Adjudin

Adjudin is a derivative of ionidamine that inhibits human spermatozoa capacitance, potentially by blocking chloride channels.¹ It inhibits spermatozoa hyperactivated motility and the acrosome reaction and prevents sperm-egg fusion in zona-free hamster eggs. It also disrupts Sertoli-germ cell junctions by increasing tight junction and basal ectoplasmic specialization protein levels, which tightens the cell permeability barrier dose-dependently in vitro.² Adjudin (25 and 50 mg/kg) increases testin expression in adult rat testes within one day and depletes spermatids and spermatocytes within 14 days.³ Under various dosing parameters, adjudin reversibly induces infertility of male rats within 3-7 weeks, which lasts 4-14 weeks, without affecting serum levels of luteinizing hormone (LH), follicle stimulating hormone (FSH), or testosterone. Adjudin also decreases proliferation of SGC-7901, MDA-MB-231, Smmc-7721, and MIA Paca-2 cells (IC₅₀s = 58, 13.8, 72.3, and 52.7 µM, respectively) and induces apoptosis via the caspase-3-dependent pathway.⁴

WARNING This product is not for human or veterinary use.

1. Li, K., Ni, Y., He, Y., et al. Inhibition of sperm capacitation and fertilizing capacity by adjudin is mediated by chloride and its channels in humans. Hum. Repod. 28(1), 47-59 (2013).

2. Su, L., Cheng, C.Y., and Mruk, D.D. Adjudin-mediated Sertoli-germ cell junction disassembly affects Sertoli cell barrier function in vitro and in vivo. Int. J. Biochem. Cell Biol. 42(11), 1864-1875 (2010).

3. Cheng, C.Y., Silvestrini, B., Grima, J., et al. Two new male contraceptives exert their effects by depleting germ cells prematurely from the testis. Biol. Reprod. 65(2), 449-461 (2001).

4. Xie, Q.R., Liu, Y., Shao, J., et al. Male contraceptive Adjudin is a potential anti-cancer drug. Biochem. Pharmacol. 85(3), 345-355 (2013).