| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
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| Targets |
Ness0327 targets the cannabinoid CB1 receptor, a G protein-coupled receptor that is the primary target of Δ⁹-tetrahydrocannabinol (THC), the psychoactive component of cannabis. CB1 receptors are widely distributed in the central nervous system and are involved in various physiological processes including pain, appetite, and cognition. By acting as a highly selective CB1 antagonist, Ness0327 blocks CB1 receptor activation. The compound shows ultra-high affinity (Ki = 350 fM) and >60,000-fold selectivity over CB2 receptors.
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| ln Vitro |
In vitro, Ness0327 binds to the CB1 receptor with ultra-high affinity (Ki = 350 fM). It shows >60,000-fold selectivity for CB1 over CB2 receptors (Ki = 21 nM). The compound is a high selectivity antagonist of the cannabinoid CB1 receptor. Detailed in vitro data are available in the primary literature. Ness0327 is a valuable tool for studying CB1 receptor function.
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| ln Vivo |
In vivo data for Ness0327 are limited in publicly available sources. Based on its ultra-high affinity and selectivity for CB1, the compound is expected to be useful for in vivo studies of CB1 receptor function in various physiological and pathological processes. Further studies are needed to fully characterize its in vivo efficacy and pharmacokinetic profile. The compound is a research tool for cannabinoid research.
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| Enzyme Assay |
In vitro receptor binding assays for Ness0327 typically use membrane preparations from cells expressing human CB1 or CB2 receptors. Radioligand binding is performed using [³H]-CP55940, [³H]-WIN55212-2, or [¹²⁵I]-AM251 as tracers. Membranes are incubated with radioligand and varying concentrations of Ness0327 in assay buffer (50 mM Tris-HCl, pH 7.4, 5 mM MgCl₂, 1 mM EDTA, 0.1% BSA) at 30°C for 60-90 minutes. Nonspecific binding is determined using excess unlabeled ligand (e.g., WIN55212-2). Bound radioactivity is measured by filtration and scintillation counting. Ki values are calculated from competition curves. Functional assays measure CB1-mediated cAMP inhibition or G-protein activation.
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| Cell Assay |
For cell-based assays, cells expressing CB1 or CB2 receptors (e.g., CHO or HEK-293 transfectants) are cultured in DMEM with 10% FBS and selection antibiotics. Cells are seeded in 96-well plates and treated with Ness0327 at various concentrations (0.0001-10 nM) for 15-30 minutes. Cells are stimulated with CB1 agonist (e.g., CP55940 or WIN55212-2). cAMP levels are measured by ELISA or AlphaScreen. IC₅₀ values for antagonist activity are calculated. Cell viability is assessed by standard assays. All treatments include vehicle controls and are performed in triplicate.
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| Animal Protocol |
In vivo, Ness0327 may be administered to rodents via intraperitoneal (IP) or intravenous (IV) injection. The compound is formulated in a suitable vehicle such as DMSO, PEG, or saline-based solutions. For behavioral studies, animals are dosed at various regimens. Endpoints include pain, appetite, and cognitive behavioral assessments. Blood and tissue samples are collected for pharmacokinetic and pharmacodynamic analysis. All procedures follow institutional animal care guidelines.
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| ADME/Pharmacokinetics |
Ness0327 (MW 489.82, C₂₄H₂₃Cl₃N₄O) is a CB1 receptor antagonist with a Ki of 350 fM. It shows >60,000-fold selectivity for CB1 over CB2 receptors. The compound shows a purity of ≥98% (HPLC). It is typically stored at -20°C. Detailed pharmacokinetic parameters are not extensively reported. Further ADME studies are needed. The compound is for research purposes.
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| Toxicity/Toxicokinetics |
Toxicology data for Ness0327 are limited in publicly available sources. As a CB1 antagonist, potential effects on CNS function should be considered. The compound is for research use only and not intended for human therapeutic applications. Standard safety pharmacology and toxicology studies would be required for therapeutic development. The compound should be handled with standard laboratory safety precautions.
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| References | |
| Additional Infomation |
Ness0327 is a research-grade CB1 receptor antagonist for studying cannabinoid signaling. Its primary applications include neuroscience, cannabinoid research, and drug discovery. The compound is not approved for clinical use and has not entered clinical trials. It is commercially available from various chemical suppliers for research purposes only. Its mechanism involves ultra-high affinity and highly selective antagonism of CB1 receptors.
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| Molecular Formula |
C24H23CL3N4O
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|---|---|
| Molecular Weight |
489.82
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| Exact Mass |
488.093
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| CAS # |
494844-07-4
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| PubChem CID |
10435654
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| Appearance |
White to off-white solid powder
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| Density |
1.5±0.1 g/cm3
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| Index of Refraction |
1.705
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| LogP |
6.66
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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 |
3
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| Heavy Atom Count |
32
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| Complexity |
663
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
NCXBPZJQQSNIRA-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H23Cl3N4O/c25-16-7-9-18-15(13-16)5-4-6-19-22(24(32)29-30-11-2-1-3-12-30)28-31(23(18)19)21-10-8-17(26)14-20(21)27/h7-10,13-14H,1-6,11-12H2,(H,29,32)
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| Chemical Name |
12-chloro-3-(2,4-dichlorophenyl)-N-piperidin-1-yl-3,4-diazatricyclo[8.4.0.02,6]tetradeca-1(10),2(6),4,11,13-pentaene-5-carboxamide
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| Synonyms |
Ness 0327; Ness-0327; Ness0327
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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 : ~9.7 mg/mL (~19.80 mM)
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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 | 2.0416 mL | 10.2078 mL | 20.4157 mL | |
| 5 mM | 0.4083 mL | 2.0416 mL | 4.0831 mL | |
| 10 mM | 0.2042 mL | 1.0208 mL | 2.0416 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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