Biological Activity
Potent PDE5 inhibitor (IC50 = 1.23 nM). Shows >100-fold selectivity for PDE5 over PDE6. Orally bioavailable.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
M. Wt | 677.79 |
Formula | C23H33N7O5S.C6H6O3S |
Storage | Desiccate at RT |
Purity | ≥99% (HPLC) |
CAS Number | 334827-98-4 |
PubChem ID | 23449797 |
InChI Key | STFRDYSZKVPPQF-UHFFFAOYSA-N |
Smiles | O=S(C1=CN=C(OCC)C(C3=NC(C2=NN(CCOC)C(CC)=C2N3)=O)=C1)(N4CCN(CC)CC4)=O.O=S(C5=CC=CC=C5)(O)=O |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
Solvent | Max Conc. mg/mL | Max Conc. mM | |
---|---|---|---|
Solubility | |||
DMSO | 67.78 | 100 | |
water | 6.78 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 677.79. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
---|---|---|---|
1 mM | 1.48 mL | 7.38 mL | 14.75 mL |
5 mM | 0.3 mL | 1.48 mL | 2.95 mL |
10 mM | 0.15 mL | 0.74 mL | 1.48 mL |
50 mM | 0.03 mL | 0.15 mL | 0.3 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Hashim and Abrams (2010) Emerging drugs for the treatment of benign prostatic obstruction. Exp.Opin.Invest.Drugs 15 159 PMID: 20446824
Rawson et al (2012) The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics. Bioorg.Med.Chem. 20 498 PMID: 22100260
Keywords: Gisadenafil besylate, supplier, pfizer, phosphodiesterases, inhibitors, inhibits, PDE5, UK369003, UK, 369003, Phosphodiesterases, Phosphodiesterases, Tocris Bioscience