Fig. 1 · Structure
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PF-3774076
PF-3774076 is a selective partial agonist for the human α1A-adrenoceptor, exhibiting potent activity as a central nervous system (CNS) penetrant. It effectively increases peak urethral pressure in anesthetized female dogs in a dose-dependent manner, influencing both the proximal and distal portions of the urethra. These properties indicate potential applications in treating stress urinary incontinence (SUI). However, PF-3774076's simultaneous activation of central and peripheral α1A receptors raises concerns about cardiovascular safety, complicating its therapeutic potential in achieving urethral selectivity while minimizing cardiovascular effects.
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Specifications
| Manufacturer | Adooq Bioscience |
|---|---|
| Actions | Partial Agonist |
| CAS Number | 1171824-96-6 |
| Formula | C14H15ClN2O |
| Molecular Weight | 262.73 |
| SMILES | COCC1=C(Cl)C=CC2=C1CC[C@H]2C3=NC=CN3 |
Storage & Solubility
In Vitro Solubility
Reported Solubility
No reported solubility data are available for this product.
Preparing Stock Solutions
| Concentration | |
|---|---|
Values use four significant digits. Prepare to the final solution volume; this is not the volume of solvent to add.
Stock preparation is unavailable for this product molecular weight.
Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.
Storage
Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.