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Gisadenafil besylate

Catalog No. T11400 CAS 334827-98-4

Synonyms: UK 369003-26

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

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Gisadenafil besylate, CAS 334827-98-4

Pack Size	Availability	Price/USD
25 mg	8-10 weeks	$ 683.00
50 mg	8-10 weeks	$ 888.00
100 mg	8-10 weeks	$ 1,340.00

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This compound is a customized synthesis product. We have a strong synthesis team with excellent synthesis technology and capabilities. However, due to various objective factors, there is a low probability that the synthesis will not be successful. If you need to learn more, please feel free to consult us, we will serve you wholeheartedly.

Biological Description

Chemical Properties

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Description	Gisadenafil besylate (UK 369003-26) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor ,prevents degradation of cyclic guanosine monophosphate (cGMP), with an IC50 of 3.6 nM .
Targets&IC50	PDE1A:9.1 μM, PDE5A:3.6 nM
In vitro	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.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.
In vivo	Gisadenafil also restores the dilation of small (<25 μm) arterioles following hypercapnia, although it fails to restore full dilation of larger (>25 μm) vessels.

Synonyms	UK 369003-26
Molecular Weight	677.79
Formula	C29H39N7O8S2
CAS No.	334827-98-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

References and Literature

1. Silva J, et al. 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. 2012 Nov 20;9:253. 2. Rawson DJ, 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 Jan 1;20(1):498-509.

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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Gisadenafil besylate 334827-98-4 Others UK 369003-26 inhibitor inhibit

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