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Reserpine hydrochloride
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Reserpine hydrochloride图片
CAS NO:16994-56-2
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
100mg电议
200mg电议
500mg电议

产品名称
利血平盐酸盐
产品介绍
Reserpine (hydrochloride) 是囊泡单胺转运蛋白 2 (VMAT2) 的抑制剂。
生物活性

Reserpine hydrochloride is an inhibitor of thevesicularmonoamine transporter2(VMAT2).

IC50& Target

VMAT2[1]

体外研究
(In Vitro)

Reserpine hydrochloride is an inhibitor of the vesicular monoamine transporter 2 (VMAT2). Reserpine hydrochloride displays a significant on the density of dopamine D1 receptors (F2,12=8.81, p<0.01) in the rat striatum. The affinity (Kd) for the dopamine D1 and D2 receptors during withdrawal from acute and chronic administration of reserpine is not change[1]. IC50values of 43.9 and 54.9 μM are obtained after 1 day of treatment with Reserpine hydrochloride in JB6 P+ and HepG2-C8 cells, respectively. Reserpine hydrochloride induces luciferase activity in a dose-dependent manner at concentrations ranging from 5 to 50 μM, and no significant induction is observed at concentrations lower than 5 μM. Results demonstrate that Reserpine hydrochloride (2.5 to 10 μM) also increases the protein expression of Nrf2, HO-1, and NQO1. Reserpine hydrochloride at concentrations of 2.5 to 10 μM decreases the mRNA expression of DNMT1, DNMT3a, and DNMT3b in a concentration-dependent manner in JB6 P+ cells after 7 days of treatment. Reserpine hydrochloride at 10 μM generates a significant difference for DNMT3a expression (p<0.05)[2].

体内研究
(In Vivo)

Withdrawal (48 h) from chronic (14-day) but not acute Reserpine hydrochloride administration in a dose of 0.2 mg/kg i.p. produces a significant reduction of the immobility time (F2,18=3.68, p<0.05), but increases the climbing time (F2,18=4.48, p<0.02), and does not change the swimming time (F2,18=1.78; NS) in the forced swim test (FST) in rats[1]. Reserpine hydrochloride at a dose of 5 mg/kg body weight produces significant increase in the urinary excretion profile of vanillylmandelic acid (VMA) compare to control animals. The amount of 5-hydroxyindoleacetic acid (5-HIAA) excreted in animals treated with Reserpine is found to be more than in the control. Dose dependent hypotension is observed with Reserpine hydrochloride. Reserpine hydrochloride at doses of 0.5, 1, 5, 10 and 15 μg/kg produce significant (p<0.01) reduction in blood pressure compare to control[3].

Clinical Trial
分子量

645.14

性状

Solid

Formula

C33H41ClN2O9

CAS 号

16994-56-2

中文名称

利血平盐酸盐

结构分类
  • Alkaloids
  • Indole Alkaloids
来源
  • Plants
  • Apocynaceae
  • Rauvolfia verticillata(Lour.) Baill.
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture and light

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

溶解性数据
In Vitro: 

DMSO : 50 mg/mL(77.50 mM;Need ultrasonic)

H2O :< 0.1 mg/mL(insoluble)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.5501 mL7.7503 mL15.5005 mL
5 mM0.3100 mL1.5501 mL3.1001 mL
10 mM0.1550 mL0.7750 mL1.5501 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℃, 6 months; -20℃, 1 month (sealed storage, away from moisture and light)。-80℃ 储存时,请在 6 个月内使用,-20℃ 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: ≥ 2.5 mg/mL (3.88 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.88 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 25.0 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 2.

    请依序添加每种溶剂: 10% DMSO    90%corn oil

    Solubility: ≥ 2.5 mg/mL (3.88 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.88 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (3.22 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (3.22 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 μL20% 的 SBE-β-CD 生理盐水水溶液中,混合均匀。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中,再用生理盐水定容至 10 mL,完全溶解,澄清透明
*以上所有助溶剂都可在本网站选购。