BAY 73-6691 was characterized in vitro as the first potent and selective inhibitor of phosphodiesterase 9 (PDE9), which is currently under preclinical development for the treatment of Alzheimer′s disease. This compound selectively inhibits human (IC50 = 55 nM) and murine (IC50 = 100 nM) PDE9 activity in vitro and shows only moderate activity against other cyclic nucleotide-specific phosphodiesterases. BAY 73-6691 alone did not significantly increase basal cGMP levels. The PDE9 inhibitor significantly potentiated the cGMP signals generated by sGC activating compounds such as BAY 58-2667 or 5-cyclopropyl-2-[1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-4-ylamine (BAY 41-2272) and induced leftward shifts of the corresponding concentration-response curves. The newly generated PDE9 reporter cell line show that BAY 73-6691 is able to efficiently penetrate cells and to inhibit intracellular PDE9 activity.†
| Molecular Weight | 356.73 |
| Formula | C15H12ClF3N4O |
| CAS Number | 794568-92-6 |
| Solubility (25°C) | DMSO: ≥20 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
| Related PDE Products |
|---|
| ME-3183
ME-3183 is an oral selective PDE4 inhibitor with anti-inflammatory activity for studies related to plaque psoriasis. |
| ART-648
ART-648 is a PDE4 inhibitor that may be used in studies related to non-alcoholic steatohepatitis. |
| (E/Z)-HA155
(E/Z)-HA155 is a potent Autotaxin (ATX) type I inhibitor for studies related to cancer, fibrous disorders, inflammation, pain and angiogenesis. |
| Autotaxin-IN-3
Autotaxin-IN-3 is an Autotaxin(ATX) inhibitor with an IC50 value of 2.4 nM. |
| HA155
HA155 is a potent and selective ATX inhibitor with an IC50 value of 5.7 nM. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.
