|DREADD激动剂21|CsnPharm

CAS No.: 56296-18-5

DREADD agonist 21 Catalog No. CSN18998

Synonyms: DREADD Agonist 21

DREADD agonist 21 is a potent muscarinic DREADD agonist with pEC50 values of 8.91, 8.48 and 7.77 for hM1Dq, hM3Dq and hM4Di, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

靶点 mAChR M3

EC50:1.7nM
描述Designer Receptors Exclusively Activated by Designer Drugs (DREADDs) have been developed as a powerful chemogenetics technology for remotely controlling neuronal activity and have been widely adopted by the neuroscience and greater biological communities. DREADDs derived from the human muscarinic acetylcholine M3 receptors (hM3Dq) are insensitive to the endogenous ligand acetylcholine (ACh). DREADD Agonist 21 is a potent full agonist (EC₅₀ = 1.7 nM, E_max = 100%) of hM3Dq^[2]. DREADD Agonist 21 potently activated hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro, and it stimulated calcium mobilization at hM3Dq with a pEC₅₀ of 8.48 ± 0.05. At a single concentration (5 μM), DREADD Agonist 21 showed agonist activity only at M4-, D2-, and H4-histamine receptors. At hM1 and hM4, DREADD Agonist 21 shifted the acetylcholine concentration response curve in pERK assays to the right indicating weak functional antagonism at these receptors. A time course of DREADD Agonist 21 accumulation in the brain and plasma following administration of 5 mg/kg demonstrated that plasma levels peaked at 1150 ng/mL (4.12 μM), whereas brain levels reached 579 ng/mL (2 μM)^[3].
参考文献

[1] Chen X, Choo H, et al. The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem Neurosci. 2015 Mar 18;6(3):476-84.
[2] Chen X, Choo H, Huang XP, et al. The first structure-activity relationship studies for designer receptors exclusively activated by designer drugs. ACS Chem Neurosci. 2015;6(3):476‐484
[3] Thompson KJ, Khajehali E, Bradley SJ, et al. DREADD Agonist 21 Is an Effective Agonist for Muscarinic-Based DREADDs in Vitro and in Vivo. ACS Pharmacol Transl Sci. 2018;1(1):61‐72

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
- 3.5926 mL
- 17.9629 mL
- 35.9258 mL
- 5 mM
- 0.7185 mL
- 3.5926 mL
- 7.1852 mL
- 10 mM
- 0.3593 mL
- 1.7963 mL
- 3.5926 mL

技术信息

CAS号

56296-18-5

储存条件

粉末: Keep in dark place,Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H18N4

运输

蓝冰

分子量

278.35

别名

DREADD Agonist 21

溶解度

DMSO	56.0 mg/mL (201.2 mM)
Water	Insoluble
Ethanol	55.0 mg/mL (197.6 mM)

动物实验配方

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DREADD agonist 21 Catalog No. CSN18998

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