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Peldesine

Catalog No. T12399   CAS 133432-71-0
Synonyms: BCX 34

Peldesine (BCX 34) is an effective, competitive, reversible, and orally active inhibitor of purine nucleoside phosphorylase. Peldesine inhibits T-cell proliferation with an IC50 of 800 nM. Peldesine can be used in research on cutaneous T-cell lymphoma, psoriasis and HIV infection.

All products from TargetMol are for Research Use Only. Not for Human or Veterinary or Therapeutic Use.
Peldesine Chemical Structure
Peldesine, CAS 133432-71-0
Pack Size Availability Price/USD Quantity
1 mg In stock $ 116.00
5 mg In stock $ 289.00
10 mg In stock $ 463.00
25 mg In stock $ 766.00
50 mg In stock $ 1,070.00
100 mg In stock $ 1,450.00
500 mg In stock $ 2,880.00
1 mL * 10 mM (in DMSO) In stock $ 318.00
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Purity: 99.95%
Purity: 99.27%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Peldesine (BCX 34) is an effective, competitive, reversible, and orally active inhibitor of purine nucleoside phosphorylase. Peldesine inhibits T-cell proliferation with an IC50 of 800 nM. Peldesine can be used in research on cutaneous T-cell lymphoma, psoriasis and HIV infection.
Targets&IC50 RBC PNP (human):36 nM , Proliferation (human T cells):800 nM , PNP (rat red blood cells):5 nM , RBC PNP (mouse):32 nM
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[1].
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[2].
Synonyms BCX 34
Molecular Weight 241.25
Formula C12H11N5O
CAS No. 133432-71-0

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 195 mg/mL (808.29 mM), Sonication is recommended.

TargetMolReferences and Literature

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. 2. 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. 3. New AIDS study suppresses T cells to stop viral growth. AIDS Alert. 1997 Jul;12(7):77-8. 4. 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.

Related compound libraries

This product is contained In the following compound libraries:
Inhibitor Library Drug Repurposing Compound Library Bioactive Compounds Library Max Orally Active Compound Library Human Metabolite Library Anti-Viral Compound Library Bioactive Compound Library Clinical Compound Library ReFRAME Related Library

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Keywords

Peldesine 133432-71-0 Cell Cycle/Checkpoint DNA Damage/DNA Repair Microbiology/Virology Proteases/Proteasome HIV Protease Nucleoside Antimetabolite/Analog Inhibitor inhibit PNP inosine dGuo HIV Nucleoside psoriasis phosphorylase Human immunodeficiency virus lymphoma IL-2 T-cell BCX 34 BCX-34 immunosuppressive BCX34 inhibitor

 

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