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Purity: ≥98%
AM-1241 (AM1241; AM 1241), an aminoalkylindole analog, is a novel, potent and selective cannabinoid (CB2) receptor agonist with potential analgesic effects (pain-killing). It exhibits 82-fold selectivity over the CB1 receptor and activates CB2 with a Ki of 3.4 nM.
| Targets |
CB2 ( Ki = 3.4 nM ); CB1 ( Ki = 280 nM )
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| Enzyme Assay |
Competition-equilibrium binding versus is used to assess cannabinoid receptor binding. Three-h After diluting AM-1241 (CP55,940) in 25 mM Tris base (pH 7.4), 5 mM MgCl2, 1 mM EDTA, and 0.1% effectively fatty acid-free BSA, the mixture is put into 96-well plates that have been treated with Regisil. Three-h Add CP55,940 (DuPont_NEN; specific activity 100–180 Ci/mmol; 1 Ci = 37 GBq) at a concentration of 0.8 nM. Packard Filtermate 196 cell harvester is used to filter the contents over Packard Unifilter GF/B 96-well filters after adding membranes made from rat brain (which contain CB1 receptors) or mouse spleen (which contain CB2 receptors) (approximately 50 μg of membrane protein per well). The plates are then incubated at 30 °C for one hour. The filters are dried after being rinsed with ice-cold 50 mM Tris base/5 mM MgCl2/0.5% BSA. The amount of bound radioactivity is measured, nonspecific binding is adjusted for, and the results are normalized between 0% and 100% [3H]. Specifically bound to CP-55,940. Using GraphPad PRISM for nonlinear regression analysis, the IC50 is calculated and converted to a Ki value. Every data set is gathered twice. Three separate experiments yielded the IC50 and Ki values.
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| Cell Assay |
Membrane samples are prepared from the CHO cell line, which stably expresses the human CB1 receptor, or from HEK cells that stably express the human CB2 receptors that were previously generated (Mukherjee et al., 2004). The following is how radioligand binding assays are carried out. In a nutshell, the cells are taken and homogenized with a Polytron for two × 10-s bursts in a buffer that contains 50 mM Tris-HCl, pH 7.4, 1 mM MgCl2, and 1 mM EDTA with protease inhibitors. This is done for 20 minutes at 45 000 g of centrifugation. After washing, the membrane pellets are frozen in aliquots at -80 °C until needed. The experiment involves conducting saturation binding reactions with [3H]CP 55,940 (0.01–8 nM) at 30 °C for 90 minutes. The reaction is stopped by rapidly vacuum filtering the mixture through UniFilter-96 GF/C filter plates, followed by four washes with cold assay buffer and 50 mM Tris-HCl, pH 7.4, 2.5 mM EDTA, 5 mM MgCl2, and 0.05% fatty acid free bovine serum albumin (BSA). In competition experiments, test compounds (0.1 nM–10 μM) are used in conjunction with 0.5 nM [3H]CP 55,940. 10 mM unlabeled CP 55,940 is used to define nonspecific binding. Using the Prism software, one site binding or one site competition curve fitting is used to determine KD values from saturation binding assays and Ki values from competition binding assays.
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| References |
| Molecular Formula |
C22H22IN3O3
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| Molecular Weight |
503.33
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| Exact Mass |
503.07
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| Elemental Analysis |
C, 52.50; H, 4.41; I, 25.21; N, 8.35; O, 9.54
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| CAS # |
444912-48-5
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| Appearance |
Solid powder
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| SMILES |
CN1CCCCC1CN2C=C(C3=CC=CC=C32)C(=O)C4=C(C=CC(=C4)[N+](=O)[O-])I
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| InChi Key |
ZUHIXXCLLBMBDW-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H22IN3O3/c1-24-11-5-4-6-16(24)13-25-14-19(17-7-2-3-8-21(17)25)22(27)18-12-15(26(28)29)9-10-20(18)23/h2-3,7-10,12,14,16H,4-6,11,13H2,1H3
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| Chemical Name |
(2-iodo-5-nitrophenyl)-[1-[(1-methylpiperidin-2-yl)methyl]indol-3-yl]methanone
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| Synonyms |
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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 |
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| 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) |
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| Solubility (In Vivo) |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9868 mL | 9.9338 mL | 19.8677 mL | |
| 5 mM | 0.3974 mL | 1.9868 mL | 3.9735 mL | |
| 10 mM | 0.1987 mL | 0.9934 mL | 1.9868 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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