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Adaptaquin

编号: 20552
Cas号: 385786-48-1
纯度: 98% Min.

Adaptaquin is a hydroxyquinoline inhibitor of HIF-PHD enzymes. Adaptaquin reduces neuronal death and behavioral deficits after intracerebral hemorrhage (ICH) in several rodent models without affecting total iron or zinc distribution in the brain.

仅供研究使用。 我们不向患者出售。

化学信息

名称Adaptaquin
Iupac 化学名称7-[(4-Chlorophenyl)[(3-hydroxy-2-pyridinyl)amino]methyl]-8-quinolinol
同义词Adaptaquin
英文同义词Adaptaquin
分子式C21H16ClN3O2
分子量377.82
SmileOC1=C2N=CC=CC2=CC=C1C(C3=CC=C(Cl)C=C3)NC4=NC=CC=C4O
InChiKeyKKYHNYRUBSYTCZ-UHFFFAOYSA-N
InChiInChI=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)
Cas号385786-48-1
相关CAS号

订购信息

包装价格库存纯度备货期
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外观性状固体粉末
纯度98% Min.
存储短期(几天到几周)为0-4摄氏度,长期(几个月)为-20摄氏度
可溶性溶于DMSO
处理方式
运输条件作为非危险化学品在环境温度下装运。这种产品在正常运输和海关工作期间可以稳定几周.
海关编码
Coming soon.
Targets
Mechanism
Cell study
Animal study
Clinical study

1: Ratan RR. The Chemical Biology of Ferroptosis in the Central Nervous System. Cell Chem Biol. 2020 May 21;27(5):479-498. doi: 10.1016/j.chembiol.2020.03.007. Epub 2020 Apr 2. PMID: 32243811; PMCID: PMC7245561.


2: Aimé P, Karuppagounder SS, Rao A, Chen Y, Burke RE, Ratan RR, Greene LA. The drug adaptaquin blocks ATF4/CHOP-dependent pro-death Trib3 induction and protects in cellular and mouse models of Parkinson's disease. Neurobiol Dis. 2020 Mar;136:104725. doi: 10.1016/j.nbd.2019.104725. Epub 2020 Jan 3. PMID: 31911115; PMCID: PMC7545957.


3: Li K, Li T, Wang Y, Xu Y, Zhang S, Culmsee C, Wang X, Zhu C. Sex differences in neonatal mouse brain injury after hypoxia-ischemia and adaptaquin treatment. J Neurochem. 2019 Sep;150(6):759-775. doi: 10.1111/jnc.14790. Epub 2019 Jul 28. PMID: 31188470.


4: Vetrovoy O, Rybnikova E. Neuroprotective action of PHD inhibitors is predominantly HIF-1-independent: An Editorial for 'Sex differences in neonatal mouse brain injury after hypoxia-ischemia and adaptaquin treatment' on page 759. J Neurochem. 2019 Sep;150(6):645-647. doi: 10.1111/jnc.14822. Epub 2019 Aug 2. PMID: 31373011.


5: Poloznikov AA, Nikulin SV, Zakhariants AA, Khristichenko AY, Hushpulian DM, Gazizov IN, Tishkov VI, Gazaryan IG. "Branched Tail" Oxyquinoline Inhibitors of HIF Prolyl Hydroxylase: Early Evaluation of Toxicity and Metabolism Using Liver- on-a-chip. Drug Metab Lett. 2019;13(1):45-52. doi: 10.2174/1872312813666181129100950. PMID: 30488807.


6: David BT, Curtin JJ, Brown JL, Coutts DJC, Boles NC, Hill CE. Treatment with hypoxia-mimetics protects cultured rat Schwann cells against oxidative stress- induced cell death. Glia. 2021 Sep;69(9):2215-2234. doi: 10.1002/glia.24019. Epub 2021 May 21. PMID: 34019306.


7: Karuppagounder SS, Alim I, Khim SJ, Bourassa MW, Sleiman SF, John R, Thinnes CC, Yeh TL, Demetriades M, Neitemeier S, Cruz D, Gazaryan I, Killilea DW, Morgenstern L, Xi G, Keep RF, Schallert T, Tappero RV, Zhong J, Cho S, Maxfield FR, Holman TR, Culmsee C, Fong GH, Su Y, Ming GL, Song H, Cave JW, Schofield CJ, Colbourne F, Coppola G, Ratan RR. 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. doi: 10.1126/scitranslmed.aac6008. PMID: 26936506; PMCID: PMC5341138.


8: Neitemeier S, Dolga AM, Honrath B, Karuppagounder SS, Alim I, Ratan RR, Culmsee C. 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(5):e2214. doi: 10.1038/cddis.2016.107. PMID: 27148687; PMCID: PMC4917646.


9: Poloznikov AA, Nersisyan SA, Hushpulian DM, Kazakov EH, Tonevitsky AG, Kazakov SV, Vechorko VI, Nikulin SV, Makarova JA, Gazaryan IG. HIF Prolyl Hydroxylase Inhibitors for COVID-19 Treatment: Pros and Cons. Front Pharmacol. 2021 Jan 29;11:621054. doi: 10.3389/fphar.2020.621054. PMID: 33584306; PMCID: PMC7878396.


10: David BT, Curtin JJ, Brown JL, Scorpio K, Kandaswamy V, Coutts DJC, Vivinetto A, Bianchimano P, Karuppagounder SS, Metcalfe M, Cave JW, Hill CE. Temporary induction of hypoxic adaptations by preconditioning fails to enhance Schwann cell transplant survival after spinal cord injury. Glia. 2023 Mar;71(3):648-666. doi: 10.1002/glia.24302. Epub 2022 Dec 24. PMID: 36565279.


11: Wei GZ, Saraswat Ohri S, Khattar NK, Listerman AW, Doyle CH, Andres KR, Karuppagounder SS, Ratan RR, Whittemore SR, Hetman M. Hypoxia-inducible factor prolyl hydroxylase domain (PHD) inhibition after contusive spinal cord injury does not improve locomotor recovery. PLoS One. 2021 Apr 5;16(4):e0249591. doi: 10.1371/journal.pone.0249591. PMID: 33819286; PMCID: PMC8021188.


12: Poloznikov AA, Nikulin SV, Hushpulian DM, Khristichenko AY, Osipyants AI, Asachenko AF, Shurupova OV, Savin SS, Lee SH, Gaisina IN, Thatcher GRJ, Narciso A, Chang EP, Kazakov SV, Krucher N, Tishkov VI, Thomas B, Gazaryan IG. Structure-Activity Relationships and Transcriptomic Analysis of Hypoxia- Inducible Factor Prolyl Hydroxylase Inhibitors. Antioxidants (Basel). 2022 Jan 24;11(2):220. doi: 10.3390/antiox11020220. PMID: 35204103; PMCID: PMC8868400.


13: Osipyants AI, Poloznikov AA, Smirnova NA, Hushpulian DM, Khristichenko AY, Chubar TA, Zakhariants AA, Ahuja M, Gaisina IN, Thomas B, Brown AM, Gazaryan IG, Tishkov VI. L-ascorbic acid: A true substrate for HIF prolyl hydroxylase? Biochimie. 2018 Apr;147:46-54. doi: 10.1016/j.biochi.2017.12.011. Epub 2017 Dec 28. PMID: 29289682; PMCID: PMC6460286.

化学结构

20552 - Adaptaquin | CAS 385786-48-1

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