| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
Prolyl endopeptidase inhibitor 2 targets prolyl endopeptidase (PEP, EC 3.4.21.26), also known as prolyl oligopeptidase (PREP). PEP is a serine protease that cleaves peptide bonds at the C-terminal side of proline residues in peptides smaller than 30 amino acids. Substrates include neuropeptides such as arginine-vasopressin, thyrotropin-releasing hormone (TRH), and substance P, as well as peptides involved in learning, memory, and cell proliferation. Inhibition of PEP may influence these neuropeptide levels.
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| ln Vitro |
In vitro, Prolyl endopeptidase inhibitor 2 (Compound 8) has been characterized as a prolyl endopeptidase (PEP) inhibitor with an IC50 value of 31.11 microM. This potency indicates that it is a relatively moderate inhibitor of PEP activity. No specific cellular activity data (e.g., effects on neuropeptide levels in neuronal cultures) are reported in the search results. The compound is a chemical tool for studying the biological roles of PEP in cellular models of neurodegenerative diseases.
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| ln Vivo |
No specific in vivo activity data for Prolyl endopeptidase inhibitor 2 are reported in the search results. However, based on its mechanism of action as a PEP inhibitor, it has potential applications in research models of neurodegenerative diseases such as Alzheimer‘s disease, Parkinson's disease, and amyotrophic lateral sclerosis (ALS). In animal models, PEP inhibitors can affect memory and learning by increasing the levels of certain neuropeptides. Specific dosing and efficacy data are not available from the search results.
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| Enzyme Assay |
The binding of Prolyl endopeptidase inhibitor 2 to PEP is measured by standard in vitro enzyme activity assays using purified recombinant PEP enzyme. The compound is incubated with the enzyme and a specific fluorogenic peptide substrate, typically Suc-Gly-Pro-AMC (succinyl-glycyl-proline-7-amido-4-methylcoumarin). Substrate cleavage by PEP releases the fluorescent AMC group, which is measured at λex=380 nm and λem=460 nm. The IC50 value (31.11 microM) is calculated from dose-response curves (0.1-1000 microM) by measuring the decrease in fluorescence over time.
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| Cell Assay |
No cellular experiments for Prolyl endopeptidase inhibitor 2 are described in the search results. For cellular studies of PEP inhibition, human neuroblastoma cell lines (e.g., SH-SY5Y, IMR-32) or primary cortical neurons would be seeded in 6- or 96-well plates. Cells would be treated with the compound at graded concentrations (1-100 microM) for 24-72 hours. PEP activity in cell lysates would be measured using the Suc-Gly-Pro-AMC fluorogenic substrate. Cellular levels of PEP substrates such as substance P, TRH, or vasopressin would be measured by ELISA. Cell viability would be assessed by MTT or LDH assays.
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| Animal Protocol |
No animal experiments for Prolyl endopeptidase inhibitor 2 are described in the search results. For in vivo evaluation of PEP inhibition in neurodegenerative disease models, 6-8-week-old male C57BL/6 mice or transgenic mouse models (e.g., 5xFAD for Alzheimer‘s disease, MPTP-treated for Parkinson‘s disease) would be used. The compound would be administered intraperitoneally (IP, 10-50 mg/kg) or orally (20-100 mg/kg) daily for 2-4 weeks. After treatment, brain regions (cortex, hippocampus, striatum) would be collected. PEP activity would be measured in brain homogenates using the fluorogenic substrate. Levels of neuropeptides (substance P, TRH, vasopressin) would be quantified by ELISA. Behavioral tests (Morris water maze for memory, rotarod for motor function) would be performed.
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| ADME/Pharmacokinetics |
Prolyl endopeptidase inhibitor 2 (C4₆H32Br2N₈O2, MW = 888.61, CAS 2362592-81-0) is a solid powder. For storage, the compound should be kept at 4degC and protected from light. For in vitro use, stock solutions in DMSO (10-50 mM) can be stored at -20degC for up to 1 month or at -80degC for up to 6 months. For in vivo use, it can be formulated in 10% DMSO / 40% PEG300 / 5% Tween-80 / 45% saline or 0.5% methylcellulose/0.1% Tween-80. Purity is typically ≥98% (HPLC). No detailed PK parameters (oral bioavailability, Cmax, Tmax, half-life) are reported.
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| Toxicity/Toxicokinetics |
No specific toxicity data for Prolyl endopeptidase inhibitor 2 are reported in the search results. As a research-grade compound, it is not intended for human or veterinary use. Standard laboratory safety precautions for handling chemicals should be followed, including the use of gloves, lab coat, and safety goggles. No LD50 or formal toxicology studies are available. The compound contains bromine atoms, which may contribute to potential toxicity.
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| References | |
| Additional Infomation |
Prolyl endopeptidase (PEP, also known as prolyl oligopeptidase, PREP) is a serine protease that cleaves proline-containing peptides. PEP is highly expressed in the brain and is thought to be involved in the metabolism of neuropeptides that regulate learning and memory. PEP inhibitors have been investigated as potential therapeutic agents for neurodegenerative and psychiatric disorders, including Alzheimer‘s disease, Parkinson's disease, and schizophrenia. Prolyl endopeptidase inhibitor 2 (Compound 8) is a research-use only tool for studying these conditions. It has not entered clinical trials or received regulatory approval. It is available from chemical suppliers with purity typically ≥98%.
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| Molecular Formula |
C46H32BR2N8O2
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| Molecular Weight |
888.61
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| Exact Mass |
888.099
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| CAS # |
2362592-81-0
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| PubChem CID |
171391417
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| Appearance |
White to light yellow solid powder
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| Hydrogen Bond Donor Count |
0
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| Rotatable Bond Count |
11
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| Heavy Atom Count |
58
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| Complexity |
1320
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C2C(=C1)C3=C(N2CC4=CN(N=N4)CC(=O)C5=CC=C(C=C5)Br)C=CC(=C3)C6=CC7=C(C=C6)N(C8=CC=CC=C87)CC9=CN(N=N9)CC(=O)C1=CC=C(C=C1)Br
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| InChi Key |
VTXFSJDLVDEEHU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C46H32Br2N8O2/c47-33-15-9-29(10-16-33)45(57)27-53-23-35(49-51-53)25-55-41-7-3-1-5-37(41)39-21-31(13-19-43(39)55)32-14-20-44-40(22-32)38-6-2-4-8-42(38)56(44)26-36-24-54(52-50-36)28-46(58)30-11-17-34(48)18-12-30/h1-24H,25-28H2
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| Chemical Name |
1-(4-bromophenyl)-2-[4-[[3-[9-[[1-[2-(4-bromophenyl)-2-oxoethyl]triazol-4-yl]methyl]carbazol-3-yl]carbazol-9-yl]methyl]triazol-1-yl]ethanone
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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 | 1.1254 mL | 5.6268 mL | 11.2535 mL | |
| 5 mM | 0.2251 mL | 1.1254 mL | 2.2507 mL | |
| 10 mM | 0.1125 mL | 0.5627 mL | 1.1254 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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