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Adaptaquin Sale

(Synonyms: HIF prolyl hydroxylase inhibitor) 目录号 : GC12487

An inhibitor of HIF-PH2

Adaptaquin Chemical Structure

Cas No.:385786-48-1

规格 价格 库存 购买数量
5mg
¥612.00
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10mg
¥1,020.00
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50mg
¥3,263.00
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Sample solution is provided at 25 µL, 10mM.

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产品描述

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.

Chemical Properties

Cas No. 385786-48-1 SDF
别名 HIF prolyl hydroxylase inhibitor
化学名 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
分子式 C21H16ClN3O2 分子量 377.8
溶解度 ≤30mg/ml in DMSO;30mg/ml in dimethyl formamide 储存条件 Store at -20°C
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储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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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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