervous system.
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| ln Vitro |
Cortistatin-14 demonstrates potent binding affinity to somatostatin receptors with IC50 values of 0.5-18.2 nM for human SST1-SST5 receptors. In isolated rat trachea preparations, Cortistatin-14 (100-10000 nM, 8-24 min) reduces capsaicin-induced release of calcitonin gene-related peptide from peripheral sensory nerve endings. The compound exhibits anticonvulsive properties and significant anti-inflammatory activity through its receptor-mediated actions. Its neuroprotective effects have been demonstrated in various in vitro neuronal models.
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| ln Vivo |
Cortistatin-14 shows in vivo anticonvulsive and neuroprotective effects. Subcutaneous administration of Cortistatin-14 (40-320 microg/kg) dose-dependently reduces growth hormone secretion in rats by greater than 80% within 10 minutes post-administration. Intracerebroventricular administration produces rapid antidepressant effects. The compound impairs recognition memory consolidation in mice through activation of sst(2), ghrelin, and GABA(A/B) receptors. Cortistatin-14 is being investigated for its potential in sepsis-induced cognitive impairment and other neurological disorders.
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| Enzyme Assay |
Receptor binding assays are performed using membrane preparations from CCL39 cells expressing human recombinant somatostatin receptor subtypes (SST1-SST5). Radioligand binding experiments are conducted using [125I]somatostatin-14 or [125I]Tyr11-somatostatin-14 as the tracer. Membranes are incubated with varying concentrations of Cortistatin-14 and a fixed concentration of radioligand in assay buffer at room temperature for 60-120 minutes. Nonspecific binding is determined in the presence of excess unlabeled somatostatin-14. Bound radioactivity is separated by filtration and counted to determine IC50 values.
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| Cell Assay |
Cellular assays are conducted using CCL39 cells or CHO-K1 cells stably expressing human somatostatin receptor subtypes. Cells are cultured in appropriate media and seeded into multi-well plates. For functional assays, cells are treated with Cortistatin-14 at various concentrations, and receptor activation is measured by assessing intracellular calcium mobilization, cAMP accumulation, or GTPgammaS binding. Anti-inflammatory activity is evaluated in macrophage or microglial cell cultures by measuring cytokine production and NF-kappaB activation following Cortistatin-14 treatment.
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| Animal Protocol |
In vivo studies are performed in rodent models including rats and mice. Cortistatin-14 is administered via subcutaneous, intraperitoneal, or intracerebroventricular routes at doses ranging from 40-320 microg/kg. For anticonvulsant studies, animals are challenged with chemoconvulsants and seizure parameters are monitored. For cognitive studies, recognition memory is assessed using novel object recognition or other behavioral paradigms. For sepsis-induced cognitive impairment models, animals are subjected to cecal ligation and puncture or LPS administration followed by Cortistatin-14 treatment and cognitive testing.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for Cortistatin-14 are limited in public literature. As a neuropeptide, it is expected to have limited oral bioavailability and may be subject to rapid proteolytic degradation in the gastrointestinal tract and circulation. Intracerebroventricular administration bypasses the blood-brain barrier and allows direct central nervous system exposure. Subcutaneous administration of Cortistatin-14 (40-320 microg/kg) produces dose-dependent pharmacological effects within 10 minutes, suggesting relatively rapid absorption and onset of action.
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| Toxicity/Toxicokinetics |
Comprehensive toxicology data for Cortistatin-14 are not extensively documented. The compound is for research use only and has not been evaluated in formal toxicology studies for clinical development. In preclinical studies, Cortistatin-14 has been administered at various doses without reported significant adverse effects. Standard laboratory safety practices should be followed when handling this compound, including the use of appropriate personal protective equipment and adherence to institutional biosafety guidelines for peptide research compounds.
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| References |
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| Additional Infomation |
Cortistatin-14 is an endogenous cyclic neuropeptide (CST-14) being studied for its neurological and anti-inflammatory properties. It binds to all five somatostatin receptor subtypes and the ghrelin receptor, exhibiting anticonvulsive, neuroprotective, and anti-inflammatory activities. The compound is being investigated for applications in sepsis-induced cognitive impairment and other neurological disorders. Cortistatin-14 is for research purposes only and has not been approved for therapeutic use.
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| Molecular Formula |
C81H113N19O19S2
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|---|---|
| Molecular Weight |
1721.00982
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| Exact Mass |
1719.79
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| CAS # |
186901-48-4
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| Related CAS # |
Cortistatin-14 TFA
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| PubChem CID |
16133803
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| Appearance |
White to off-white solid powder
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| LogP |
3.128
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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 |
C[C@H]([C@H]1C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@@H](CSSC[C@@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N[C@H](C(=O)N1)CCCCN)CC2=CNC3=CC=CC=C32)CC4=CC=CC=C4)CC5=CC=CC=C5)CC(=O)N)CCCCN)NC(=O)[C@@H]6CCCN6)C(=O)N[C@@H](CCCCN)C(=O)O)CO)CO)CC7=CC=CC=C7)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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| 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 : ~100 mg/mL (~58.14 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 100 mg/mL (58.14 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(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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