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| Targets |
Z-321 targets prolyl endopeptidase (PREP), an enzyme that cleaves peptide bonds on the carboxyl side of proline residues. PREP is involved in the metabolism of various neuropeptides, including those that are important for learning and memory. By inhibiting PREP, Z-321 can modulate the levels of these neuropeptides and affect synaptic transmission.
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| ln Vitro |
In vitro, Z-321 is characterized as an inhibitor of prolyl endopeptidase. Its activity is assessed in enzyme activity assays using purified PREP or tissue homogenates. It is not a drug with a typical "activity" in cell proliferation assays; its activity is defined by its ability to inhibit the enzymatic activity of PREP. It has been shown to augment the potentiation of synaptic transmission in rat hippocampal slices.
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| ln Vivo |
Z-321 is an inhibitor of prolyl peptidase (PEP). Following dosage, the mean lordosis quotient (LQ) dropped in the 100 or 200 mg/kg Z-321 treatment groups. Still, there was no statistically significant change between the pre- and post-values. On the other hand, females treated with 300 mg/kg Z-321 had a mean lower LQ than they had before to injection (P<0.005). Furthermore, there was a substantial decrease in mean LQ when compared to controls treated with a vehicle (p<0.05). There was no statistically significant difference in the occurrence of solicitation behavior after treatment with 300 mg/kg Z-321 compared to before treatment. Additionally, this study demonstrates that Z-321 at a dose of 300 mg/kg can successfully suppress lordosis behavior without impairing motor function [1].
In vivo, Z-321 has been studied for its effects on learning and memory. By inhibiting PREP, it can modulate the levels of neuropeptides that are involved in cognitive function. Its effects on synaptic transmission in the hippocampus suggest it could have potential for treating cognitive disorders. |
| Enzyme Assay |
The in vitro activity of Z-321 against prolyl endopeptidase is determined using enzyme activity assays. In a cell-free protocol, the PREP enzyme is incubated with a fluorogenic substrate (e.g., Z-Gly-Pro-AMC) and varying concentrations of Z-321. The cleavage of the substrate releases a fluorescent product, which is measured. The IC50 for enzyme inhibition is then calculated.
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| Cell Assay |
Cellular assays for Z-321 involve studying its effects on PREP activity in cells or tissue slices. In a typical protocol, rat hippocampal slices are treated with Z-321, and the effect on synaptic transmission is measured using electrophysiological techniques, such as recording field excitatory postsynaptic potentials (fEPSPs).
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| Animal Protocol |
The in vivo activity of Z-321 can be evaluated in animal models of learning and memory. In a typical protocol, rodents are administered Z-321, and their performance in behavioral tests, such as the Morris water maze or novel object recognition test, is assessed. The compound's ability to improve cognitive function is a measure of its in vivo activity.
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| ADME/Pharmacokinetics |
Z-321 has a molecular weight of 344.47 and a molecular formula of C₁₉H₂₄N₂O₂S. It is a small-molecule inhibitor of prolyl endopeptidase. It is typically supplied as a powder for research use. As a research chemical, detailed pharmacokinetic data are not typically reported, as its primary use is in preclinical studies to probe PREP function.
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| Toxicity/Toxicokinetics |
The toxicity of Z-321 is not extensively documented, as it is a research tool rather than a therapeutic candidate. Standard safety precautions should be taken when handling the compound. At concentrations used in in vitro assays, it is not considered highly toxic. For in vivo studies, the dose would be carefully selected to avoid systemic toxicity.
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| References |
[1]. Oosuka I, et al. Decrease of sexual receptivity by prolylendopeptidase inhibitor in female rats. Jpn J Pharmacol. 2000 May;83(1):82-5
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| Additional Infomation |
Z-321 is an inhibitor of prolyl endopeptidase (PREP). It has been shown to augment the potentiation of synaptic transmission in rat hippocampal slices. It is a research tool used to study the role of PREP in the central nervous system, particularly in learning and memory. It is not an approved drug and has no clinical applications.
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| Molecular Formula |
C19H24N2O2S
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|---|---|
| Molecular Weight |
344.473
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| Exact Mass |
344.155
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| CAS # |
130849-58-0
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| PubChem CID |
9798234
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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 |
588.8±50.0 °C at 760 mmHg
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| Flash Point |
309.9±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.622
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| LogP |
2.6
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
24
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| Complexity |
478
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O=C([C@H]1N(C(CC2CC3=C(C=CC=C3)C2)=O)CSC1)N4CCCC4
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| InChi Key |
GDOVFSONSLOIAK-KRWDZBQOSA-N
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| InChi Code |
InChI=1S/C19H24N2O2S/c22-18(11-14-9-15-5-1-2-6-16(15)10-14)21-13-24-12-17(21)19(23)20-7-3-4-8-20/h1-2,5-6,14,17H,3-4,7-13H2/t17-/m0/s1
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| Chemical Name |
2-(2,3-dihydro-1H-inden-2-yl)-1-[(4R)-4-(pyrrolidine-1-carbonyl)-1,3-thiazolidin-3-yl]ethanone
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| Synonyms |
Z 321; Z321; Z-321
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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) |
DMSO : ~250 mg/mL (~725.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 6.25 mg/mL (18.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 6.25 mg/mL (18.14 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 6.25 mg/mL (18.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.9030 mL | 14.5151 mL | 29.0301 mL | |
| 5 mM | 0.5806 mL | 2.9030 mL | 5.8060 mL | |
| 10 mM | 0.2903 mL | 1.4515 mL | 2.9030 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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