CP21

CP21 is an iron chelator that binds to iron in a 3:1 (ligand:iron) ratio.¹ It is active against P. falciparum when used at concentrations of 10 and 100 µM.² CP21 inhibits production of prostaglandin I₂ (PGI₂; Item No. 18220) induced by epinephrine, arachidonic acid (Item Nos. 90010 | 90010.1 | 10006607), or A23187 (Item No. 11016) in isolated rat aortic rings with IC₅₀ values of 1.3, 1.3, and 1.4 mM, respectively.³ It inhibits glutamate-induced oxytosis, as well as decreases iodoacetic acid-induced cytotoxicity in an in vitro model of ischemia, in HT22 mouse hippocampal cells (EC₅₀s = 13 and 9.5 µM, respectively).⁴ CP21 (200 mg/kg) increases the excretion of iron, but not copper, zinc, calcium, or magnesium, in rabbits.⁵

WARNING This product is not for human or veterinary use.

1. Dobbin, P.S., Hider, R.C., Hall, A.D., et al. Synthesis, physicochemical properties, and biological evaluation of N-substituted 2-alkyl-3-hydroxy-4(1H)-pyridinones: Orally active iron chelators with clinical potential. J. Med. Chem. 36(17), 2448-2458 (1993).

2. Heppner, D.G., Hallaway, P.E., Kontoghiorghes, G.J., et al. Antimalarial properties of orally active iron chelators. Blood 72(1), 358-361 (1988).

3. Jeremy, J.Y., Kontoghiorghes, G.J., Hoffbrand, A.V., et al. The iron chelators desferrioxamine and 1-alkyl-2-methyl-3-hydroxypyrid-4-ones inhibit vascular prostacyclin synthesis in vitro. Biochem. J. 254(1), 239-244 (1988).

4. Maher, P., and Kontoghiorghes, G.J. Characterization of the neuroprotective potential of derivatives of the iron chelating drug deferiprone. Neurochem. Res. 40(3), 609-620 (2015).

5. Kontoghiorghes, G.J., and Hoffbrand, A.V. Orally active α-ketohydroxy pyridine iron chelators intended for clinical use: In vivo studies in rabbits. Br. J. Haematol. 62(4), 607-613 (1986).