Adaptaquin is an inhibitor of HIF-PHD2 with an IC50 of 2 μM. It can inhibit lipid peroxidation and preserve mitochondrial function[1][2].
Adaptaquin 细胞实验
Cell Line
Concentration
Treated Time
Description
References
immortalized striatal neuroblasts (Q7 cells)
0.25–10 mM
24 h
To investigate the protective effects of adaptaquin against hemin-induced toxicity. Adaptaquin significantly reduced neuronal death in all three cell types, with EC50 values of 34.1 µM in primary cortical neurons, 50.8 µM in HT22 cells, and 26.7 µM in Q7 cells
Sci Transl Med. 2016 Mar 2;8(328):328ra29
HT-22 cells
2 μM
15 h
Adaptaquin inhibits HIF-PHDs, preventing glutamate-induced oxidative stress and cell death, and maintains mitochondrial function.
Cell Death Dis. 2016 May 5;7(5):e2214
Ventral midbrain dopaminergic (VM DA) neurons
0.5 μM
24 h
To evaluate the neuroprotective potential of Adaptaquin against 6-OHDA and MPP+-induced dopaminergic neuron death. Results showed that 0.5 μM Adaptaquin significantly protected dopaminergic neurons from the toxicity of 6-OHDA and MPP+.
Neurobiol Dis. 2020 Mar;136:104725
Neuronal PC12 cells
0.5 μM
48 h
To evaluate the neuroprotective potential of Adaptaquin against MPP+-induced cell death. Results showed that 0.5 μM Adaptaquin significantly increased cell survival and reduced the formation of intracellular vacuoles.
Neurobiol Dis. 2020 Mar;136:104725
Neuronal PC12 cells
0.1 μM, 0.5 μM, 1 μM, 5 μM
24 h
To evaluate the neuroprotective potential of Adaptaquin against 6-OHDA-induced cell death. Results showed that 0.5 μM and higher concentrations of Adaptaquin significantly protected PC12 cells from 6-OHDA-induced cell death and preserved cell morphology.
Neurobiol Dis. 2020 Mar;136:104725
Schwann cells
10 μM
16 h
Induction of hypoxia-related adaptive responses, including increased expression of HIF-1α and its target genes
Glia. 2023 Mar;71(3):648-666
rat Schwann cells
10 μM
16 h
To evaluate the effect of Adaptaquin on HIF-1α stabilization and HIF-1α target gene transcriptional activity in Schwann cells. Results showed that Adaptaquin significantly increased HIF-1α stabilization and HIF-1α target gene transcriptional activity.
Glia. 2021 Sep;69(9):2215-2234
Adaptaquin 动物实验
Species
Animal Model
Administration
Dosage
Frequency
Description
References
Mice
Collagenase-induced ICH model
Intraperitoneal injection
30 mg/kg
Once daily for 7 days
To evaluate the effect of adaptaquin on functional recovery after ICH, results showed that adaptaquin significantly improved sensorimotor function and reduced neuronal degeneration
Sci Transl Med. 2016 Mar 2;8(328):328ra29
C57BL/6 mice
6-OHDA-induced Parkinson’s disease model
Intraperitoneal injection
30 mg/kg
Once daily for 7 days
To evaluate the protective effects of Adaptaquin on 6-OHDA-induced death of substantia nigra dopaminergic neurons and striatal TH immunoreactivity. Results showed that Adaptaquin significantly increased the survival of dopaminergic neurons in the substantia nigra and partially restored TH immunoreactivity in the striatum. Additionally, Adaptaquin significantly improved motor function.
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