Jatrorrhizine chloride

SKU: orb1220279

Description

Jatrorrhizine chloride is a potent and orally active uptake-2 transporter inhibitor. It exhibits a critical neuroprotective role in H2O2-induced apoptosis via inhibition of the MAPK pathway in HT22 hippocampal neurons.

Images & Validation

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Key Properties

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CAS Number	6681-15-8
MW	373.8
Purity	>98% (HPLC)
Formula	C₂₀H₂₀ClNO₄
SMILES	COc(ccc1cc(-c(cc2OC)c(CC3)cc2O)[n+]3cc11)c1OC.[Cl-]
Target	OCT\| PMAT
Solubility	DMSO:5 mg/mL (13.38 mM)

Bioactivity

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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). Animal model: Male ICR albino mice. Dosage: 5, 10, 20 mg/kg. Administration: Intraperitoneal injection; 5, 10, 20 mg/kg. Result: Reduced immobility period in tail suspension test.

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. The hOCT2 (organic cation transporter 2), hOCT3, and PMAT (plasma membrane monoamine transporter) are capable of transporting monoamine neurotransmitters in the brain. 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). 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.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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Neprotine chloride | Yatrorhizine chloride

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Gene Symbol

OCT| PMAT

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