DREADD AGONIST 21
- CAS号:56296-18-5
- 英文名:11-Piperazinyldibenzo[b,e][1,4]diazepine
- 中文名:DREADD AGONIST 21
- CBNumber:CB52650796
- 分子式:C17H18N4
- 分子量:278.35
- MOL File:56296-18-5.mol
- 沸点 :470.1±55.0 °C(Predicted)
- 密度 :1.28±0.1 g/cm3(Predicted)
- 储存条件 :Store at -20°C
- 溶解度 :DMSO:PBS (pH 7.2) (1:1):0.5(Max Conc. mg/mL);1.8(Max Conc. mM)
Ethanol:29.61(Max Conc. mg/mL);106.39(Max Conc. mM) - 形态 :A crystalline solid
- 酸度系数(pKa) :8.56±0.10(Predicted)
- 颜色 :Yellow
DREADD AGONIST 21性质、用途与生产工艺
- 生物活性 DREADD agonist 21 是一种有效的 human muscarinic acetylcholine M3 receptors (hM3Dq) 激动剂,其EC50值为1.7 nM。
-
靶点
Target Value hM3Dq
(Cell-free assay)1.7 nM(EC50) -
体外研究
DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC 50 =1.7 nM) and does not activate human M3 receptor (hM3). In addition to being inactive at hM3, DREADD agonist 21, a potent full agonist of hM3Dq (EC 50 =1.7 nM), is only 3.5-fold selective for hM3Dq over H1, 40-fold selective over 5HT2A, 100-fold selective over 5HT2C, and 165-fold selective over α1A. DREADD agonist 21 shows high binding affinities to 5HT2A and 5HT2C serotonin receptor, α1A adrenergic receptor, and H1 histamine receptor with K i values of 66, 170, 280, and 6 nM, respectively.
DREADD agonist 21 potently activates hM1Dq, hM3Dq, and hM4Di. DREADD agonist 21 binds to hM1, hM4, hM1Dq and hM4Di receptors with pK i s of 5.97, 5.44, 7.20, and 6.75, respectively. DREADD agonist 21 potently activates hM3Dq in Chinese hamster ovary (CHO) cells transfected cells in vitro with a pEC 50 of 8.48±0.05. DREADD agonist 21 is a highly selective and potent agonist for muscarinic DREADDs (pEC 50 for hM1Dq=6.54 and that for hM4Di=7.77 in pERK assays). -
体内研究
DREADD agonist 21 (0.3, 1.0, and 3.0 mg/kg; i.p.) activates neuronal hM3Dq in mice.
DREADD agonist 21 has excellent bioavailability, pharmacokinetic properties, and brain penetrability. DREADD agonist 21 (0.1, 1, and 10 mg/kg; i.p.) displays 95.1% plasma protein binding and 95% brain protein bounding in mice.
- 更新日期:2024/08/19
- 产品编号:HY-100234
- 产品名称:DREADD AGONIST 21 DREADD agonist 21
- CAS编号:56296-18-5
- 包装:2mg
- 价格:600元
- 更新日期:2024/08/19
- 产品编号:HY-100234
- 产品名称:DREADD AGONIST 21 DREADD agonist 21
- CAS编号:56296-18-5
- 包装:10mM * 1mLin DMSO
- 价格:920元
- 公司名称:TOCRIS-US
- 联系电话:--
- 电子邮件:customerservice@tocris.co.uk
- 国家:英国
- 产品数:5729
- 优势度:77