DREADD agonist 21 dihydrochloride|cas:2250025-92-2|西域试剂

DREADD agonist 21 dihydrochloride,98.53%

产品编号：Bellancom-100234A| CAS NO：2250025-92-2| 分子式：C₁₇H₂₀Cl₂N₄| 分子量：351.27

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货号	价格	库存与货期
Bellancom-100234A	￥1000.00	杭州北京（现货）
Bellancom-100234A	￥1500.00	杭州北京（现货）
Bellancom-100234A	￥2600.00	杭州北京（现货）
Bellancom-100234A	￥4200.00	杭州北京（现货）
Bellancom-100234A	￥6700.00	杭州北京（现货）

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DREADD agonist 21 dihydrochloride

产品介绍

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)。

生物活性

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

体外研究

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 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_is 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).

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

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.

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

体内研究

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

性状

Solid

溶解性数据

In Vitro:

DMSO : 200 mg/mL (569.36 mM; ultrasonic and warming and heat to 60°C)

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
10 mM	0.2847 mL	1.4234 mL	2.8468 mL

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。

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)

参考文献