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CAS No.: 868273-06-7

Org 27569 Catalog No. CSN13721

Synonyms: ORG-27569

Org 27569 is an allosteric modulator of cannabinoid CB1 receptor, induces a CB1 receptor state that is characterized by enhanced agonist affinity and decreased inverse agonist affinity.

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技术信息

生物活性

描述Cannabinoid CB₁ receptor is a G protein-coupled receptor predominantly expressed at the central and peripheral nerve terminals. Org 27569 is an allosteric modulator of cannabinoid CB₁ receptor. In the presence of 1μM Org 27569, clonidine inhibited electrically evoked contractions of mice with pEC₅₀ and E_max values of 8.66±0.11 and 77%, respectively.^[3] In mouse brain membranes and hCB₁-expressing cells, Org 27569 at 10nM-1μM caused a dose-related reduction in E_max values for two cannabinoid CB₁ receptors, CP55490 and WIN55212. In hCB1-expressing cells, Org 27569 at 100nM and 1μM also significantly increased the E_max value for CP55940-induced ERK phosphorylation.^[4] Org 27569 at a dose of 30mg/kg significantly reduced the consumption of sweet cereal in CB₁ (−/−) and (+/+) mice. The intracerebroventricular administration of 100μg Org 27569 did not alter the pharmacological effect of CP55,940 in vivo.^[5]
作用机制Org 27569 binds allosterically to the cannabinoid CB₁ receptor. It increases the binding of the CB₁ receptor agonist and decreases the affinity of the CB₁ receptor inverse agonist.^[3]
参考文献

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
- 2.4393 mL
- 12.1966 mL
- 24.3931 mL
- 5 mM
- 0.4879 mL
- 2.4393 mL
- 4.8786 mL
- 10 mM
- 0.2439 mL
- 1.2197 mL
- 2.4393 mL

技术信息

CAS号

868273-06-7

储存条件

粉末: Sealed in dry,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C24H28ClN3O

运输

蓝冰

分子量

409.95

别名

ORG-27569

溶解度

DMSO	82.0 mg/mL (200.0 mM)
Water	Insoluble
Ethanol	Insoluble

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