| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 25mg |
|
||
| 50mg | |||
| 100mg | |||
| Other Sizes |
| Targets |
Neuropeptide; antioxidant; anxiolytic
The primary targets of δ-Sleep Inducing Peptide are believed to be located in the central nervous system, particularly in areas involved in sleep regulation such as the hypothalamus and brainstem. DSIP may interact with specific receptors or modulate neurotransmitter systems involved in sleep-wake regulation, including GABA, serotonin, and dopamine pathways. The peptide also affects the hypothalamic-pituitary-adrenal (HPA) axis and may modulate stress responses. |
|---|---|
| ln Vitro |
In vitro studies have shown that DSIP affects neurotransmitter release and receptor binding in brain tissue preparations. The peptide modulates the activity of GABAergic and serotonergic systems, which are involved in sleep regulation. DSIP has also been shown to affect the release of corticotropin-releasing hormone (CRH) and other neuropeptides. In cell culture, DSIP may have neuroprotective effects, protecting neurons from oxidative stress and excitotoxicity.
|
| ln Vivo |
In rabbits, δ-Sleep Inducing Peptide (DSIP) causes modest reductions in cardiac and respiratory rates together with enhanced spindle activity [1]. When administered intraperitoneally to rats and acute stress rats at a dose of 40 μg/kg, δ-Sleep Inducing Peptide (DSIP; 40-360 μg/kg) increases the activities of catalase and superoxide dismutase (SOD) at a concentration of malondialdehyde (MDA) in liver homogenates. However, at 120 μg/kg and 360 μg/kg, the opposite effects were noted [2].
In vivo studies in animal models have demonstrated that DSIP induces sleep-like states and alters sleep architecture. Administration of DSIP to animals results in increased slow-wave sleep and reduced sleep latency. The peptide also affects the HPA axis, reducing stress-induced corticosterone release. DSIP has been shown to have analgesic effects in pain models and neuroprotective effects in models of neurodegenerative diseases. These effects have been observed in various species including rats, rabbits, and humans. |
| Enzyme Assay |
Non-cellular assays for DSIP typically involve receptor binding studies using radiolabeled DSIP or competition binding assays with brain membrane preparations. These assays determine the binding affinity and specificity of DSIP for potential receptors. The peptide's stability in biological fluids is assessed by incubating it in serum or cerebrospinal fluid and measuring its degradation over time using HPLC or mass spectrometry.
|
| Cell Assay |
Cellular assays for DSIP are conducted using neuronal cell lines or primary neuronal cultures. The peptide's effects on cell viability, neurotransmitter release, and signaling pathways are assessed. Neuroprotective effects are evaluated by exposing cells to oxidative stress or excitotoxic insults in the presence or absence of DSIP. Receptor activation is assessed by measuring changes in intracellular calcium or cAMP levels.
|
| Animal Protocol |
In vivo animal experiments for DSIP typically involve administration of the peptide via intracerebroventricular (ICV), intravenous, or intraperitoneal injection. Sleep parameters are measured using electroencephalography (EEG) and electromyography (EMG). Stress responses are assessed by measuring plasma corticosterone levels. Pain sensitivity is evaluated using standard pain models such as the hot plate or tail flick tests. Neuroprotective effects are assessed in models of stroke or neurodegeneration.
|
| ADME/Pharmacokinetics |
Pharmacokinetic studies of DSIP have shown that the peptide has a short half-life in circulation due to rapid degradation by peptidases. The peptide penetrates the blood-brain barrier to some extent, although the efficiency of penetration is limited. For research applications, DSIP is typically administered directly into the brain (ICV) to achieve sufficient concentrations in the central nervous system. The peptide's stability can be enhanced by formulation or by using protease inhibitors.
|
| Toxicity/Toxicokinetics |
Toxicological data for DSIP are limited, as the peptide is used primarily as a research tool. No significant toxicity has been reported at the doses used in research studies. The peptide is generally well-tolerated, and adverse effects have not been extensively documented. Standard laboratory safety precautions should be followed when handling the peptide. The compound is not approved for human use.
