Bulk Inquiry
Gisadenafil besylate
- UK 369003 - PF 01224715
- Parent CAS: 334826-98-1
- Soluble in water and DMSO
- MF: C22H31N7O5S.C7H8O3S
- MW: 677.79
Description
Gisadenafil besylate is a potent and selective cGMP-specific phosphodiesterase 5 (PDE5) inhibitor with reported IC50 of 1.23 nM. It shows improved selectivity over PDE6, with reported PDE5/PDE6 selectivity of 117 and more than 3000-fold selectivity over other PDEs.
PDE5 controls cGMP breakdown in smooth muscle, vascular and urogenital tissues. Gisadenafil is relevant for studying PDE5-mediated cGMP pharmacology, erectile dysfunction mechanisms and lower urinary tract/BPH-related smooth-muscle signaling.
Key Features
- Potent PDE5 inhibitor
- High selectivity over PDE6 and other PDEs
- Modulates cGMP signaling pathways
- Sildenafil-related pharmacological comparator
Applications
- PDE5 enzyme assays
- cGMP signaling studies
- Erectile dysfunction model research
- BPH and smooth-muscle pharmacology
Note: Gisadenafil is a close analogue of Sildenafil (Axon 2046).
More Information
| Parent CAS No. | 334826-98-1 |
|---|---|
| Chemical Name | 5-(2-ethoxy-5-(4-ethylpiperazin-1-ylsulfonyl)pyridin-3-yl)-3-ethyl-2-(2-methoxyethyl)-2H-pyrazolo[4,3-d]pyrimidin-7(6H)-one benzenesulfonate |
| extra_info | . |
| SMILES | C1(C2=CC(S(N3CCN(CC)CC3)(=O)=O)=CN=C2OCC)NC(=O)C2=NN(CCOC)C(CC)=C2N=1.C1(S(O)(=O)=O)C=CC=CC=1 |
| MFCD | MFCD16619298 |
| InChi | InChI=1S/C23H33N7O5S.C6H6O3S/c1-5-18-19-20(27-30(18)12-13-34-4)22(31)26-21(25-19)17-14-16(15-24-23(17)35-7-3)36(32,33)29-10-8-28(6-2)9-11-29;7-10(8,9)6-4-2-1-3-5-6/h14-15H,5-13H2,1-4H3,(H,25,26,31);1-5H,(H,7,8,9) |
| InChiKey | STFRDYSZKVPPQF-UHFFFAOYSA-N |
| CID | 135564628 |
| Short Description | PDE5 inhibitor |
References
- D.J. Rawson et al. The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics. Bioorg. Med. Chem. 2012, 20, 498-509.
- N.A.M. Tamimi et al. A placebo-controlled study investigating the efficacy and safety of the phosphodiesterase type 5 inhibitor UK-369,003 for the treatment of men with lower urinary tract symptoms associated (...). BJU Int. 2010, 106, 674–680.
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