2. GPCR/G Protein Neuronal Signaling
  3. mAChR
  4. DREADD agonist 21 dihydrochloride

DREADD agonist 21 dihydrochloride 

目录号: HY-100234A 纯度: 98.53%
COA 产品使用指南

摩尔计算器

DREADD agonist 21 dihydrochloride 是一种有效的人毒蕈碱乙酰胆碱 M3 受体 (hM3Dq) 激动剂 (EC50=1.7 nM)。

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DREADD agonist 21 dihydrochloride Chemical Structure

DREADD agonist 21 dihydrochloride Chemical Structure

CAS No. : 2250025-92-2

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1 mg ￥454
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5 mg ￥1000
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10 mg ￥1500
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25 mg ￥2600
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50 mg ￥4200
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Other Forms of DREADD agonist 21 dihydrochloride:

DREADD agonist 21 dihydrochloride 相关抗体

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MCE 顾客使用本产品发表的 1 篇科研文献

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

DREADD agonist 21 dihydrochloride is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=1.7 nM)[1].

IC50 & Target

EC50: 1.7 nM (hM3Dq)[1]
pKi: 5.97 (hM1), 5.44 (hM4), 7.20 (hM1Dq), and 6.75 (hM4Di)[2]
Ki: 6 nM (H1 histamine receptor), 66 nM (5HT2A serotonin receptor 5HT2A), 170 nM (5HT2C serotonin receptor), 280 nM (α1A adrenergic receptor)[1]
体外研究
(In Vitro)

DREADD agonist 21 is a potent human muscarinic acetylcholine M3 receptors (hM3Dq) agonist (EC50=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 (EC50=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 Ki values of 66, 170, 280, and 6 nM, respectively[1].
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)[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

DREADD agonist 21 dihydrochloride 相关抗体:
体内研究
(In Vivo)

DREADD agonist 21 (0.3, 1.0, and 3.0 mg/kg; i.p.) activates neuronal hM3Dq in mice[2].
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[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
分子量

351.27

Formula

C17H20Cl2N4
CAS 号
性状

固体

颜色

Light yellow to yellow

运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 200 mg/mL (569.36 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

H2O 中的溶解度 : 100 mg/mL (284.68 mM; 超声助溶)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.8468 mL 14.2341 mL 28.4681 mL
5 mM 0.5694 mL 2.8468 mL 5.6936 mL
查看完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
该产品水溶性佳，请具体参考实测 水 / PBS / Saline 中的溶解度数据。
您所需的储备液浓度超过该产品的实测溶解度，如有需要，请与 MCE 中国技术支持联系。
纯度 & 产品资料
参考文献

DREADD agonist 21 dihydrochloride 相关分类

完整储备液配制表

* 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。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (stored under nitrogen)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.8468 mL 14.2341 mL 28.4681 mL 71.1703 mL
5 mM 0.5694 mL 2.8468 mL 5.6936 mL 14.2341 mL
10 mM 0.2847 mL 1.4234 mL 2.8468 mL 7.1170 mL
15 mM 0.1898 mL 0.9489 mL 1.8979 mL 4.7447 mL
20 mM 0.1423 mL 0.7117 mL 1.4234 mL 3.5585 mL
25 mM 0.1139 mL 0.5694 mL 1.1387 mL 2.8468 mL
30 mM 0.0949 mL 0.4745 mL 0.9489 mL 2.3723 mL
40 mM 0.0712 mL 0.3559 mL 0.7117 mL 1.7793 mL
50 mM 0.0569 mL 0.2847 mL 0.5694 mL 1.4234 mL
60 mM 0.0474 mL 0.2372 mL 0.4745 mL 1.1862 mL
80 mM 0.0356 mL 0.1779 mL 0.3559 mL 0.8896 mL
100 mM 0.0285 mL 0.1423 mL 0.2847 mL 0.7117 mL

* 备注：如您选择水作为储备液，请稀释至工作液后，再用 0.22 μm 的滤膜过滤除菌后使用。

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

DREADD agonist 212250025-92-2DREADD agonist21DREADD agonist-21mAChRMuscarinic acetylcholine receptormuscarinicacetylcholineM3receptorshM3DqneurodegenerativediseaseschizophreniaDREADDneuronalactivationInhibitorinhibitorinhibit

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目录号：
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