| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| Other Sizes |
| 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.
|
|---|---|
| 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.
|
| 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.
|
| 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.
|
| 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.
|
| 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.
|
| 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.
|
| 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.
|
| 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.
|
| Molecular Formula |
C10H17NO5
|
|---|---|
| Molecular Weight |
231.2457
|
| Exact Mass |
231.11
|
| CAS # |
308277-46-5
|
| Related CAS # |
(Rac)-ZLc-002;ZLc-002;1446971-41-0
|
| PubChem CID |
10823397
|
| Appearance |
Off-white to light yellow solid powder
|
| LogP |
0.8
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
7
|
| Heavy Atom Count |
16
|
| Complexity |
274
|
| Defined Atom Stereocenter Count |
1
|
| 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
|
| InChi Key |
BWPKYDAJBOUZDX-VIFPVBQESA-N
|
| 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
|
| Chemical Name |
methyl (2S)-2-[(3-methoxy-3-oxopropanoyl)amino]-3-methylbutanoate
|
| 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 | 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
