產(chǎn)品目錄

規(guī)格	10mM (in 1mL DMSO) 5mg 25mg
CAS	886047-22-9
別名
化學(xué)名	3-amino-5-chloro-N-cyclopropyl-4-methyl-6-[2-(4-methylpiperazin-1-yl)-2-oxoethoxy]thieno[2,3-b]pyridine-2-carboxamide
分子式	C19H24ClN5O3S
分子量	437.94
溶解度	≥ 21.897mg/mL in DMSO
儲存條件	Store at -20°C
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

產(chǎn)品描述：

LY2119620 is a selective positive allosteric modulator of M2/M4 receptor [1].

Muscarinic acetylcholine receptors (M1-M5) are G-protein coupled receptors regulating the action of the neurotransmitter ACh and play an important role in smooth muscle control, exocrine gland function, mood and cognition [1].

LY2119620 is a selective positive allosteric modulator of M2/M4 receptor. In [35S]GTPγS-binding experiments, LY2119620 exhibited a modest allosteric agonism of 23.2% and 16.8% at the M2 and M4 receptors, respectively. LY2119620 and ACh binding caused cooperativity factor α of 79.4 and 19.5 for the M4 receptor and the M2 receptor, respectively. The cooperativity between LY2119620 and orthosteric agonists (Iperoxo or Oxo-M) was also observed [1]. M2 receptor simultaneously bound to LY2119620 and iperoxo. LY2119620 exhibited mild negative cooperativity with the inverse agonist NMS and strong positive cooperativity with iperoxo [2]. LY2119620 significantly increased Bmax values without changes in Kd when cooperativity binding of [3H]LY2119620 with mAChR, suggesting a G protein-dependent process [3].

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原創(chuàng)作者：上海莼試生物技術(shù)有限公司

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