Axon 2552
CAS [252025-52-8]
MF C15H12Cl2N4OMW 335.19
Non-hormonal male contraceptive that exerts its effect by disrupting Sertoli-germ cell adhesion junctions, most notably apical ectoplasmic specialization (apical ES), by targeting testin and actin filament bundles that disrupt the actin-based cytoskeleton in Sertoli cells. Adjudin is a potent blocker of Cl- channels. Moreover, Adjudin is shown to induce apoptosis in cancer cells through a Caspase-3-dependent pathway, and triggers mitochondrial dysfunction in cancer cells, apparently affecting the mitochondrial mass, inducing the loss of mitochondrial membrane potential and reducing cellular ATP levels. Furthermore, Adjudin posesses anti-inflammation, anti-neurodegeneration, and anti-ototoxicity activities based on studies using different in vitro and in vivo models.
KEYWORDS: Adjudin | supplier | Male contraceptive | AF 2364 | AF2364 | CAS [252025-52-8] | Chloride | CFTR | Inhibitor | Ion Channels | fertility | actin | testin | Sertoli-germ | apical ectoplasmic specialization | cytoskeleton | blocker | apoptosis | Caspase-3 | mitochondrial | dysfunction | cancer cells | membrane potential | ATP
CY Cheng et al. Two new male contraceptives exert their effects by depleting germ cells prematurely from the testis. Biol Reprod. 2001 Aug;65(2):449-61. |
QR Xie et al. Male contraceptive Adjudin is a potential anti-cancer drug. Biochem Pharmacol. 2013 Feb 1;85(3):345-55. |
K Li et al. Inhibition of sperm capacitation and fertilizing capacity by adjudin is mediated by chloride and its channels in humans. Hum Reprod. 2013 Jan;28(1):47-59. |
YH Cheng et al. Adjudin - A Male Contraceptive with Other Biological Activities. Recent Pat Endocr Metab Immune Drug Discov. 2015;9(2):63-73. |
1-(2,4-dichlorobenzyl)-1H-indazole-3-carbohydrazide
[252025-52-8]
Axon Medchem的业务之一,是独有的Axon Ligands配体库,在世界范围内,被认为是药物研发的标准。这其中,针对850余种生物靶标(包括细胞信号、基因转录、凋亡、细胞周期调控、CNS等),Axon Medchem拥有多达2000余种小分子抑制剂或调节剂。除了配体库,Axon Medchem还是欧洲著名的CRO公司,主要针对生物活性分子和药物类似分子展开合成及协议开发工作,在过去的10年中,Axon Medchem已经发现了多种潜在药物分子,并在生物医药界享有一定的声誉。