Adaptaquin (Synonyms: HIF prolyl hydroxylase inhibitor) |
| رقم الكتالوجGC12487 |
Adaptaquin هو مثبط للعامل المحرض بنقص الأكسجة ، بروليل هيدروكسيلاز 2 (HIF-PHD2) ، مع IC 50 من 2 ميكرومتر
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 385786-48-1
Sample solution is provided at 25 µL, 10mM.
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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].
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.
| Cas No. | 385786-48-1 | SDF | |
| المرادفات | HIF prolyl hydroxylase inhibitor | ||
| Chemical Name | 7-[(4-chlorophenyl)[(3-hydroxy-2-pyridinyl)amino]methyl]-8-quinolinol | ||
| Canonical SMILES | OC1=CC=CN=C1NC(C2=CC=C(Cl)C=C2)C3=C(O)C(N=CC=C4)=C4C=C3 | ||
| Formula | C21H16ClN3O2 | M.Wt | 377.8 |
| الذوبان | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.6469 mL | 13.2345 mL | 26.469 mL |
| 5 mM | 0.5294 mL | 2.6469 mL | 5.2938 mL |
| 10 mM | 0.2647 mL | 1.3235 mL | 2.6469 mL |
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Quality Control & SDS
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- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
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Average Rating: 5 (Based on Reviews and 21 reference(s) in Google Scholar.)
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