| 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 |
NK2 NK3
Eledoisin targets neurokinin receptors, exhibiting vasodilatory and bronchoconstrictive activities. It binds neurokinin receptors. It is a natural tachykinin and neurokinin A receptor ligand. By activating neurokinin receptors, it modulates various physiological processes, including vasodilation, smooth muscle contraction, and pain transmission. |
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| ln Vitro |
Eledoisin, also known as eledone peptide, raises the value measured under basal conditions by 24.5±3.7%; however, the concurrent presence of CP99994 considerably (P<0.01) reduces this stimulation to 13.1±1.9%. The sensitivity of Eledoisin stimulation to 0.1 μM SR48968 or 0.1 μM SB222200 is also measured using the same procedure. While SB222200 has little impact, SR48968 significantly (P < 0.01) reduces the stimulation caused by eledoisin. NK1 and NK2 antagonists, CP99994 and SR48968, respectively, decrease elegiosin stimulation[1].
In vitro, Eledoisin binds neurokinin receptors. It contracts smooth muscles, such as those in the bladder. It causes vasodilation and induces gastric contractions. Its activity is typically assessed in smooth muscle contraction assays and receptor binding studies. As a tachykinin, it shares the conserved COOH-terminal structure of the family. |
| ln Vivo |
When rats are treated with eledoisin (Eledone peptide; 0.1–1 nmol/kg), their cardiovascular responses are biphasic, with a drop in systemic blood pressure (8–15 mm Hg) and a subsequent rise (20–22 mm Hg). Mice's scratching and grooming behaviors are enhanced by intracerebroventricular injection of elidomycin[2].
In vivo, Eledoisin is a potent vasodilating peptide. It causes vasodilation in vivo and induces gastric contractions. At low doses, it exhibits vasodilatory and bronchoconstrictive activities. It increases the value recorded under basal conditions by 24.5±3.7%. It is used in research to study the role of tachykinins in various physiological processes. |
| Enzyme Assay |
For non-cell-based receptor binding assays, Eledoisin can be evaluated using membrane preparations from cells expressing neurokinin receptors. Radioligand binding displacement experiments are performed using a suitable radiolabeled ligand such as [125I]-Neurokinin A or [3H]-Substance P. Membrane homogenates are incubated with increasing concentrations of the test compound and a fixed concentration of the radioligand. Bound radioligand is separated from free by rapid filtration through glass fiber filters. Non-specific binding is determined in the presence of excess unlabeled ligand. Ki values are calculated from displacement curves using nonlinear regression analysis.
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| Cell Assay |
For in vitro cellular assays, cells expressing neurokinin receptors are cultured in appropriate media. For functional assays, calcium mobilization is measured using fluorescent calcium indicators. Cells are loaded with the dye and treated with various concentrations of Eledoisin. Fluorescence intensity is measured using a fluorescence plate reader. The increase in calcium signal compared to control wells indicates agonist activity. EC50 values are calculated from dose-response curves. For smooth muscle contraction assays, isolated tissue preparations are used.
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| Animal Protocol |
For in vivo animal studies, Eledoisin can be administered to rodents via intravenous or intraperitoneal injection. In models of vasodilation, its effects on blood pressure and vascular tone are assessed. In models of smooth muscle contraction, its effects on gastric and bladder motility are evaluated. Dosing regimens vary depending on the specific model and desired exposure levels.
