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Description: Potent allosteric modulator of CB1 receptors
Chemical Name: 5-Chloro-3-ethyl-N-[2-[4-(1-piperidinyl)phenyl]ethyl-1H-indole-2-carboxamide
Purity: ≥99% (HPLC)
Biological Activity for Org 27569
Org 27569 is a potent CB1 receptor allosteric modulator (pEC50 = 8.24). 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). Inhibits CB1 receptor antagonist efficacy in vitro (pKb = 7.57).
Technical Data for Org 27569
| M. Wt | 409.95 |
| Formula | C24H28ClN3O |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 868273-06-7 |
| PubChem ID | 44828492 |
| InChI Key | AHFZDNYNXFMRFQ-UHFFFAOYSA-N |
| Smiles | CCC2=C(C(NCCC3=CC=C(N4CCCCC4)C=C3)=O)NC1=CC=C(Cl)C=C12 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for Org 27569
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 40.99 | 100 |
Preparing Stock Solutions for Org 27569
The following data is based on the product molecular weight 409.95. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.44 mL | 12.2 mL | 24.39 mL |
| 5 mM | 0.49 mL | 2.44 mL | 4.88 mL |
| 10 mM | 0.24 mL | 1.22 mL | 2.44 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.49 mL |
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Product Datasheets for Org 27569
References for Org 27569
References are publications that support the biological activity of the product.
Price et al (2005) Allosteric modulation of the Cannabinoid CB1 receptor. Mol.Pharmacol. 68 1484 PMID: 16113085
Ross (2007) Allosterism and the cannabinoid CB1 receptors: the shape of things to come. Trends Pharmacol.Sci. 28 567 PMID: 18029031
If you know of a relevant reference for Org 27569, please let us know.
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Keywords: Org 27569, Org 27569 supplier, Potent, allosteric, CB1, modulators, cannabinoids, Receptors, Org27569, cb1r, 2957, Tocris Bioscience
2 Citations for Org 27569
Citations are publications that use Tocris products. Selected citations for Org 27569 include:
Cawston et al (2013) Real-time characterization of cannabinoid receptor 1 (CB1 ) allosteric modulators reveals novel mechanism of action. Br J Pharmacol 170 893 PMID: 23937487
Baillie et al (2013) CB(1) receptor allosteric modulators display both agonist and signaling pathway specificity. Mol Pharmacol 83 322 PMID: 23160940
Do you know of a great paper that uses Org 27569 from Tocris? Please let us know.
Reviews for Org 27569
Average Rating: 5 (Based on 1 Review.)
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Works as described, very interesting compound..
By
Jonathan Fay on 05/30/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: COSH-1
Allosteric modulation of radioactive Agonist (CP) and Antagonist (SR) binding by various concentrations of Org 27569 and inhibition of agonist stimulated GTPgS binding.
For a constitutively inactive mutant tested, Org 27569 had enhanced potency and appeared to slow radio-labeled agonist dissociation so much that equilibrium was not achieved during the typical 1 hour incubation, at higher Org concentrations.
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