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CI 972 anhydrous is a potent, orally active, and competitive inhibitor of purine nucleoside phosphorylase (PNP) (Ki=0.83 μM) under development as a T cell-selective immunosuppressive agent[1][2]. Ki: 0.83 μM (PNP)[1]

CI 972 anhydrous (5-150 mg/kg; p.o.) produces dose-dependent elevation of plasma inosine one hour after administration to rats[1].

[1]. Gilbertsen RB, et al. Biochemical and pharmacological properties of CI-972, a novel 9-deazaguanine analog purine nucleoside phosphorylase (PNP) inhibitor. Adv Exp Med Biol. 1991;309A:41-4. [2]. Gilbertsen RB,et al. Selective in vitro inhibition of human MOLT-4 T lymphoblasts by the novel purine nucleoside phosphorylase inhibitor, CI-972. Biochem Biophys Res Commun. 1991 Aug 15;178(3):1351-8.

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