| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
|
||
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 250mg | |||
| Other Sizes |
| Targets |
CB1 (cannabinoid receptor 1). AM4113 is a potent and selective CB1 receptor antagonist/inverse agonist. It binds to the CB1 receptor with high affinity and blocks the effects of endogenous and exogenous cannabinoids. Additionally, as an inverse agonist, it reduces constitutive CB1 receptor activity. This mechanism contributes to its effects on food intake and body weight.
|
|---|---|
| ln Vitro |
AM4113 demonstrates potent antagonist/inverse agonist activity at the CB1 receptor in vitro, with high affinity (Ki in the low nanomolar range). The compound inhibits cannabinoid-induced signaling, including inhibition of adenylyl cyclase and activation of MAP kinase. It shows high selectivity for CB1 over CB2 receptors. Its in vitro potency and selectivity have been characterized in receptor binding and functional assays.
|
| ln Vivo |
In vivo, AM4113 has been shown to reduce food intake, body weight, and adiposity in animal models of obesity. The compound also reduces drug-seeking behavior and has been studied for its potential in treating addiction. Its effects are mediated through CB1 receptor antagonism in the central nervous system. The compound has demonstrated efficacy in preclinical studies.
|
| Enzyme Assay |
In vitro receptor binding assays for AM4113 involve competition binding experiments using radiolabeled ligands such as [3H]CP-55,940 for CB1 receptors. Membranes are prepared from cells expressing the CB1 receptor. AM4113 is incubated at varying concentrations, and bound radioactivity is measured. Ki values are calculated from displacement curves. Functional assays measure inverse agonist activity by assessing constitutive receptor activity.
|
| Cell Assay |
Cellular assays for AM4113 involve culturing cells expressing the CB1 receptor. Cells are treated with AM4113, and receptor signaling is measured. Inhibition of adenylyl cyclase is measured by cAMP accumulation assays. MAP kinase activation is measured by Western blotting for phosphorylated ERK. Inverse agonist activity is assessed by measuring changes in constitutive receptor activity.
|
| Animal Protocol |
In vivo animal studies for AM4113 have been conducted in rodent models of obesity and addiction. The compound is typically administered intraperitoneally or orally. Food intake, body weight, and adiposity are measured. Drug-seeking behavior is assessed using self-administration or conditioned place preference paradigms. Dosing regimens vary.
|
| ADME/Pharmacokinetics |
AM4113 is a lipophilic compound with high blood-brain barrier penetration, enabling its effects on central CB1 receptors. It is metabolized in the liver and excreted via the biliary and renal routes. Detailed pharmacokinetic parameters such as half-life and bioavailability have been characterized in animal models. The compound is intended for research use only.
|
| Toxicity/Toxicokinetics |
AM4113 has shown a favorable safety profile in preclinical studies, with no significant toxicity observed at therapeutic doses. The compound is generally well-tolerated in animal models. However, comprehensive toxicological data are limited. The compound is intended for research use only and is not approved for human therapeutic applications.
|
| References | |
| Additional Infomation |
AM4113 is a potent and selective CB1 receptor antagonist/inverse agonist with potential applications in obesity, metabolic disorders, and addiction. It has shown efficacy in reducing food intake and body weight in preclinical models. The compound is not approved for clinical use and is available for research purposes only.
|
| Molecular Formula |
C17H12CL3N3O
|
|---|---|
| Molecular Weight |
380.655680656433
|
| Exact Mass |
379.004
|
| CAS # |
614726-85-1
|
| PubChem CID |
66844170
|
| Appearance |
White to off-white solid powder
|
| LogP |
5
|
| Hydrogen Bond Donor Count |
1
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
24
|
| Complexity |
458
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
N1(C2=CC=C(Cl)C=C2Cl)C(C2=CC=C(Cl)C=C2)=C(C)C(C(N)=O)=N1
|
| InChi Key |
BBUKVPCUOHFAQN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C17H12Cl3N3O/c1-9-15(17(21)24)22-23(14-7-6-12(19)8-13(14)20)16(9)10-2-4-11(18)5-3-10/h2-8H,1H3,(H2,21,24)
|
| Chemical Name |
5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methylpyrazole-3-carboxamide
|
| 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) |
DMSO : ~62.5 mg/mL (~164.19 mM)
|
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.46 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 20.8 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: ≥ 2.08 mg/mL (5.46 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 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6270 mL | 13.1351 mL | 26.2702 mL | |
| 5 mM | 0.5254 mL | 2.6270 mL | 5.2540 mL | |
| 10 mM | 0.2627 mL | 1.3135 mL | 2.6270 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.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT02512666 | Completed | Device: AM4113-N5UT Dino-Lite | Hematologic Malignancy | Massachusetts General Hospital | 2015-09 | Not Applicable |
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
