56296-18-5
56296-18-5 結(jié)構(gòu)式
基本信息
DREADD Agonist 21
11-Piperazinyldibenzo[b,e][1,4]diazepine
11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine
5H-Dibenzo[b,e][1,4]diazepine, 11-(1-piperazinyl)-
物理化學(xué)性質(zhì)
Ethanol:29.61(Max Conc. mg/mL);106.39(Max Conc. mM)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2024/08/19 | HY-100234 | DREADD AGONIST 21 DREADD agonist 21 | 56296-18-5 | 2mg | 600元 |
| 2024/08/19 | HY-100234 | DREADD AGONIST 21 DREADD agonist 21 | 56296-18-5 | 10mM * 1mLin DMSO | 920元 |
| 2024/08/19 | HY-100234 | DREADD AGONIST 21 DREADD agonist 21 | 56296-18-5 | 5mg | 1100元 |
常見問題列表
| Target | Value |
|
hM3Dq
(Cell-free assay) | 1.7 nM(EC50) |
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).
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.