1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Gisadenafil besylate

Gisadenafil besylate (Synonyms: UK 369003-26)

Cat. No.: HY-108619
Handling Instructions

Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).

For research use only. We do not sell to patients.

Gisadenafil besylate Chemical Structure

Gisadenafil besylate Chemical Structure

CAS No. : 334827-98-4

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Description

Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP)[1].

IC50 & Target[1]

PDE5A

3.6 nM (IC50)

PDE1A

9.1 μM (IC50)

In Vitro

Since some PDE5 inhibitors can also interact with PDE1 isotypes found within the cerebral vasculature, the specificity of Gisadenafil for PDE5 is confirmed. This is directly tested with recombinant PDE5A and PDE1A overexpressed in COS-7 cells. The IC50 of Gisadenafil for PDE5A is 3.6 nM. In contrast, the IC50 of Gisadenafil for PDE1A is 9.1 μM, an approximately 2500-fold difference in specificity[1].

In Vivo

Gisadenafil (2 mg/kg; intraperitoneal injection; for 2 hours; male Tat-transgenic mice) treatment largely restores the normal increase in cortical flow following hypercapnia in Tat-tg mice (17.5% above baseline). Gisadenafil also restores the dilation of small (<25 μm) arterioles following hypercapnia, although it fails to restore full dilation of larger (>25 μm) vessels[1].

Animal Model: Male Tat-transgenic (Tat-tg) mice (8 weeks old) exposed to hypercapnia[1]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection; for 2 hours
Result: Largely restored the normal increase in cortical flow following hypercapnia in Tat-tg mice (17.5% above baseline). Also restored the dilation of small (<25 μm) arterioles following hypercapnia.
Molecular Weight

676.78

Formula

C₂₉H₃₈N₇O₈S₂-

CAS No.

334827-98-4

SMILES

O=C1C2=NN(CCOC)C(CC)=C2N=C(C3=CC(S(=O)(N4CCN(CC)CC4)=O)=CN=C3OCC)N1.O=S(C5=CC=CC=C5)([O-])=O

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Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

Gisadenafil besylateUK 369003-26Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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