All AbMole products are for research use only, cannot be used for human consumption.
Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24). Org 27569 inhibits CB1 receptor antagonist efficacy in vitro (pKb = 7.57). Org 27569 binds to a regulatory site on the CB1 receptor target, causing a conformational change that increases the binding affinity of CB1 agonists such as CP 55,940, while decreasing the binding affinity of CB1 antagonists or inverse agonists such as rimonabant. Org 27569 significantly increases binding of the CB1 agonist [3H]CP 55.940 (pKb = 5.67) and decreases binding of the CB1 inverse agonist [3H]SR 141716A (pKb = 5.95), and so in practice behaves as an insurmountable antagonist of CB1 receptor function.
| Cell Experiment | |
|---|---|
| Cell lines | HEK293 cells expressing the wild-type (●), T210I (△), and T210A (■) receptors |
| Preparation method | GTPγS Binding Assay 15 μg of membranes were incubated for 60 min at 30 °C in a total volume of 500 μM GTPγS binding assay buffer (50 mM Tris-HCl, pH 7.4, 3 mM MgCl2, 0.2 mM EGTA, and 100 mM NaCl) with unlabeled ligand (at least nine different concentrations were used ranging between 100 pM and 100 μM), 0.1 nM [35S]GTPγS (1250 Ci/mmol; PerkinElmer Life Sciences), 10 μM GDP, and 0.1% (w/v) BSA. The basal GTPγS binding was measured in the absence of ligand. Nonspecific binding was determined with 10 μM unlabeled GTPγS (Sigma). The reaction was terminated by rapid filtration through Whatman GF/C filters. The radioactivity trapped in the filters was determined by liquid scintillation counting. |
| Concentrations | 0~10 μ M |
| Incubation time | 5~15 min |
| Animal Experiment | |
|---|---|
| Animal models | Adult male Sprague–Dawley rats |
| Formulation | a mixture of 1 part absolute ethanol, 1 part Emulphor-620 (Rhodia Inc., Cranbury, NJ), and 18 parts physiological saline |
| Dosages | 8 days of daily 5.6 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 409.95 |
| Formula | C24H28ClNO3 |
| CAS Number | 868273-06-7 |
| Solubility (25°C) | DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Cannabinoid Products |
|---|
| UCM707
UCM707, a potent and selective inhibitor of endocannabinoid uptake, potentiates hypokinetic and antinociceptive effects of Anandamide. |
| SCH 336
SCH 336 is a potent, selective, inverse and orally active CB2 agonist. |
| JTE-907
JTE-907 is a highly selective, orally active CB2 receptor inverse agonist and exerts anti-inflammatory effects in vivo. |
| LEI-101
LEI-101 is a potent, selective, and orally bioavailable cannabinoid CB2 receptor agonist, with a pEC50 of 8 for hCB2, and a pKi of less than 4 for hERG. |
| AEF0117
AEF0117 is a signaling-specific inhibitor of the cannabinoid receptor 1 (CB1-SSi). |
All AbMole products are for research use only, cannot be used for human consumption or veterinary use. We do not provide products or services to individuals. Please comply with the intended use and do not use AbMole products for any other purpose.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2024 AbMole BioScience. All Rights Reserved.
