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Peldesine

SKU: orb1309274

Description

Peldesine (BCX-34) is a potent, orally bioavailable, and reversible inhibitor of purine nucleoside phosphorylase. It suppresses T-cell proliferation with an IC50 of 800 nM and has been investigated in preclinical research for cutaneous T-cell lymphoma, psoriasis, and HIV infection.

Research Area

Cell Biology, Infectious Disease & Virology, Molecular Biology, Protein Biochemistry

Images & Validation

Key Properties

CAS Number133432-71-0
MW241.25
Purity99.95% (May vary between batches)
FormulaC12H11N5O
SMILESC(C=1C2=C(NC1)C(=O)N=C(N)N2)C=3C=CC=NC3
TargetNucleoside Antimetabolite/Analog,HIV Protease
Solubility10% DMSO+40% PEG300+5% Tween 80+45% Saline:5 mg/mL (20.73 mM);DMSO:195 mg/mL (808.29 mM)

Bioactivity

Target IC50
Proliferation (human T cells):800 nM |RBC PNP (human):36 nM |PNP (rat red blood cells):5 nM |RBC PNP (mouse):32 nM
In Vivo
Peldesine demonstrates oral efficacy by elevating plasma inosine levels in rats (2-fold at 30 mg/kg), significantly reducing ex vivo red blood cell (RBC) purine nucleoside phosphorylase (PNP) activity in rats (98% at 3 hours, 100 mg/kg), and moderately suppressing ex vivo skin PNP activity in mice (39% at 3 hours, 100 mg/kg). Additionally, Peldesine exhibits an oral bioavailability of 76% in rats.
In Vitro
The IC50s are 36 nM, 5 nM, and 32 nM for human, rat, and mouse red blood cell purine nucleoside phosphorylase, respectively. In Jurkat cells, Peldesine (BCX 34; 0-50 µM; 72 hours) inhibits 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.

Storage & Handling

StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

dGuo, Analog, BCX 34, BCX34, BCX-34, inhibit, IL-2, immunosuppressive, Inhibitor, Nucleoside, Nucleoside Antimetabolite, Nucleoside Antimetabolite/Analog, NucleosideAntimetabolite, lymphoma, HIV, HIV Protease, HIVProtease, inosine, Human immunodeficiency virus, phosphorylase, PNP, Peldesine, T-cell, psoriasis, Purine nucleoside phosphorylase

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Key Properties

No computed properties available.

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Peldesine (orb1309274)

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% DMSO +
%+
% Tween 80 +
%

Available Sizes

Select a size below

1 mg
$ 160.00
5 mg
$ 330.00
1 ml x 10 mM (in DMSO)
$ 360.00
10 mg
$ 510.00
25 mg
$ 810.00
50 mg
$ 1,110.00
100 mg
$ 1,490.00
500 mg
$ 2,920.00
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