Gisadenafil besylate

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Cat.No. 4165 - Gisadenafil besylate | C23H33N7O5S.C6H6O3S | CAS No. 334827-98-4
Description: Potent PDE5 inhibitor; orally bioavailable
Alternative Names: UK 369003
Chemical Name: 5-[2-Ethoxy-5-[(4-ethyl-1-piperazinyl)sulfonyl]-3-pyridinyl]-3-ethyl-2,6-dihydro-2-(2-methoxyethyl)-7H-pyrazolo[4,3-d]pyrimidin-7-one benzenesulfonate
Purity: ≥99% (HPLC)
Datasheet
Citations (1)
Reviews
Literature (2)

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.

Compound Libraries

Gisadenafil besylate is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
water 6.78 10
DMSO 67.78 100

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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
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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References

References are publications that support the biological activity of the product.

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


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Keywords: Gisadenafil besylate, Gisadenafil besylate supplier, pfizer, phosphodiesterases, inhibitors, inhibits, PDE5, UK369003, UK, 369003, Phosphodiesterases, 4165, Tocris Bioscience

1 Citation for Gisadenafil besylate

Citations are publications that use Tocris products. Selected citations for Gisadenafil besylate include:

Silva et al (2012) Transient hypercapnia reveals an underlying cerebrovascular pathology in a murine model for HIV-1 associated neuroinflammation: role of NO-cGMP signaling and normalization by inhibition of cyclic nucleotide phosphodiesterase-5. J Neuroinflammation 9 253 PMID: 23167821


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Literature in this Area

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