1. Cell Cycle/DNA Damage
    Anti-infection
  2. Nucleoside Antimetabolite/Analog
    HIV
  3. Peldesine

Peldesine (Synonyms: BCX 34)

Cat. No.: HY-106934
Handling Instructions

Peldesine (BCX 34) 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 is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection treatment.

For research use only. We do not sell to patients.

Peldesine Chemical Structure

Peldesine Chemical Structure

CAS No. : 133432-71-0

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Description

Peldesine (BCX 34) 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 is also a T-cell proliferation inhibitor with an IC50 of 800 nM. Peldesine has the potential for cutaneous T-cell lymphoma, psoriasis and HIV infection treatment[1][2][3][4].

IC50 & Target

IC50: 36 nM (Human RBC PNP), 5 nM (Rat RBC PNP), 32 nM (Mouse RBC PNP), and 800 nM (Human T-cell proliferation)[3]
Ki: 23 nM (Human RBC PNP)[3]
HIV[4]

In Vitro

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].

Cell Proliferation Assay[1]

Cell Line: Jurkat cells
Concentration: 0 µM, 10 µM, 20 µM, 30 µM, 40 µM, 50 µM
Incubation Time: 72 hours
Result: In the presence of 10 µM dCuo, had a complete inhibitory effect for T-cell lines.
In Vivo

Oral bioavailability of Peldesine in rats is 76%. Peldesine is orally active in elevating plasma inosine in rats (2-fold at 30 mg/kg), in suppressing ex vivo RBC PNP activity in rats (98% at 3 h. 100 mg/kg), and in suppressing ex vivo skin PNP in mice (39% at 3 h, 100 mg/kg)[3].

Molecular Weight

241.25

Formula

C₁₂H₁₁N₅O

CAS No.

133432-71-0

SMILES

O=C1C(NC=C2CC3=CC=CN=C3)=C2N=C(N)N1

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

PeldesineBCX 34BCX34BCX-34Nucleoside Antimetabolite/AnalogHIVHuman immunodeficiency virusNucleosidephosphorylaseT-cellPNPimmunosuppressivedGuoIL-2inosinepsoriasislymphomaInhibitorinhibitorinhibit

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