Jatrorrhizine

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Jatrorrhizine

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。

CAS NO:

3621-38-3

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
20mg	电议

产品介绍

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

IC₅₀& Target

IC50: 872 nM (AChE)^[1]

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 (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

338.38

Formula

C₂₀H₂₀NO₄⁺

CAS 号

3621-38-3

结构分类

Alkaloids
Isoquinoline Alkaloids

Phenols
Monophenols

来源

Plants
other families

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

溶解性数据

In Vitro:

H₂O : 5 mg/mL(14.78 mM;Need ultrasonic)

DMSO : 3.33 mg/mL(9.84 mM;Need ultrasonic)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.9553 mL	14.7763 mL	29.5526 mL
5 mM	0.5911 mL	2.9553 mL	5.9105 mL
10 mM	0.2955 mL	1.4776 mL	2.9553 mL