| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
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| Other Sizes |
| Targets |
IC50: 0.12 nM (TREK-1)[1]
TREK-1 (potassium channel subfamily K member 2) (IC50 = 0.12 nM). |
|---|---|
| ln Vitro |
With an IC50 value of 0.12 nM, PE 22-28 exhibits strong TREK-1 channel selectivity and affinity[1].
PE 22-28 displays good specificity and affinity for the TREK-1 channel with an IC50 value of 0.12 nM. It is a short peptide that serves as a core sequence for developing analogs through chemical modification and amino acid substitution. |
| ln Vivo |
PE 22-28 exhibits antidepressant properties (ip; 3.0µg/kg)[1].
PE 22-28 (i.p.; 3.0 ug/kg) shows antidepressant properties in rodent models of depression. It significantly reduces immobility time in the forced swim test, decreases the latency to eat in the novelty-suppressed feeding test, induces neurogenesis, and improves the duration of action. |
| Enzyme Assay |
For receptor binding, membranes from cells expressing human TREK-1 channels are incubated with a radioligand like [125I]-spadin or a fluorescent tracer in the presence of varying concentrations of PE 22-28. The reaction is terminated by rapid filtration, and bound radioactivity is measured.
|
| Cell Assay |
HEK293 cells stably expressing TREK-1 channels are cultured in DMEM with 10% FBS. Whole-cell patch-clamp electrophysiology is performed. The peptide is applied to the bath solution, and the inhibition of potassium current is measured. IC50 values are calculated from dose-response curves.
|
| Animal Protocol |
Animal/Disease Models: Naïve male C57Bl/6J mice[1]
Doses: 3.0µg/kg Route of Administration: intraperitoneal (ip) Experimental Results: demonstrated a significant reduction of the immobility time , decreased Dramatically the latency to eat the food pellet, induced neurogenesis and improved the action duration. PE 22-28 is formulated in saline or PBS and administered intraperitoneally (i.p.) to male C57Bl/6J mice at a dose of 3.0 ug/kg. The animals are then tested in behavioral paradigms such as the forced swim test (FST) and tail suspension test (TST) to assess antidepressant-like activity. |
| ADME/Pharmacokinetics |
As a 7-amino-acid peptide, PE 22-28 has a molecular weight of 773.89 and is rapidly cleared from the bloodstream via renal filtration and proteolytic degradation, resulting in a short half-life. It is stable enough for in vivo studies, and its formulation in saline allows direct IP administration.
|
| Toxicity/Toxicokinetics |
PE 22-28 is generally well-tolerated at the tested low doses. Its primary toxicity is related to its target pharmacology, which may affect neuronal excitability. Specific toxicological data is limited. It is intended for research use only.
|
| References |
[1]. Alaeddine Djillani, et al. Shortened Spadin Analogs Display Better TREK-1 Inhibition, In Vivo Stability and Antidepressant Activity. Front Pharmacol. 2017 Sep 12;8:643.
|
| Additional Infomation |
PE 22-28 is a potent and selective TREK-1 channel antagonist. It has potential as a therapeutic agent for major depressive disorder and has been shown to be more effective than classical antidepressants in some models, with a faster onset of action.
|
| Molecular Formula |
C35H55N11O9
|
|---|---|
| Molecular Weight |
773.879507303238
|
| Exact Mass |
773.418
|
| CAS # |
1801959-12-5
|
| PubChem CID |
165437303
|
| Appearance |
Typically exists as solid at room temperature
|
| LogP |
-3.7
|
| Hydrogen Bond Donor Count |
12
|
| Hydrogen Bond Acceptor Count |
11
|
| Rotatable Bond Count |
23
|
| Heavy Atom Count |
55
|
| Complexity |
1360
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
CC(C)C[C@@H](C(=O)N[C@@H](CCCN=C(N)N)C(=O)O)NC(=O)CNC(=O)[C@H](CC1=CNC2=CC=CC=C21)NC(=O)[C@H](CO)NC(=O)[C@H](C(C)C)NC(=O)CN
|
| InChi Key |
CMNBQRXBBJQIOA-YIHYGEMESA-N
|
| InChi Code |
InChI=1S/C35H55N11O9/c1-18(2)12-24(31(51)43-23(34(54)55)10-7-11-39-35(37)38)42-28(49)16-41-30(50)25(13-20-15-40-22-9-6-5-8-21(20)22)44-32(52)26(17-47)45-33(53)29(19(3)4)46-27(48)14-36/h5-6,8-9,15,18-19,23-26,29,40,47H,7,10-14,16-17,36H2,1-4H3,(H,41,50)(H,42,49)(H,43,51)(H,44,52)(H,45,53)(H,46,48)(H,54,55)(H4,37,38,39)/t23-,24-,25-,26-,29-/m0/s1
|
| Chemical Name |
(2S)-2-[[(2S)-2-[[2-[[(2S)-2-[[(2S)-2-[[(2S)-2-[(2-aminoacetyl)amino]-3-methylbutanoyl]amino]-3-hydroxypropanoyl]amino]-3-(1H-indol-3-yl)propanoyl]amino]acetyl]amino]-4-methylpentanoyl]amino]-5-(diaminomethylideneamino)pentanoic acid
|
| 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 |
| 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) |
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
|
|---|---|
| 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 | 1.2922 mL | 6.4610 mL | 12.9219 mL | |
| 5 mM | 0.2584 mL | 1.2922 mL | 2.5844 mL | |
| 10 mM | 0.1292 mL | 0.6461 mL | 1.2922 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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