| Identification | Back Directory | [Name]
Gisadenafil Besylate | [CAS]
334827-98-4 | [Synonyms]
UK 369003-26
Gisadenafil besylate
Gisadenafil besylate salt
Gisadenafil besylate - UK 369003 | PF 01224715
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-onebenzenesulfonate
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 besylate salt | [Molecular Formula]
C23H33N7O5S.C6H6O3S | [MDL Number]
MFCD18384964 | [MOL File]
334827-98-4.mol | [Molecular Weight]
678 |
| Chemical Properties | Back Directory | [storage temp. ]
Desiccate at RT | [solubility ]
DMSO: >35mg/mL | [form ]
powder | [color ]
white to off-white | [InChIKey]
STFRDYSZKVPPQF-UHFFFAOYSA-N | [SMILES]
OS(=O)(=O)c1ccccc1.CCOc2ncc(cc2C3=NC(=O)c4nn(CCOC)c(CC)c4N3)S(=O)(=O)N5CCN(CC)CC5 |
| Hazard Information | Back Directory | [Uses]
Gisadenafil (UK 369003) is a PDE5 inhibitor. It is 80 fold selective over PDE6, and greater than 3000 fold selective over PDEs 1-4 and 7. Gisadenafil is used for the treatment of LUTS. | [Uses]
Gisadenafil Besylate is a PDE5 inhibitor. It is 80 fold selective over PDE6, and greater than 3000 fold selective over PDEs 1-4 and 7. Gisadenafil is used for the treatment of LUTS.
| [Biological Activity]
Gisadenafil (UK 369003) is a PDE5 inhibitor. It is 80 fold selective over PDE6, and greater than 3000 fold selective over PDEs 1-4 and 7. | [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.
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| [IC 50]
PDE5A: 3.6 nM (IC50); PDE1A: 9.1 μM (IC50) | [storage]
Desiccate at RT |
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| Company Name: |
BOC Sciences
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| Tel: |
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| Website: |
https://www.bocsci.com |
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