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Amodiaquine hydrochloride

Catalog No. T22242 CAS 69-44-3

Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a member of the 4-aminoquinoline class, serves as an antimalarial agent and exhibits potent oral activity as a histamine N-methyltransferase inhibitor, displaying a K i value of 18.6 nM. Additionally, it acts as a Nurr1 agonist, targeting the Nurr1-LBD (ligand binding domain) with an EC 50 of approximately 20 μM, thereby demonstrating an anti-inflammatory effect [1] [2] [3] [4] [5].

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Amodiaquine hydrochloride Chemical Structure

Amodiaquine hydrochloride, CAS 69-44-3

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Biological Description

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Description	Amodiaquine dihydrochloride (Amodiaquin dihydrochloride), a member of the 4-aminoquinoline class, serves as an antimalarial agent and exhibits potent oral activity as a histamine N-methyltransferase inhibitor, displaying a K i value of 18.6 nM. Additionally, it acts as a Nurr1 agonist, targeting the Nurr1-LBD (ligand binding domain) with an EC 50 of approximately 20 μM, thereby demonstrating an anti-inflammatory effect [1] [2] [3] [4] [5].
In vitro	Amodiaquine treatment ranging from 10-20 μM for 4 hours significantly reduces the expression of proinflammatory cytokines (IL-1β, interleukin-6, TNF-α, and iNOS) induced by LPS in a dose-dependent manner. Additionally, at a concentration of 5 μM over 24 hours, Amodiaquine markedly diminishes 6-OHDA-induced cell death in primary dopamine neurons, as evidenced by the preservation of TH+ neuron numbers and dopamine uptake. This neuroprotective effect is corroborated in rat PC12 cells. RT-PCR results from primary microglia treated with 10 μM, 15 μM, and 20 μM Amodiaquine for 4 hours further confirm the suppression of LPS-induced proinflammatory cytokine expression, demonstrating Amodiaquine’s potent anti-inflammatory and neuroprotective activities.
In vivo	Amodiaquine administration (40 mg/kg; intraperitoneal injection; daily for 3 days) in male ICR mice aged 8-10 weeks with induced intracerebral hemorrhage (ICH) significantly diminished the activation of perihematomal microglia/macrophages and astrocytes. Furthermore, the treatment effectively suppressed ICH-induced mRNA expression levels of IL-1β, CCL2, and CXCL2, concurrently ameliorating the motor dysfunction observed in these animals.

Molecular Weight	428.78
Formula	C20H24Cl3N3O
CAS No.	69-44-3

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Powder: -20°C for 3 years | In solvent: -80°C for 1 year

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Keywords

Amodiaquine hydrochloride 69-44-3 Amodiaquine Hydrochloride inhibitor inhibit

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