Description
Adaptaquin is a selective hydroxyquinoline HIF prolyl hydroxylase (HIF-PHD) inhibitor . The hypoxia-inducible factor prolyl hydroxylase domain enzymes (HIF-PHDs) are a family of oxygen sensors that has been implicated in neuronal survival. Catalysis by the HIF-PHDs destabilizes the transcriptional activator HIF-1a under normoxia. HIF-PHDs are promising target candidates for mitochondrial protection in paradigms of oxidative stress. The inhibition of HIF-PHDs prevented neuronal cell death induced by mitochondrial toxins . Adaptaquin is a hydroxyquinoline HIF-PHD inhibitor. Adaptaquin inhibited purified and recombinant PHD2. Adaptaquin (30 mg/kg) penetrated the blood-brain barrier, resulting in inhibition of the oxygen-sensing HIF-PHDs and activation of HIF-dependent gene expression . In HT-22 cells, Adaptaquin protected against glutamate-induced cell death. Adaptaquin could also restore the mitochondrial ATP production . In intracerebral hemorrhage (ICH) mice model, Adaptaquin decreased edema and significantly improved tape removal task, which were associated with a reduction in the number of degenerating neurons in perihematomal and hematomal areas of the mouse striatum .
Product information
CAS Number: 385786-48-1
Molecular Weight: 377.82
Formula: C21H16ClN3O2
Chemical Name: 7-[(4-chlorophenyl)[(3-hydroxypyridin-2-yl)amino]methyl]quinolin-8-ol
Smiles: OC1=CC=CN=C1NC(C1C=CC2=CC=CN=C2C=1O)C1C=CC(Cl)=CC=1
InChiKey: KKYHNYRUBSYTCZ-UHFFFAOYSA-N
InChi: InChI=1S/C21H16ClN3O2/c22-15-8-5-14(6-9-15)18(25-21-17(26)4-2-12-24-21)16-10-7-13-3-1-11-23-19(13)20(16)27/h1-12,18,26-27H,(H,24,25)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥12 months if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
Products are for research use only. Not for human use.
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