CI 972
CI 972 Basic information
- Product Name:
- CI 972
- Synonyms:
-
- CI 972
- CI 972 (anhydrous)
- 2,6-Diamino-3,5-dihydro-7-(3-thienylmethyl)-4H-pyrrolo(3,2-D)pyrimidin-4-one
- CAS:
- 115787-68-3
- MF:
- C11H12ClN5OS
- MW:
- 297.76
- Mol File:
- 115787-68-3.mol
CI 972 Chemical Properties
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
CI 972 Usage And Synthesis
Uses
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].
in vivo
CI 972 anhydrous (5-150 mg/kg; p.o.) produces dose-dependent elevation of plasma inosine one hour after administration to rats[1].
References
[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. DOI:10.1007/978-1-4899-2638-8_8
[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. DOI:10.1016/0006-291x(91)91042-b
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