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Adjudin

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Chemical Structure| 252025-52-8 同义名 : AF-2364
CAS号 : 252025-52-8
货号 : A946828
分子式 : C15H12Cl2N4O
纯度 : 98%
分子量 : 335.19
MDL号 : MFCD06198883
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: 16 mg/mL(47.73 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 Adjudin, a small molecule compound known to possess antispermatogenic function, attenuates microglia activation by suppression of the NF-κB pathway. Adjudin protects against cerebral ischemia reperfusion injury[3]. Adjudin, a potential non-hormonal male contraceptive, exhibits additional function to reduce the production of proinflammatory mediators. Adjudin significantly inhibited LPS-induced IL-6 release and IL-6, IL-1β, TNF-α expression in BV2 microglial cells. Furthermore, Adjudin exhibited anti-inflammatory properties by suppression of NF-κB p65 nuclear translocation and DNA binding activity as well as ERK MAPK phosphorylation[4]. Adjudin attenuated the development of TBI-induced (traumatic brain injury) cerebral edema at least partly via anti-inflammatory effects and inhibition of the NF-κB pathway[5]. Adjudin induced apoptosis in cancer cells through a Caspase-3-dependent pathway. Adjudin could trigger mitochondrial dysfunction in cancer cells, apparently affecting the mitochondrial mass, inducing the loss of mitochondrial membrane potential and reducing cellular ATP levels. Intraperitoneal administration of Adjudin to tumor-bearing athymic nude mice also significantly suppressed the lung and prostate tumor growth. When used in combination with cisplatin, Adjudin enhances the sensitivity to cisplatin-induced cancer cell cytotoxicity[6]. Adjudin acts through activation of mitochondrion-located Sirt3 to safeguard hair cells of the cochlea from ototoxicant such as gentamycin. Adjudin could attenuate oxidative stress and cellular senescence[7].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.98mL

0.60mL

0.30mL

14.92mL

2.98mL

1.49mL

29.83mL

5.97mL

2.98mL

参考文献

[1]Quan Y, Xia L, et al. Adjudin protects rodent cochlear hair cells against gentamicin ototoxicity via the SIRT3-ROS pathway. Sci Rep. 2015 Feb 2;5:8181.

[2]Liu T, Zhang T, et al. Adjudin protects against cerebral ischemia reperfusion injury by inhibition of neuroinflammation and blood-brain barrier disruption. J Neuroinflammation. 2014 Jun 14;11:107.

[3]Liu T, Zhang T, Yu H, Shen H, Xia W. Adjudin protects against cerebral ischemia reperfusion injury by inhibition of neuroinflammation and blood-brain barrier disruption. J Neuroinflammation. 2014 Jun 14;11:107

[4]Shao J, Liu T, Xie QR, Zhang T, Yu H, Wang B, Ying W, Mruk DD, Silvestrini B, Cheng CY, Xia W. Adjudin attenuates lipopolysaccharide (LPS)- and ischemia-induced microglial activation. J Neuroimmunol. 2013 Jan 15;254(1-2):83-90

[5]Liu YL, Yuan F, Yang DX, Xu ZM, Jing Y, Yang GY, Geng Z, Xia WL, Tian HL. Adjudin Attenuates Cerebral Edema and Improves Neurological Function in Mice with Experimental Traumatic Brain Injury. J Neurotrauma. 2018 Dec 1;35(23):2850-2860

[6]Xie QR, Liu Y, Shao J, Yang J, Liu T, Zhang T, Wang B, Mruk DD, Silvestrini B, Cheng CY, Xia W. Male contraceptive Adjudin is a potential anti-cancer drug. Biochem Pharmacol. 2013 Feb 1;85(3):345-55

[7]Xia W, Geng K. A sirtuin activator and an anti-inflammatory molecule-multifaceted roles of adjudin and its potential applications for aging-related diseases. Semin Cell Dev Biol. 2016 Nov;59:71-78