Gisadenafil besylate

Name: Gisadenafil besylate
Brand: Tocris Bioscience
SKU: 4165

Tocris Bioscience a Bio-Techne Brand

Catalog # 4165

Citations (1)

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Key Product Details

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)
Molecular Weight:	677.79

View Full Technical Details for Gisadenafil besylate

Biological Activity for Gisadenafil besylate

Gisadenafil besylate is a 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 for Gisadenafil besylate

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

Technical Data for Gisadenafil besylate

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 for Gisadenafil besylate

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

Preparing Stock Solutions for Gisadenafil besylate

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.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.48 mL	7.38 mL	14.75 mL
5 mM	0.30 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	0.30 mL

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References for Gisadenafil besylate

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

Rawson The discovery of UK-369003, a novel PDE5 inhibitor with the potential for oral bioavailability and dose-proportional pharmacokinetics. Bioorg.Med.Chem. 2012 PMID: 22100260
Hashim and Abrams Emerging drugs for the treatment of benign prostatic obstruction. Exp.Opin.Invest.Drugs 2010 PMID: 20446824

Citations for Gisadenafil besylate (1)

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Citations are publications that use Bio-Techne 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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