Peldesine dihydrochloride

• CAT Number: I045665
• CAS Number: 2772702-10-8
• Molecular Formula: C12H13Cl2N5O
• Molecular Weight: 314.17
• Purity: ≥95%
• Synonyms: 2-amino-7-(pyridin-3-ylmethyl)-3,5-dihydropyrrolo[3,2-d]pyrimidin-4-one;dihydrochloride
• InChI: InChI=1S/C12H11N5O.2ClH/c13-12-16-9-8(4-7-2-1-3-14-5-7)6-15-10(9)11(18)17-12;;/h1-3,5-6,15H,4H2,(H3,13,16,17,18);2*1H
• InChIKey: HQJPQOLISXXDRJ-UHFFFAOYSA-N
• SMILES: C1=CC(=CN=C1)CC2=CNC3=C2N=C(NC3=O)N.Cl.Cl

Peldesine (BCX 34) dihydrochloride is a potent, competitive, reversible and orally active purine nucleoside phosphorylase (PNP) inhibitor with IC50s of 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell (RBC) PNP, respectively. Peldesine dihydrochloride is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine dihydrochloride has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection research[1][2][3][4].
Peldesine (BCX 34; 0-50 µM; 72 hours; Jurkat cells) could inhibit the T-cell proliferation completely at a concentration of less than 10 μM, in the presence of dGuo (10 μM). In contrast, the B-cell proliferation is not affected by Peldesine[1].
Peldesine (BCX 34) suppresses T-cell immune reaction in an IL-2-independent manner, and this means that Peldesine might affect a late phase rather than an early stage in T-cell activation[1].
Peldesine also, in the presence but not in the absence of deoxyguanosine, inhibits human leukemia CCRF-CEM T-cell proliferation with an IC50 of 0.57 μM but not rat or mouse T-cell proliferation up to 30 μM[3].

Reference

[1]. Wada Y, et al. BCX-34: a novel T-cell selective immunosuppressant: purine nucleoside phosphorylase (PNP) inhibitor. Artif Organs. 1996 Aug;20(8):849-52.
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[2]. Duvic M, et al. A phase III, randomized, double-blind, placebo-controlled study of peldesine (BCX-34) cream as topical therapy for cutaneous T-cell lymphoma. J Am Acad Dermatol. 2001 Jun;44(6):940-7.
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[3]. Bantia S, et al. In vivo and in vitro pharmacologic activity of the purine nucleoside phosphorylase inhibitor BCX-34: the role of GTP and dGTP. Immunopharmacology. 1996 Oct;35(1):53-63.
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[4]. New AIDS study suppresses T cells to stop viral growth. AIDS Alert. 1997 Jul;12(7):77-8.
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