| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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Purity: ≥98%
Org 27569 (Org27569; Org-27569), similar to the anorectic antiobesity drug rimonabant, is a novel, potent and selective allosteric modulator of cannabinoid CB1 receptor with anti-obesity effects.
| Targets |
CB1
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| ln Vitro |
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| ln Vivo |
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| Enzyme Assay |
The CB1 receptor antagonist [3H]SR 141716A (1.2 nM) and the CB1 receptor agonist [3H]CP 55,940 (0.7 nM) are used in binding assays, along with 500 μL of total assay volume, 1 mg/mL BSA, and 50 mM Tris buffer containing 0.5 mM MgCl2 and 0.1 mM EDTA, pH 7.4. The addition of 30 μg of mouse brain membranes starts the binding process. Whatman GF/B glass-fiber filters that have been soaked in wash buffer at 4°C for 24 hours are used in conjunction with a 24-well sampling manifold to perform assays at 37°C for 60 minutes. The assays are then terminated by adding ice-cold wash buffer (50 mM Tris buffer and 1 mg/mL BSA) and vacuum filtration. Using a 4-mL aliquot of buffer, each reaction tube is cleaned five times. Radioactivity is measured using liquid scintillation spectrometry after the filters are oven-dried for 60 minutes and submerged in 5 mL of scintillation fluid. The difference between the binding that happens with and without 1 μM concentrations of the corresponding unlabeled ligand is known as specific binding, which accounts for 70–80% of net binding.
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| Cell Assay |
ORG27569 (10 μM) is applied to CB1 receptor-expressing cells for a duration of 5 to 15 minutes. To treat the toxin and prevent Gi coupling effects, 5 ng/ml of PTX is added to the medium. After the cells are incubated with the toxin for eighteen hours, they are twice washed with PBS and treated with various compounds. After washing the cells in ice-cold PBS, the cells are harvested and treated with ice-cold lysis buffer (150 mM NaCl, 1.0% IGEPAL CA-630, 0.5% sodium deoxycholate, 0.1% SDS, and 50 mM Tris, pH 7.5) that contains protease inhibitors such as pepstatin A, E-64, bestatin, leupeptin, and aprotinin.
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| Animal Protocol |
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| References |
| Molecular Formula |
C24H28CLN3O
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| Molecular Weight |
409.95
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| Exact Mass |
409.19
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| Elemental Analysis |
C, 70.31; H, 6.88; Cl, 8.65; N, 10.25; O, 3.90
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| CAS # |
868273-06-7
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| Related CAS # |
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| Appearance |
Solid powder
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| SMILES |
CCC1=C(NC2=C1C=C(C=C2)Cl)C(=O)NCCC3=CC=C(C=C3)N4CCCCC4
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| InChi Key |
AHFZDNYNXFMRFQ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C24H28ClN3O/c1-2-20-21-16-18(25)8-11-22(21)27-23(20)24(29)26-13-12-17-6-9-19(10-7-17)28-14-4-3-5-15-28/h6-11,16,27H,2-5,12-15H2,1H3,(H,26,29)
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| Chemical Name |
5-chloro-3-ethyl-N-[2-(4-piperidin-1-ylphenyl)ethyl]-1H-indole-2-carboxamide
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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) |
Solubility in Formulation 1: 2.5 mg/mL (6.10 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 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: 2.5 mg/mL (6.10 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (6.10 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4393 mL | 12.1966 mL | 24.3932 mL | |
| 5 mM | 0.4879 mL | 2.4393 mL | 4.8786 mL | |
| 10 mM | 0.2439 mL | 1.2197 mL | 2.4393 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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