产品说明书

S29434

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Chemical Structure| 874484-20-5 同义名 : NMDPEF
CAS号 : 874484-20-5
货号 : A1191668
分子式 : C21H18N4O3
纯度 : 99%+
分子量 : 374.393
MDL号 : MFCD28160701
存储条件:

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 18 mg/mL(48.08 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
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.
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.67mL

0.53mL

0.27mL

13.35mL

2.67mL

1.34mL

26.71mL

5.34mL

2.67mL

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.