| Identification | Back Directory | [Name]
PF-3774076 >=98% (HPLC) | [CAS]
1171824-96-6 | [Synonyms]
PF-3774076
PF-3774076 >=98% (HPLC)
1H-Imidazole, 2-[(1R)-5-chloro-2,3-dihydro-4-(methoxymethyl)-1H-inden-1-yl]- | [Molecular Formula]
C14H15ClN2O | [MOL File]
1171824-96-6.mol | [Molecular Weight]
262.73 |
| Chemical Properties | Back Directory | [Boiling point ]
457.1±45.0 °C(Predicted) | [density ]
1.279±0.06 g/cm3(Predicted) | [storage temp. ]
room temp | [solubility ]
DMSO: 10mg/mL, clear | [form ]
powder | [pka]
13.69±0.10(Predicted) | [color ]
white to beige |
| Hazard Information | Back Directory | [Uses]
PF-3774076 is a highly central nervous system (CNS) penetrant, potent, and selective human α1A-adrenoceptor partial agonist. It exhibits good potency and selectivity in multiple binding and functional assays. PF-3774076 increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner via a central mechanism. PF-3774076 affects both the proximal and distal portions of the urethra in vivo. These properties suggest that PF-3774076 may have significant benefit in the treatment of stress urinary incontinence (SUI) as a CNS-penetrant α1A receptor partial agonist. However, despite its partial agonism and selectivity for α1A receptors, PF-3774076 failed to provide adequate safety differences in in vivo models of cardiovascular function. This may be due to the simultaneous activation of both peripheral and central α1A receptors. These data suggest that while central α1A partial agonists may have significant benefit in the treatment of SUI, this class of agents may have difficulty achieving the desired urethral selectivity without affecting cardiovascular function. | [Biological Activity]
PF-3774076 is a CNS penetrantpotentselectivepartial agonist at the human α1A adrenoceptor. PF-3774076 is selective over α1B and α1D adrenoceptors. |
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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|