Biological Activity
Potent CB1 receptor antagonist/inverse agonist (Ki = 141 nM) with greater than 70-fold selectivity over CB2 receptors (Ki > 10 μM). Structurally dissimilar from SR 141716A and AM 251. Shows weak binding to both 5-HT2 (Ki = 6.4 μM) and muscarinic receptors (Ki = 2.1 μM).
Technical Data
| M. Wt | 383.4 |
| Formula | C24H17NO4 |
| Storage | Store at RT |
| Purity | ≥98% (HPLC) |
| CAS Number | 176977-56-3 |
| PubChem ID | 5311257 |
| InChI Key | RYNSGDFWBJWWSZ-UHFFFAOYSA-N |
| Smiles | COC1=CC=C(C=C1)C1=C(C(=O)C2=CC=C(C=C2)C#N)C2=CC=C(OC)C=C2O1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 11.5 | 30 |
Preparing Stock Solutions
The following data is based on the product molecular weight 383.4. Batch specific molecular weights may vary from batch to batch due to solvent 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 | 2.61 mL | 13.04 mL | 26.08 mL |
| 5 mM | 0.52 mL | 2.61 mL | 5.22 mL |
| 10 mM | 0.26 mL | 1.3 mL | 2.61 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Felder et al (1998) LY320135, a novel cannabinoid CB1 receptor antagonist, unmasks coupling of the CB1 receptor to stimulation of cAMP accumulation. J.Pharmacol.Exp.Ther. 284 291 PMID: 9435190
Holland et al (1999) Cannabinoid CB1 receptors fail to cause relaxation, but couple via Gi/Go to the inhibition of adenylyl cyclase in carotid artery smooth muscle. Br.J.Pharmacol. 128 597 PMID: 10516638
Pertwee (2005) Inverse agonism and neutral antagonism at cannabinoid CB1 receptors. Life Sci. 76 1307 PMID: 15670612
Keywords: LY 320135, supplier, Selective, CB1, receptor, antagonists, inverse, agonists, cannabinoids, Receptors, LY320135, cb1r, CB1, Receptors, CB1, Receptors, Tocris Bioscience
