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Jatrorrhizine chloride
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。
Jatrorrhizine chloride图片
CAS NO:6681-15-8
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
20mg电议
50mg电议
100mg电议

产品介绍
Jatrorrhizine chloride 是从黄连中分离得到的生物碱,具有神经保护、抗菌、抗疟原虫和抗氧化活性。Jatrorrhizine chloride 是有效的,具有口服活性的乙酰胆碱酯酶 (AChE) (IC50=872 nM) 的抑制剂,是对 BuChE 的选择性为 115 倍。Jatrorrhizine chloride 通过抑制 uptake-2 transporter 的活性减少血清素 (5-HT) 和去甲肾上腺素 (NE) 的摄取。
生物活性

Jatrorrhizine chloride is an alkaloid isolated from Coptis chinensiswith neuroprotective, antimicrobial, antiplasmodial and antioxidant activities[1]. Jatrorrhizine chloride is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE[2]. Jatrorrhizine chloride reduces uptake ofserotonin (5-HT)andnorepinephrine (NE)via inhibition of uptake-2 transporters[3].

IC50& Target

AChE

 

体外研究
(In Vitro)

Jatrorrhizine has antiplasmodial and antiamoebic activity, it againstPlasmodium falciparumandE. histolyticawith IC50values of 3.15 and 82.7 μM, respectively[1].
The hOCT2 (organic cation transporter 2), hOCT3, and PMAT (plasma membrane monoamine transporter) are capable of transporting monoamine neurotransmitters in the brain[3].
Jatrorrhizine has the inhibitory potency of jatrorrhizine on 5-HT and NE uptake in hOCT2-, hOCT3-, and PMAT-transfected cells. Jatrorrhizine strongly inhibits PMAT-mediated MPP+uptake with an IC50value of 1.05 μM and reduces 5-HT and NE uptake mediated by hOCT2, hOCT3, and hPMAT with IC50values of 0.1-1 μM (for OCT2 and OCT3) and 1-10 μM (for PMAT)[3].
Clearance of neurotransmitters released into the synaptic cleft is defined by two distinct processes. Uptake-1, the common target of current applied antidepressants, is comprised of the serotonin transporter (SERT), the “SERT”, had a high affinity but low capacity to take up [3H]5-HT. Uptake-2 transporters are an important supplementary regulation system in monoamine clearancethought to be the “NET”, has low affinity but high capacity to take up [3H]5-HT into brain slices.
Jatrorrhizine significantly inhibited 5-HT and NE uptake in synaptosomes at 25 μM and 50 μM[3].

体内研究
(In Vivo)

Jatrorrhizine chloride (intraperitoneal injection; 5, 10, 20 mg/kg) can significantly reduce the duration of immobility when compared with vehicle control group in tail suspension test (TST)[2].

Animal Model:Male ICR albino mice[2]
Dosage:5, 10, 20 mg/kg
Administration:Intraperitoneal injection; 5, 10, 20 mg/kg
Result:Reduced immobility period in tail suspension test.
分子量

373.83

性状

Solid

Formula

C20H20ClNO4

CAS 号

6681-15-8

结构分类
  • Alkaloids
  • Isoquinoline Alkaloids
  • Phenols
  • Monophenols
来源
  • Plants
  • Ranunculaceae
  • Coptis chinensisFranch.
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 : 5 mg/mL(13.38 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.6750 mL13.3751 mL26.7501 mL
5 mM0.5350 mL2.6750 mL5.3500 mL
10 mM0.2675 mL1.3375 mL2.6750 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)。-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: ≥ 2.08 mg/mL (5.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.56 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。

    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% (20%SBE-β-CDin saline)

    Solubility: ≥ 2.08 mg/mL (5.56 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (5.56 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。