| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 100mg | |||
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| Targets |
ZCZ011 targets the cannabinoid 1 (CB1) receptor, a G protein-coupled receptor involved in pain modulation, appetite regulation, and other physiological processes. As a positive allosteric modulator (PAM), it binds to a site distinct from the orthosteric (agonist) binding site and enhances the effects of endogenous cannabinoids like anandamide and exogenous agonists like CP55,940.
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| ln Vitro |
In vitro, ZCZ011 potentiates the binding of the CB1 orthosteric agonist CP55,940 with a pEC50 value of 6.90. It enhances anandamide (AEA)-stimulated GTPγS binding in mouse brain membranes. Additionally, ZCZ011 increases β-arrestin recruitment and ERK phosphorylation in hCB1 cells.
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| ln Vivo |
In vivo, ZCZ011 reduces neuropathic pain in mice with no psychoactive effects. Its brain-penetrant properties allow it to exert central effects, making it a valuable tool for studying the role of CB1 receptors in pain and other neurological conditions.
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| Enzyme Assay |
In vitro receptor binding assays for ZCZ011 involve measuring its ability to enhance the binding of radiolabeled agonists (such as [³H]-CP55,940) to CB1 receptors in cell membrane preparations. The compound's positive allosteric modulation is assessed by measuring its effect on GTPγS binding, which reflects G protein activation. These assays quantify the compound's potency and efficacy as a CB1 PAM.
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| Cell Assay |
In vitro cellular assays for ZCZ011 are performed using cells expressing human CB1 receptors (hCB1 cells). Cells are treated with the compound, and β-arrestin recruitment is measured using BRET or other assays. ERK phosphorylation is assessed by Western blotting or phospho-ERK ELISA. These assays provide functional evidence of the compound's PAM activity at the CB1 receptor.
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| Animal Protocol |
In vivo animal experiments for ZCZ011 are conducted in mouse models of neuropathic and inflammatory pain. A typical protocol involves administration of the compound (e.g., via intraperitoneal or oral routes) to mice with induced neuropathic pain, followed by assessment of pain-related behaviors such as mechanical allodynia or thermal hyperalgesia. The compound's lack of psychoactive effects is also evaluated in behavioral assays.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of ZCZ011 have been characterized in preclinical studies. It is a brain-penetrant compound, indicating good blood-brain barrier permeability. The compound has a molecular weight of 362.44, molecular formula C21H18N2O2S, and is soluble in DMSO (40 mg/mL). It should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years.
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| Toxicity/Toxicokinetics |
Toxicological data for ZCZ011 are not extensively reported in the available literature. As a research-use compound, its safety profile has not been formally evaluated in comprehensive preclinical toxicology studies. The compound is intended for research purposes only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling this compound.
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| References | |
| Additional Infomation |
ZCZ011 is a CB1 receptor positive allosteric modulator that has been investigated for the treatment of neuropathic and inflammatory pain. It is a research compound with potential therapeutic applications in pain management, offering the advantage of reducing pain without the psychoactive effects associated with direct CB1 agonists. This product is for research use only.
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| Molecular Formula |
C21H18N2O2S
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|---|---|
| Molecular Weight |
362.447
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| Exact Mass |
362.108
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| CAS # |
1998197-39-9
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| PubChem CID |
71819307
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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 |
602.8±55.0 °C at 760 mmHg
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| Flash Point |
318.4±31.5 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.677
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| LogP |
6.37
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
26
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| Complexity |
491
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
RJSPNRDBWHHFMH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H18N2O2S/c1-14-9-10-16-18(12-14)22-21(15-6-3-2-4-7-15)20(16)17(13-23(24)25)19-8-5-11-26-19/h2-12,17,22H,13H2,1H3
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| Chemical Name |
6-methyl-3-(2-nitro-1-thiophen-2-ylethyl)-2-phenyl-1H-indole
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| Synonyms |
ZCZ 011; ZCZ-011; ZCZ011
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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 | 2.7590 mL | 13.7950 mL | 27.5900 mL | |
| 5 mM | 0.5518 mL | 2.7590 mL | 5.5180 mL | |
| 10 mM | 0.2759 mL | 1.3795 mL | 2.7590 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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