Gisadenafil Besylate
Gisadenafil Besylate Basic information
- Product Name:
- Gisadenafil Besylate
- Synonyms:
-
- 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
- Gisadenafil besylate
- 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
- Gisadenafil besylate salt
- UK 369003-26
- CAS:
- 334827-98-4
- MF:
- C29H39N7O8S2
- MW:
- 677.79
- Product Categories:
-
- Amines, Heterocycles, Pfizer compounds, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds
- Mol File:
- 334827-98-4.mol
Gisadenafil Besylate Chemical Properties
- storage temp.
- Desiccate at RT
- solubility
- DMSO: >35mg/mL
- form
- powder
- color
- white to off-white
Gisadenafil Besylate Usage And Synthesis
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.
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.
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. |
IC 50
PDE5A: 3.6 nM (IC50); PDE1A: 9.1 μM (IC50)
storage
Desiccate at RT
Gisadenafil BesylateSupplier
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