Gisadenafil
Gisadenafil (UK-369003) is a specific, orally active phosphodiesterase 5 (PDE5) inhibitor with an IC50 of 3.6 nM and prevents degradation of cyclic guanosine monophosphate (cGMP).
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- CAS No.: 334826-98-1
- 화학식: C23H33N7O5S
- 분자량:519.62
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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PDE5A 3.6 nM (IC50) |
PDE1A 9.1 μM (IC50) |
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male Tat-transgenic (Tat-tg) mice (8 weeks old) exposed to hypercapnia[1]
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Dosage:2 mg/kg
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Administration:Intraperitoneal injection; for 2 hours
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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.
Chemical Information
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CAS No. 334826-98-1
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분자량 519.62
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화학식 C23H33N7O5S
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SMILES
O=C1C2=NN(CCOC)C(CC)=C2N=C(C3=CC(S(=O)(N4CCN(CC)CC4)=O)=CN=C3OCC)N1
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Synonyms
UK-369003
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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. [Content Brief]
[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. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Gisadenafil Related Classifications
HY-14841 Related Classifications
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