| AdaptaquinHIF-prolyl hydroxylase-2 (PHD2) inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity ≥ 95.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
Chemical structure
Adaptaquin Dilution Calculator
calculate
Adaptaquin Molarity Calculator
calculate
| Cas No. | 385786-48-1 | SDF | Download SDF |
| Synonyms | 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 |
| Solubility | ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
