Scopolamine hydrobromide - CAS:114-49-8

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Scopolamine hydrobromide (Synonyms:Hyoscine hydrobromide; Scopine (-tropate hydrobromide; Scopine tropate hydrobromide))

目录号 : KM15814 CAS No. : 114-49-8 纯度 : 98%

Data Sheet 产品使用指南

Scopolamine hydrobromide 是高亲和力的 (nM 级别) 毒蕈碱 (muscarinic) 拮抗剂。Scopolamine 可逆抑制 5-HT₃ 受体反应，IC₅₀ 为 2.09 μM。

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100mg		In-stock
500mg		In-stock
1g	询价	In-stock
5g	询价	In-stock

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生物活性

Scopolamine hydrobromide is a high affinity (nM) muscarinic antagonist. 5-HT₃ receptor-responses are reversibly inhibited by Scopolamine with an IC₅₀ of 2.09 μM.

体外研究

Application of Scopolamine to oocytes expressing 5-HT₃ receptors does not elicit a response when applied alone, but causes a concentration-dependent inhibition of the response during a co-application of 2 μM 5-HT. The pIC₅₀ value for Scopolamine is 5.68±0.05 (IC₅₀=2.09 μM, n=6) with a Hill Slope of 1.06 ± 0.05. This gave a K_b of 3.23 μM. The same concentration-dependent effect is also seen when Scopolamine is applied during the 5-HT application. To further test for a competitive binding at the 5-HT₃ receptor, the competition of unlabelled Scopolamine is measured with [H]granisetron, an established high-affinity competitive antagonist at these receptors. Scopolamine displays concentration-dependent competition with 0.6 nM [H]granisetron (~K_d), yielding an average pK_i of 5.17±0.24 (K_i=6.76 μM, n=3).

体内研究

In the histopathology study, there is no significant change in the histology of the brain. However, it is observed that there is a reduction in density of cells in the hippocampus of the control mice pretreated with Scopolamine who received only distilled water. Scopolamine administration alone significantly increases the activity of Acetylcholinesterase enzyme (AchE) (7.98±0.065; P<0.001) when compared to the normal group (3.06±0.296). The animals treated with Scopolamine report a significant increase (34.61±4.85; P<0.01) in levels of malondialdehyde (MDA) as compared to the normal group (12.82±2.86). The Scopolamine-treated group shows significant decrease in reduced glutathione (GSH) level (P<0.001; 0.1504±0.03) as compared to the normal group (0.3906±0.02). The Scopolamine-treated rats show a significant increase in the concentration ofβ amyloid (Aβ_1-42) (P<0.001; 146.2±1.74) as compared to the normal group (43.21±3.46).

分子式

C₁₇H₂₂BrNO₄

分子量

384.26

CAS号

114-49-8

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

溶解性数据

In Vitro:

DMSO : 250 mg/mL (650.60 mM; Need ultrasonic)

H₂O : ≥ 100 mg/mL (260.24 mM)

* "≥" means soluble, but saturation unknown.

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.6024 mL	13.0120 mL	26.0240 mL
5 mM	0.5205 mL	2.6024 mL	5.2048 mL
10 mM	0.2602 mL	1.3012 mL	2.6024 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 (sealed storage, away from moisture)。-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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.41 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.41 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。