| Bioactivity | LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist. | ||||||||||||
| Target | M2/M4 receptor | ||||||||||||
| Invitro | LY2119620 shows a modest allosteric agonism of 23.2±2.18% and 16.8±5.01% at the M2 and M4 receptors, respectively. Minimal allosteric agonism (<20%) is observed for LY2119620 at the M1, M3, and M5 receptors. The variable KB of LY2119620 for the allosteric binding site on the unoccupied receptor is found to be consistently about 1.9 to 3.4 µM. Results show a Bmax increase at the M2 receptor from 793±1.95 fmol/mg to 2850±162 fmol/mg upon addition of 10 µM LY2119620, and about a 5-fold increase in Bmax at the M4 receptor, 284±18.3 fmol/mg to 1340±42.2 fmol/mg[1]. | ||||||||||||
| Name | LY2119620 | ||||||||||||
| CAS | 886047-22-9 | ||||||||||||
| Formula | C19H24ClN5O3S | ||||||||||||
| Molar Mass | 437.94 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
|
||||||||||||
| Reference | [1]. Croy CH, et al. Characterization of the novel positive allosteric modulator, LY2119620, at the muscarinic M(2) and M(4) receptors. Mol Pharmacol. 2014 Jul;86(1):106-15. |