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250mg |
Purity: ≥98%
Ulodesine (formerly also known as BCX4208) is a novel and potent inhibitor of purine nucleoside phosphorylase (PNP) with the potential to be used for the treatment of psoriasis and gout. It inhibits PNP with an IC50 of 0.5 nM. It is currently being developed by Biocryst as a once-daily oral, chronic treatment for gout. Ulodesine acts at the upstream of xanthine oxidase in the purine metabolism pathway to reduce the production of serum uric acid (sUA) by inhibiting PNP. BCX-4208 is currently in early clinical investigation in psoriasis and gout.
ln Vivo |
PNP is potently inhibited by ulodesine (iv), having an IC50 value of 2.293 nM/L[1]. Ulodesine (iv) removes uric acid buildup in the mouse model's blood[1].
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References |
[1]. Xujuan YANG, et al. Establishment of a novel hyperuricemiaanimal model using mice and assessment ofhyporuricemia action of PNP inhibitor Ulodesine.
[2]. Cesar Diaz-Torné, et al. New medications in development for the treatment of hyperuricemia of gout. Curr Opin Rheumatol. 2015 Mar;27(2):164-9. |
Molecular Formula |
C12H16N4O3
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Molecular Weight |
264.28
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CAS # |
548486-59-5
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SMILES |
O=C1C(NC=C2CN3C[ C@H](O)[C@@H](CO)C3)=C2N=CN1
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Chemical Name |
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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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) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (3.78 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (3.78 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 10.0 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: ≥ 1 mg/mL (3.78 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 | 3.7839 mL | 18.9193 mL | 37.8387 mL | |
5 mM | 0.7568 mL | 3.7839 mL | 7.5677 mL | |
10 mM | 0.3784 mL | 1.8919 mL | 3.7839 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.