| Size | Price | Stock | Qty |
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| Targets |
nNOS-Capon coupling. nNOS (neuronal nitric oxide synthase) is the primary source of nitric oxide (NO) in the nervous system, where it plays critical roles in neurotransmission, synaptic plasticity, and pain signaling. Capon is a protein that binds to the PDZ domain of nNOS and regulates its localization and activity. ZLc-002 is a selective inhibitor of nNOS-Capon coupling. By disrupting the interaction between nNOS and Capon, ZLc-002 modulates nNOS activity and NO production in specific neuronal compartments. (S)-ZLc002 is the S-enantiomer of ZLc-002.
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| ln Vitro |
In vitro, (S)-ZLc002 is the S-enantiomer of ZLc-002. ZLc-002 is a selective inhibitor of nNOS-Capon coupling. By inhibiting nNOS-Capon interaction, ZLc-002 modulates nNOS activity and NO production. The compound demonstrates selectivity for the nNOS-Capon interaction over other nNOS interactions or other NOS isoforms.
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| ln Vivo |
In vivo, ZLc-002 suppresses inflammatory nociception and chemotherapy-induced neuropathic pain. By inhibiting nNOS-Capon coupling, ZLc-002 reduces nNOS-mediated NO production in pain pathways, attenuating the sensitization of nociceptive neurons. The compound has been investigated for potential therapeutic applications in pain management. However, detailed in vivo efficacy data for (S)-ZLc002 specifically are limited in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding (cell-free) assay for (S)-ZLc002 typically involves measuring the inhibition of nNOS-Capon coupling using purified proteins. The assay is performed by incubating nNOS and Capon proteins in the presence of varying concentrations of (S)-ZLc002. The disruption of the nNOS-Capon interaction is measured using a fluorescence polarization or pull-down assay. The IC50 for inhibition of nNOS-Capon coupling is determined from dose-response curves.
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| Cell Assay |
In vitro cellular assays for (S)-ZLc002 are performed using neuronal cell lines or primary neurons that express nNOS and Capon. Cells are treated with varying concentrations of (S)-ZLc002, and the interaction between nNOS and Capon is assessed by immunoprecipitation or proximity ligation assays. nNOS activity is measured by assessing NO production using fluorescent NO probes or by measuring the conversion of L-arginine to L-citrulline.
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| Animal Protocol |
In vivo animal experiments for (S)-ZLc002 are conducted in rodent models of inflammatory pain and chemotherapy-induced neuropathic pain. (S)-ZLc002 is administered via oral gavage or intraperitoneal injection at various dose levels. Pain-related behaviors, such as mechanical allodynia and thermal hyperalgesia, are evaluated using von Frey filaments and hot plate tests. The compound's ability to suppress pain is determined by its effects on pain behaviors compared to vehicle-treated controls.
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| ADME/Pharmacokinetics |
Pharmacokinetic data for (S)-ZLc002 are limited. As a small molecule with a molecular weight of 231.25 g/mol and a molecular formula of C10H17NO5, the compound is expected to have moderate oral bioavailability and tissue distribution. The compound is soluble in DMSO at 100 mg/mL. Further pharmacokinetic studies would be required to fully characterize its absorption, distribution, metabolism, and excretion (ADME) properties.
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| Toxicity/Toxicokinetics |
Toxicology data for (S)-ZLc002 are limited. The compound is used for research purposes only and is not approved for human use. No significant toxicities have been reported in the available literature. As a modulator of nNOS activity, the compound may have effects on neurotransmission and cardiovascular function, requiring careful evaluation of safety for therapeutic development.
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| References | |
| Additional Infomation |
(S)-ZLc002 (CAS: 308277-46-5) is the S-enantiomer of ZLc-002. It has a molecular formula of C10H17NO5 and a molecular weight of 231.25. ZLc-002 is a selective inhibitor of nNOS-Capon coupling that suppresses inflammatory nociception and chemotherapy-induced neuropathic pain. (S)-ZLc002 is not approved for human use and is intended for research purposes only.
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| Molecular Formula |
C10H17NO5
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|---|---|
| Molecular Weight |
231.2457
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| Exact Mass |
231.11
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| CAS # |
308277-46-5
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| Related CAS # |
(Rac)-ZLc-002;ZLc-002;1446971-41-0
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| PubChem CID |
10823397
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
0.8
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
16
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| Complexity |
274
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| Defined Atom Stereocenter Count |
1
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| SMILES |
O(C([H])([H])[H])C([C@]([H])(C([H])(C([H])([H])[H])C([H])([H])[H])N([H])C(C([H])([H])C(=O)OC([H])([H])[H])=O)=O
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| InChi Key |
BWPKYDAJBOUZDX-VIFPVBQESA-N
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| InChi Code |
InChI=1S/C10H17NO5/c1-6(2)9(10(14)16-4)11-7(12)5-8(13)15-3/h6,9H,5H2,1-4H3,(H,11,12)/t9-/m0/s1
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| Chemical Name |
methyl (2S)-2-[(3-methoxy-3-oxopropanoyl)amino]-3-methylbutanoate
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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: ~100 mg/mL (~432.4 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.81 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: ≥ 2.5 mg/mL (10.81 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (25.0 mg/mL) to 900 μL of corn oil and mix well. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.3243 mL | 21.6216 mL | 43.2432 mL | |
| 5 mM | 0.8649 mL | 4.3243 mL | 8.6486 mL | |
| 10 mM | 0.4324 mL | 2.1622 mL | 4.3243 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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