|
| References |
|
| Additional Infomation |
We investigated the effects of δ-sleep-inducing peptide (intraperitoneal injection 1 hour before the experiment at doses of 40, 120, and 360 μg/kg) on liver free radical oxidation, aminotransferase activity, and serum total protein content in male Wistar rats under restraint stress. Under acute stress, δ-sleep-inducing peptide at a dose of 40 μg/kg increased the activity of catalase and superoxide dismutase (SOD) and the concentration of malondialdehyde (MDA) in liver homogenate. No significant changes were observed at other doses of δ-sleep-inducing peptide. Under chronic stress, the effect of δ-sleep-inducing peptide at a dose of 40 μg/kg was the most significant. At this time, the activity of catalase and SOD and the concentration of MDA decreased, while the activity of aminotransferase and the serum total protein content remained unchanged. δ-sleep-inducing peptide at a dose of 120 μg/kg decreased the activity of SOD and the concentration of MDA, increased the serum total protein content, and decreased the activity of aspartate aminotransferase (AST). Increasing the dose of peptide to 360 μg/kg eliminated its effect. [2]
Other information includes DSIP's role as a neuropeptide involved in sleep regulation and stress modulation. It was discovered in the 1970s and has been the subject of numerous studies investigating its physiological functions and potential therapeutic applications. The peptide has been studied for potential use in sleep disorders, stress-related conditions, pain management, and neurodegenerative diseases. However, it has not received regulatory approval for any clinical indication. DSIP remains a valuable research tool for studying sleep and neuropeptide biology. |
| Molecular Formula |
C37H52N10O17
|
|---|---|
| Molecular Weight |
908.87
|
| Exact Mass |
908.35119023
|
| Related CAS # |
δ-Sleep Inducing Peptide;62568-57-4
|
| PubChem CID |
163337005
|
| Sequence |
H-Trp-Ala-Gly-Gly-Asp-Ala-Ser-Gly-Glu-OH.CH3CO2H; L-tryptophyl-L-alanyl-glycyl-glycyl-L-alpha-aspartyl-L-alanyl-L-seryl-glycyl-L-glutamic acid acetic acid
|
| SequenceShortening |
WAGGDASGE
|
| Appearance |
White to off-white solid powder
|
| Hydrogen Bond Donor Count |
15
|
| Hydrogen Bond Acceptor Count |
18
|
| Rotatable Bond Count |
25
|
| Heavy Atom Count |
64
|
| Complexity |
1640
|
| Defined Atom Stereocenter Count |
6
|
| SMILES |
C[C@@H](C(=O)NCC(=O)NCC(=O)N[C@@H](CC(=O)O)C(=O)N[C@@H](C)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CCC(=O)O)C(=O)O)NC(=O)[C@H](CC1=CNC2=CC=CC=C21)N.CC(=O)O
|
| InChi Key |
PMAPMBRAJAMLEE-BMMXBKKXSA-N
|
| InChi Code |
InChI=1S/C35H48N10O15.C2H4O2/c1-16(41-32(56)20(36)9-18-11-37-21-6-4-3-5-19(18)21)30(54)39-12-25(47)38-13-26(48)44-23(10-29(52)53)34(58)42-17(2)31(55)45-24(15-46)33(57)40-14-27(49)43-22(35(59)60)7-8-28(50)51;1-2(3)4/h3-6,11,16-17,20,22-24,37,46H,7-10,12-15,36H2,1-2H3,(H,38,47)(H,39,54)(H,40,57)(H,41,56)(H,42,58)(H,43,49)(H,44,48)(H,45,55)(H,50,51)(H,52,53)(H,59,60);1H3,(H,3,4)/t16-,17-,20-,22-,23-,24-;/m0./s1
|
| Chemical Name |
acetic acid;(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[[2-[[2-[[(2S)-2-[[(2S)-2-amino-3-(1H-indol-3-yl)propanoyl]amino]propanoyl]amino]acetyl]amino]acetyl]amino]-3-carboxypropanoyl]amino]propanoyl]amino]-3-hydroxypropanoyl]amino]acetyl]amino]pentanedioic acid
|
| Synonyms |
Emideltide (acetate); DSIP ACETATE; AT42481
|
| HS Tariff Code |
2934.99.9001
|
| 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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
| Solubility (In Vitro) |
H2O :~100 mg/mL (~110.03 mM)
|
|---|---|
| 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 | 1.1003 mL | 5.5013 mL | 11.0027 mL | |
| 5 mM | 0.2201 mL | 1.1003 mL | 2.2005 mL | |
| 10 mM | 0.1100 mL | 0.5501 mL | 1.1003 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
