56296-18-5_化工百科

中文名	DREADD agonist 21
英文名	DREADD agonist 21
别名	DREADD激动剂21 化合物DREADD AGONIST 21
英文别名	DREADD agonist 1 DREADD Agonist 21 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)-
CAS	56296-18-5
化学式	C17H18N4
分子量	278.35
密度	1.28±0.1 g/cm3(Predicted)
沸点	470.1±55.0 °C(Predicted)
溶解度	DMSO: ≥ 78 mg/mL
酸度系数	8.56±0.10(Predicted)
存储条件	-20℃
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.

56296-18-5 - 配置溶液浓度参考

	1mg	5mg	10mg
1 mM	3.593 ml	17.963 ml	35.926 ml
5 mM	0.719 ml	3.593 ml	7.185 ml
10 mM	0.359 ml	1.796 ml	3.593 ml
5 mM	0.072 ml	0.359 ml	0.719 ml

最后更新：2024-01-02 23:10:35

北京索莱宝科技有限公司

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产品名: DREADD agonist 21 去供应商网站查看询盘
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上海吉至生化科技有限公司

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产品名: DREADD激动剂21 去供应商网站查看询盘
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上海麦克林生化科技股份有限公司

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上海源叶生物科技有限公司

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产品名: DREADD agonist 21 去供应商网站查看询盘
CAS: 56296-18-5
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