874484-20-5|N-(2-(2-Methoxy-6H-dipyrido[2,3-a:3',2'-e]pyrrolizin-11-yl)ethyl)furan-2-carboxamide|CsnPharm

CAS No.: 874484-20-5

S29434 Catalog No. CSN24723

Synonyms: NMDPEF

S29434 is a potent, nanomolar inhibitor of QR2 with IC₅₀ of 5-16 nM at different organizational levels.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述Quinone reductase 2 (QR2) is an enzyme which recognizes putative metabolites of NADH, such as N-methyl- and N-ribosyl-dihydronicotinamide. It has been particularly associated with reactive oxygen species and memory, strongly suggesting a link among QR2 (as a possible key element in pro-oxidation), autophagy, and neurodegeneration^[1]. S29434 is a potent, nanomolar inhibitor of QR2 with IC₅₀ of 5-16 nM at different organizational levels^[1]. Paraquat (PQ) (30 mg/kg) and S29434 were administered i.p. to Wistar rats and animals were monitored for 28 days. S29434 potently antagonized non-apoptotic PQ-induced cell death, reactive oxygen species (ROS) generation and inhibited cellular QR2 activity. Significantly, S29434 (4.5 mg/kg) potently antagonized PQ-induced systemic toxicity and animal mortality. Microinfusion of S29434 into substantia nigra (SN) prevented severe behavioural and electrocortical effects of PQ which correlated with inhibition of malondialdehyde accumulation in cells and tissues^[2].
作用机制S29434 fits deeply into a QR2 hydrophobic cavity (Protein Data Bank: 3OX3), interacting with subunits A and B with its amido-furan side chains pointing toward the solvent.
参考文献

[1] Boutin JA, Bouillaud F, Janda E, Gacsalyi I, Guillaumet G, Hirsch EC, Kane DA, Nepveu F, Reybier K, Dupuis P, Bertrand M, Chhour M, Le Diguarher T, Antoine M, Brebner K, Da Costa H, Ducrot P, Giganti A, Goswami V, Guedouari H, Michel PP, Patel A, Paysant J, Stojko J, Viaud-Massuard MC, Ferry G. S29434, a Quinone Reductase 2 Inhibitor: Main Biochemical and Cellular Characterization. Mol Pharmacol. 2019 Mar;95(3):269-285. doi: 10.1124/mol.118.114231. Epub 2018 Dec 19. PMID: 30567956.
[2] Janda E, Parafati M, Aprigliano S, Carresi C, Visalli V, Sacco I, Ventrice D, Mega T, Vadalá N, Rinaldi S, Musolino V, Palma E, Gratteri S, Rotiroti D, Mollace V. The antidote effect of quinone oxidoreductase 2 inhibitor against paraquat-induced toxicity in vitro and in vivo. Br J Pharmacol. 2013 Jan;168(1):46-59. doi: 10.1111/j.1476-5381.2012.01870.x. PMID: 22289031; PMCID: PMC3570002.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.6710 mL
- 13.3550 mL
- 26.7099 mL
- 5 mM
- 0.5342 mL
- 2.6710 mL
- 5.3420 mL
- 10 mM
- 0.2671 mL
- 1.3355 mL
- 2.6710 mL

技术信息

CAS号

874484-20-5

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H18N4O3

运输

蓝冰

分子量

374.39

别名

NMDPEF

溶解度

DMSO	17.0 mg/mL (45.4 mM)
Water	insoluble

动物实验配方

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