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| ADME/Pharmacokinetics |
Metabolism / Metabolites
Free toxins can be cleared through opsonization by the reticuloendothelial system (mainly in the liver and kidneys) and degraded through endocytosis by lysosomes. Lysosomes are membrane-bound organelles containing various digestive enzymes, including several proteases. Eledoisin has a molecular weight of 1188.44. It is an undecapeptide of mollusk origin. The compound should be stored according to the manufacturer's recommendations. It is for research use only and is not intended for human consumption. |
| Toxicity/Toxicokinetics |
Toxicity Summary
Aledoxine is a tachykinin. Tachykinins can excite neurons, induce behavioral responses, and are potent vasodilators and secretagogues. They can also (directly or indirectly) contract various smooth muscles. These effects are achieved by acting on three tachykinin receptors (T170, L1109, and L1717). The toxicity profile of Eledoisin has not been extensively reported. As a tachykinin peptide, potential adverse effects may include modulation of neurokinin signaling, vasodilation, and bronchoconstriction. The compound is for research use only and is not intended for human consumption. Standard safety precautions should be observed when handling the compound. |
| References | |
| Additional Infomation |
Eledoisin is a peptide. It is a peptide extracted from or synthesized from the postsalivary glands of certain small octopuses (Eledoisin, mollusks). Its action is similar to substance P; it is a potent vasodilator that increases capillary permeability. (Excerpt from Martindale Pharmacopoeia, 30th edition, page 1364)
Eledoisin (Eledone peptide, CAS 69-25-0) is an undecapeptide of mollusk origin that belongs to the tachykinin family of neuropeptides. It was first isolated from the posterior salivary glands of Eledone species. It is a potent vasodilating peptide and natural tachykinin and neurokinin A receptor ligand. It is available for research purposes only. |
| Molecular Formula |
C54H85N13O15S
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|---|---|
| Molecular Weight |
1188.40
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| Exact Mass |
1187.6
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| CAS # |
69-25-0
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| PubChem CID |
10328936
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| Appearance |
White to off-white solid powder
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| Density |
1.3±0.1 g/cm3
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| Boiling Point |
1618.1±65.0 °C at 760 mmHg
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| Flash Point |
932.4±34.3 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.569
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| LogP |
-1.36
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| Hydrogen Bond Donor Count |
14
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| Hydrogen Bond Acceptor Count |
17
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| Rotatable Bond Count |
36
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| Heavy Atom Count |
83
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| Complexity |
2270
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| Defined Atom Stereocenter Count |
11
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| SMILES |
CC[C@H](C)[C@@H](C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](C)NC(=O)[C@H](CC(=O)O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@@H]2CCCN2C(=O)[C@@H]3CCC(=O)N3
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| InChi Key |
AYLPVIWBPZMVSH-FCKMLYJASA-N
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| InChi Code |
InChI=1S/C54H85N13O15S/c1-7-30(4)44(53(81)57-27-42(70)60-36(24-29(2)3)49(77)61-33(45(56)73)20-23-83-6)66-50(78)37(25-32-14-9-8-10-15-32)63-46(74)31(5)58-48(76)38(26-43(71)72)64-47(75)34(16-11-12-21-55)62-51(79)39(28-68)65-52(80)40-17-13-22-67(40)54(82)35-18-19-41(69)59-35/h8-10,14-15,29-31,33-40,44,68H,7,11-13,16-28,55H2,1-6H3,(H2,56,73)(H,57,81)(H,58,76)(H,59,69)(H,60,70)(H,61,77)(H,62,79)(H,63,74)(H,64,75)(H,65,80)(H,66,78)(H,71,72)/t30-,31-,33-,34-,35-,36-,37-,38-,39-,40-,44-/m0/s1
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| Chemical Name |
(3S)-3-[[(2S)-6-amino-2-[[(2S)-3-hydroxy-2-[[(2S)-1-[(2S)-5-oxopyrrolidine-2-carbonyl]pyrrolidine-2-carbonyl]amino]propanoyl]amino]hexanoyl]amino]-4-[[(2S)-1-[[(2S)-1-[[(2S,3S)-1-[[2-[[(2S)-1-[[(2S)-1-amino-4-methylsulfanyl-1-oxobutan-2-yl]amino]-4-methyl-1-oxopentan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-1-oxopropan-2-yl]amino]-4-oxobutanoic 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: 18.15 mg/mL (15.27 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 | 0.8415 mL | 4.2073 mL | 8.4147 mL | |
| 5 mM | 0.1683 mL | 0.8415 mL | 1.6829 mL | |
| 10 mM | 0.0841 mL | 0.4207 mL | 0.8415 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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