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  3. Jatrorrhizine hydroxide

Jatrorrhizine hydroxide is an alkaloid isolated from Coptis chinensis with neuroprotective, antimicrobial, antiplasmodial and antioxidant activities. Jatrorrhizine hydroxide is a potent and orally active inhibitor of AChE (IC50=872 nM) over >115-fold selectivity for BuChE. Jatrorrhizine hydroxide reduces uptake of serotonin (5-HT) and norepinephrine (NE) via inhibition of uptake-2 transporters.

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Jatrorrhizine hydroxide Chemical Structure

Jatrorrhizine hydroxide Chemical Structure

CAS No. : 483-43-2

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Description

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

IC50 & Target

IC50: 872 nM (AChE)[1]

In Vitro

Jatrorrhizine has antiplasmodial and antiamoebic activity, it against Plasmodium falciparum and E. histolytica with IC50 values 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 IC50 value of 1.05 μM and reduces 5-HT and NE uptake mediated by hOCT2, hOCT3, and hPMAT with IC50 values 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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

355.38

Formula

C20H21NO5

CAS No.
Appearance

Solid

Color

Brown to black

SMILES

COC1=C(OC)C2=C[N+]3=C(C4=CC(OC)=C(O)C=C4CC3)C=C2C=C1.[OH-]

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Solvent & Solubility
In Vitro: 

H2O : 5 mg/mL (14.07 mM; Need ultrasonic)

DMSO : 3.33 mg/mL (9.37 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8139 mL 14.0694 mL 28.1389 mL
5 mM 0.5628 mL 2.8139 mL 5.6278 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
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Working solution concentration: mg/mL
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO / H2O 1 mM 2.8139 mL 14.0694 mL 28.1389 mL 70.3472 mL
5 mM 0.5628 mL 2.8139 mL 5.6278 mL 14.0694 mL
H2O 10 mM 0.2814 mL 1.4069 mL 2.8139 mL 7.0347 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Product Name:
Jatrorrhizine hydroxide
Cat. No.:
HY-N0749A
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