| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
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| ln Vitro |
Peldesine (BCX 34; 0-50 μM; 72 hours; Jurkat cells) totally suppresses T cell proliferation in the presence of dGuo (10 μM) at doses below 10 μM. Peldesine, on the other hand, has no effect on B cell proliferation [1]. Peldesine (BCX 34) may influence late rather than early phases of T cell activation since it decreases T cell immunological responses in an IL-2-independent way [1]. With an IC50 of 0.57 μM, pendelasine also reduced the proliferation of human leukemia CCRF-CEM T cells, but not that of rat or mouse T cells, when deoxyguanosine was present. As much as 30 μM[3].
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| ln Vivo |
Rats have a 76% oral bioavailability of Peldesine. Peldesine can be taken orally and have the following effects: it can decrease rat RBC PNP activity in vitro (98% at 100 mg/kg in 3 hours), increase rat plasma inosine (2-fold at 30 mg/kg), and prevent mice from expressing isolated skin PNP. Medium (39% at 3 hours, 100 mg/kg) [3].
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| Cell Assay |
Cell Proliferation Assay[1]
Cell Types: Jurkat Cell Tested Concentrations: 0 µM, 10 µM, 20 µM, 30 µM, 40 µM, 50 µM Incubation Duration: 72 hrs (hours) Experimental Results: Complete inhibition in the presence of 10 µM dCuo for T Cell lines. |
| References | |
| Additional Infomation |
Peldesine is a potent inhibitor of human CCRF-CEM T-cell proliferation. It has undergone phase I trials for the treatment of Human Immunodeficiency Virus (HIV) infections.
Peldesine is a pyrimidine analogue and purine nucleoside phosphorylase inhibitor with immunosuppressive and antineoplastic properties. Peldesine inhibits purine nucleoside phosphorylase (PNP) that plays a pivotal role in T-cell proliferation and is responsible for the catalysis of the reversible phosphorolytic cleavage of purine ribonucleosides and 2'-deoxyribonucleosides. Inhibition of PNP results in accumulation of dGTP and the subsequent failure of DNA synthesis. This agent maybe used in T-cell related autoimmune diseases including psoriasis, rheumatoid arthritis and Crohn s disease and T-cell cancers |
| Molecular Formula |
C12H11N5O
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|---|---|
| Molecular Weight |
241.24864
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| Exact Mass |
241.096
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| CAS # |
133432-71-0
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| Related CAS # |
Peldesine dihydrochloride;2772702-10-8
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| PubChem CID |
135413525
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.57g/cm3
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| Boiling Point |
534ºC at 760mmHg
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| Flash Point |
276.7ºC
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| Vapour Pressure |
1.76E-11mmHg at 25°C
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| Index of Refraction |
1.794
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| LogP |
1.161
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
18
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| Complexity |
370
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
DOHVAKFYAHLCJP-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C12H11N5O/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)
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| Chemical Name |
2-amino-7-(pyridin-3-ylmethyl)-3,5-dihydropyrrolo[3,2-d]pyrimidin-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~829.02 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 5 mg/mL (20.73 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 5 mg/mL (20.73 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 50.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 5 mg/mL (20.73 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 4.1451 mL | 20.7254 mL | 41.4508 mL | |
| 5 mM | 0.8290 mL | 4.1451 mL | 8.2902 mL | |
| 10 mM | 0.4145 mL | 2.0725 mL | 4.1451 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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