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Purity: ≥98%
BW-A 78U is a novel and potent PDE4 (phosphodiesterase 4) inhibitor with an IC50 of 3 μM. Adenine derivatives substituted in position 9 have been demonstrated to have potent (PDE) inhibition properties with high selectivity toward PDE4. BW-A 78U fails to significantly inhibit arachidonate release. BW-A 78U is ineffective to inhibit the lipopolysaccharide (LPS)-induced TNF-α release.
| ln Vitro |
PDE4 inhibitor BW-A 78U has an IC50 of 3 μM. Arachidonate release is not appreciably inhibited by BW-A 78U. The release of TNF-α produced by lipopolysaccharide (LPS) cannot be inhibited by BW-A 78U[1].
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| References |
[1]. Boichot E, et al. Anti-inflammatory activities of a new series of selective phosphodiesterase 4 inhibitors derivedfrom 9-benzyladenine. J Pharmacol Exp Ther. 2000 Feb;292(2):647-53
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| Molecular Formula |
C₁₃H₁₂FN₅
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| Molecular Weight |
257.27
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| CAS # |
101155-02-6
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| Related CAS # |
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| SMILES |
CNC1=C2N=CN(CC3=CC=CC=C3F)C2=NC=N1
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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: ≥ 2.5 mg/mL (9.72 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 25.0 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: ≥ 2.5 mg/mL (9.72 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 25.0 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: ≥ 2.5 mg/mL (9.72 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 | 3.8870 mL | 19.4348 mL | 38.8697 mL | |
| 5 mM | 0.7774 mL | 3.8870 mL | 7.7739 mL | |
| 10 mM | 0.3887 mL | 1.9435 mL | 3.8870 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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