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WUHAN SUN-SHINE BIO-TECHNOLOGY Co., Ltd.
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Product Name:Adaptaquin
CAS:385786-48-1
Purity:98% HPLC Package:50.0mg;100.0mg; 200.0mg;500mg;1g;5g; 10g
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| Company Name: |
BOC Sciences
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| Products Intro: |
Product Name:Adaptaquin
CAS:385786-48-1
Purity:97% by HPLC Remarks:Adaptaquin is an inhibitor of hypoxia-inducible factor (HIF) prolyl hydroxylase 2 (PHD2) with IC50 value of 2 μM in a reporter assay using SH-SY5Y-ODD-Luc cells. It displays neuroprotective effects an
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| | Adaptaquin Basic information |
| Product Name: | Adaptaquin | | Synonyms: | Adaptaquin;HIF Prolyl Hydroxylase Inhibitor - CAS 385786-48-1 - Calbiochem;7-[(4-Chlorophenyl)[(3-hydroxy-2-pyridinyl)amino]methyl]-8-quinolinol;Hypoxia-inducible factors,peroxidation,mitochondrial,HIFs,HIF-PH,inhibit,HIF-PHD2,HIF/HIF Prolyl-Hydroxylase,Adaptaquin,Inhibitor;8-Quinolinol, 7-[(4-chlorophenyl)[(3-hydroxy-2-pyridinyl)amino]methyl]-;7-((4-Chlorophenyl)((3-hydroxypyridin-2-yl)amino)methyl)quinolin-8-ol | | CAS: | 385786-48-1 | | MF: | C21H16ClN3O2 | | MW: | 377.82 | | EINECS: | | | Product Categories: | | | Mol File: | 385786-48-1.mol |  |
| | Adaptaquin Chemical Properties |
| Boiling point | 650.9±55.0 °C(Predicted) | | density | 1.437±0.06 g/cm3(Predicted) | | storage temp. | -20C | | solubility | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide | | form | Tan solid | | pka | 4.07±0.50(Predicted) |
| | Adaptaquin Usage And Synthesis |
| Uses | General Uses:Ischemic injury Research, Renal anemia, HIF Prolyl Hydroxylase Inhibitor, Antioxidant, NeuroprotectiveDescription:Adaptaquin inhibits the HIF PHDs in brain in a dose dependent fashion and penetrates blood brain barrier (BBB). Exhibited functional recovery in intra-cerebral hemorrhage rat model; inhibits ATF4 gene. Potent HIF PHD inhibitor (hypoxia inducible factor), Selective PDH2 inhibitor.This compound is suitable for pyruvate dehydrogenase (PDH) related research. | | Biological Activity | adaptaquin is a selective hydroxyquinoline hif prolyl hydroxylase (hif-phd) inhibitor [1][2].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 [1][2].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 [1]. in ht-22 cells, adaptaquin protected against glutamate-induced cell death. adaptaquin could also restore the mitochondrial atp production [2].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 [1]. | | Enzyme inhibitor | This brain-penetrant PHD2 inhibitor and antioxidant (FW = 377.82 g/mol; CAS 385786-48-1; Soluble to 100 mM in DMSO), also named 7-[(4chlorophenyl)[(3-hydroxy-2-pyridinyl)amino]methyl]-8-quinolinol, targets Hypoxia-Inducible Factor (or HIF) prolyl hydroxylase-2, a critical regulator of hematopoietic stem cell (HSC) maintenance during steadystate and stress. Indeed, this branched oxyquinoline molecule was named adaptaquin (AQ) to signify its ability to inhibit the HIF-PHDs and activate adaptive responses to hypoxia. Hypoxia is a prominent feature in the maintenance of HSC quiescence and multipotency. Adaptaquin also exhibits neuroprotective effects, enhancing functional recovery in rodent intracerebral hemorrhage models, via inhibition of ATF4 dependent genes. | | storage | Store at -20°C | | references | [1]. karuppagounder ss, alim i, khim sj, et al. therapeutic targeting of oxygen-sensing prolyl hydroxylases abrogates atf4-dependent neuronal death and improves outcomes after brain hemorrhage in several rodent models. sci transl med. 2016 mar 2;8(328):328ra29.
[2]. neitemeier s, dolga am, honrath b, et al. inhibition of hif-prolyl-4-hydroxylases prevents mitochondrial impairment and cell death in a model of neuronal oxytosis. cell death dis. 2016 may 5;7:e2214. |
| | Adaptaquin Preparation Products And Raw materials |
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