LY2119620

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

LY2119620 是人 M2 和 M4 毒蕈碱乙酰胆碱受体的特异性变构激动剂。

LY2119620 is a positive allosteric modulator of the M2 and M4 muscarinic acetylcholine receptors (mAChRs).

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.

——

LY2119620 | LY 2119620 | LY-2119620

Others

Other Targets

M2 mAChR|M4 mAChR

Neurological Disease

——

886047-22-9

437.94

C19H24ClN5O3S

>98% (HPLC)

DMSO : 67.5 mg/mL. 154.13 mM; H2O : < 0.1 mg/mL

CN1CCN(CC1)C(=O)COc1nc2sc(C(=O)NC3CC3)c(N)c2c(C)c1Cl

3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methyl-1-piperazinyl)-2-oxoethoxy]-thieno[2,3-b]pyridine-2-carboxamide

(-20℃)

With Ice Pack

≥ 2 years