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Org 27569

Cat. No. M1907
Org 27569 Structure
Size Price Availability Quantity
10mg USD 105 In stock
50mg USD 440 In stock
100mg USD 500 In stock
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Quality Control
  • Current batch:
  • Purity >99%
  • COA
  • MSDS
Biological Activity

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.

Protocol
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
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Chemical Information
Molecular Weight 409.95
Formula C24H28ClNO3
CAS Number 868273-06-7
Purity >99%
Solubility DMSO
Storage at -20°C
References

Behavioral effects of the cannabinoid CB1 receptor allosteric modulator ORG27569 in rats.
Ding Y, et al. Pharmacol Res Perspect. 2014 Dec;2(6):e00069. PMID: 25431655.

Allosteric modulator ORG27569 induces CB1 cannabinoid receptor high affinity agonist binding state, receptor internalization, and Gi protein-independent ERK1/2 kinase activation.
Ahn KH, et al. J Biol Chem. 2012 Apr 6;287(15):12070-82. PMID: 22343625.

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  Catalog
Abmole Inhibitor Catalog 2017




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