| 中文名称: | DREADD agonist 21 | ||||
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| 英文名称: | DREADD agonist 21 | ||||
| 别名: | 11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine | ||||
| CAS No: | 56296-18-5 | 分子式: | C17H18N4 | 分子量: | 278.35 |
| CAS No: | 56296-18-5 | ||||
| 分子式: | C17H18N4 | ||||
| 分子量: | 278.35 | ||||
基本信息
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产品编号： |
D10051 |
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产品名称： |
DREADD agonist 21 |
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CAS: |
56296-18-5 |
储存条件 |
粉末 |
-20℃ |
四年 |
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分子式： |
溶于液体 |
-80℃ |
6个月 |
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分子量： |
278.35 |
-20℃ |
1个月 |
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化学名： |
11-(1-Piperazinyl)-5H-dibenzo[b,e][1,4]diazepine |
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Solubility (25°C)： |
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体外:
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DMSO |
56mg/mL (201.18mM) |
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Ethanol |
56mg/mL (201.18mM) |
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Water |
Insoluble |
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体内(现配现用): |
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＜1mg/ml表示微溶或不溶。 |
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普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。 |
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请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；⼀旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 |
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制备储备液
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浓度
溶液体积 质量 |
1mg |
5mg |
10mg |
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1mM |
3.5926mL |
17.9630mL |
35.9260mL |
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5mM |
0.7185mL |
3.5926mL |
7.1852mL |
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10mM |
0.3593mL |
1.7963mL |
3.5926mL |
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50mM |
0.0719mL |
0.3593mL |
0.7185mL |
生物活性
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产品描述 |
一种毒蕈碱型HM3DQ受体激动剂，EC50:1.7nM. |
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靶点 |
hM3Dq |
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1.7nM(EC50) |
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体外研究 |
DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7nM) and does not activate human M3 receptor (hM3).In addition to being inactive at hM3,DREADD agonist 21,a potent full agonist of hM3Dq (EC50=1.7nM),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 Ki values of 66,170,280,and 6nM,respectively.DREADD agonist 21 potently activates hM1Dq,hM3Dq,and hM4Di.DREADD agonist 21 binds to hM1,hM4,hM1Dq and hM4Di receptors with pKis 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 pEC50 of 8.48±0.05.DREADD agonist 21 is a highly selective and potent agonist for muscarinic DREADDs (pEC50 for hM1Dq=6.54 and that for hM4Di=7.77 in pERK assays). |
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体内研究 |
DREADD agonist 21 (0.3,1.0,and 3.0mg/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 10mg/kg;i.p.) displays 95.1% plasma protein binding and 95% brain protein bounding in mice. |
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (g) = 浓度 (mol/L) x 体积 (L) x 分子量 (g/mol)
摩尔浓度计算公式
用本工具协助配置特定浓度的溶液，使用的计算公式为：
开始浓度 x 开始体积 = 最终浓度 x 最终体积
稀释公式
稀释公式一般简略地表示为：C1V1 = C2V2 ( 输入 输出 )
