|3-氨基-5-氯-N-环丙基-4-甲基-6-(2-(4-甲基哌嗪-1-基)-2-氧乙基)噻吩并[2,3-b]吡啶-2-甲酰胺|CsnPharm

CAS No.: 886047-22-9

LY2119620 Catalog No. CSN16587

Synonyms: LY2119620

LY2119620 is a specific, and allosteric agonist of human M2 and M4 muscarinic acetylcholine receptors.

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400-920-2911

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述LY2119620 is a M2/M4 receptor-selective positive allosteric modulator with EC50 values of 2.12nM and 8.47nM for M2 receptor and M4 receptor (for iperoxo), respectively. It bound allosterically to the M2 and M4 mAChRs and was positively cooperative with muscarinic orthosteric agonists.
作用机制LY2119620 is an allosteric modulator of M2/M4 receptor. It recognizes a largely pre-formed binding site in the extracellular vestibule of the iperoxo-bound receptor, inducing a slight contraction of this outer binding pocket.^[1]^[3]
参考文献

[1] Croy CH, Schober DA, 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.
[2] Schober DA, Croy CH, et al. Development of a radioligand, [(3)H]LY2119620, to probe the human M(2) and M(4) muscarinic receptor allosteric binding sites. Mol Pharmacol. 2014 Jul;86(1):116-23.
[3] Kruse AC, Ring AM, et al. Activation and allosteric modulation of a muscarinic acetylcholine receptor. Nature. 2013 Dec 5;504(7478):101-6.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2834 mL
- 11.4170 mL
- 22.8340 mL
- 5 mM
- 0.4567 mL
- 2.2834 mL
- 4.5668 mL
- 10 mM
- 0.2283 mL
- 1.1417 mL
- 2.2834 mL

技术信息

CAS号

886047-22-9

储存条件

粉末: Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C19H24ClN5O3S

运输

蓝冰

分子量

437.94

别名

LY2119620

溶解度

DMSO	87.0 mg/mL (198.7 mM)
Water	Insoluble
Ethanol	10.0 mg/mL (22.8 mM) warming

动物实验配方

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