BAY 73-6691 ((R)-BAY 73-6691) (Synonyms: (R)-BAY 73-6691) |
| رقم الكتالوجGC30923 |
BAY 73-6691 ((R) -BAY 73-6691) ((R) -BAY 73-6691 ((R) -BAY 73-6691)) هو مثبط قوي ، مخترق للدماغ ، وانتقائي PDE9A.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 794568-92-6
Sample solution is provided at 25 µL, 10mM.
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BAY 73-6691 is a potent, selective brain penetrant PDE9A inhibitor.
The BAY 73-6691 dose-dependently alleviates cell viability loss due to Aβ25-35 treatment. It is found that when SH-SY5Y cells are cultured by Aβ25-35, a high degree of cell apoptosis is observed, while additional stimulation with BAY 73-6691 causes attenuation of cell apoptosis. BAY 73-6691 dose-dependently attenuates oxidative stress induced by Aβ25-35, and BAY 73-6691 at 200 μg/mL almost neutralizes Aβ25-35-induced oxidative damage. The BAY 73-6691 attenuates Aβ25-35-induced increase of apoptosis cells[1].
BAY 73-6691 dose-dependently improves the acquisition performance in the Aβ25-35-injected mice on days 7 to 10 (day 7, F(5,54)=65.153; day 8, F(5,54)=62.340; day 9, F(5,54)=37.529; day 10, F(5,54)=38.624; P<0.001). BAY 73-6691 at 3 mg/kg can almost completely abolish the prolongation of escape-latency on days 9 to 10. BAY 73-6691 dose-dependently elevates the Aβ25-35-induced decrease of the dwell time on the 10th day post Aβ25-35 injection (day 10, F(5,54)=27.360, P<0.001). Results reveal that the Aβ25-35 injection and BAY 73-6691 treatment cause no influence on the swimming speed. Treatment with BAY 73-6691 does not cause detectable alteration of spatial memory in sham mice. BAY 73-6691 alleviates Aβ25-35-induced abnormalities of the above indices. The BAY 73-6691 causes no influence on the four indices mentioned above in sham mice. The BAY 73-6691 has no significant effect on the apoptosis of hippocampal neurons in sham mice[1].
[1]. Li J, et al. Protective effects of BAY 73-6691, a selective inhibitor of phosphodiesterase 9, on amyloid-β peptides-induced oxidative stress in in-vivo and in-vitro models of Alzheimer's disease. Brain Res. 2016 Jul 1;1642:327-335.
Cell experiment: | The SH-SY5Y human neuroblastoma cell line is used in this study. The cells are routinely cultured in a mixture of Dulbecco's modified Eagle's medium (DMEM)/Ham's F12 containing 10% fetal bovine serum, 2 mM L-glutamine, antibiotic and antimycotic solution under a humidified atmosphere of 5% CO2-95% air at 37°C. The SH-SY5Y are plated in 96-well plates at 1×105 cells per well for the treatment with Aβ25-35 and the BAY 73-6691. Before experiments, freshly prepared Aβ25-35 peptide at 20 μM is added to the cells with or without exposure to different concentrations (50, 100, 150 and 200 μg/mL) of BAY 73-6691[1]. |
Animal experiment: | Male ICR mice (weighing 25 to 30 g) are used to induce the animal model of Alzheimer's disease (AD). All mice are housed in a temperature- and humidity-controlled room with a constant light-dark cycle (12 h/12 h) and are maintained on ad libitum food and water. BAY 73-6691 at different doses (0.3, 1 and 3 mg/kg) is consecutively injected (i.p.) once daily at 7:30 A.M on days 1 to 10 after injection of Aβ25-35 (day 0). Mice are divided into six groups: (I) sham, (II) Aβ, (III) Aβ+0.3 mg/kg BAY 73-6691, (IV) Aβ+1 mg/kg BAY 73-6691, (V) Aβ+3 mg/kg BAY 73-6691 and (VI) 3 mg/kg BAY 73-6691[1]. |
References: [1]. Li J, et al. Protective effects of BAY 73-6691, a selective inhibitor of phosphodiesterase 9, on amyloid-β peptides-induced oxidative stress in in-vivo and in-vitro models of Alzheimer's disease. Brain Res. 2016 Jul 1;1642:327-335. | |
| Cas No. | 794568-92-6 | SDF | |
| المرادفات | (R)-BAY 73-6691 | ||
| Canonical SMILES | O=C1C2=C(N(C3=CC=CC=C3Cl)N=C2)NC(C[C@@H](C)C(F)(F)F)=N1 | ||
| Formula | C15H12ClF3N4O | M.Wt | 356.73 |
| الذوبان | DMSO : 160 mg/mL (448.52 mM) | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8032 mL | 14.0162 mL | 28.0324 mL |
| 5 mM | 0.5606 mL | 2.8032 mL | 5.6065 mL |
| 10 mM | 0.2803 mL | 1.4016 mL | 2.8032 mL |
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Quality Control & SDS
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- Purity: >99.50%
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Average Rating: 5 (Based on Reviews and 5 reference(s) in Google Scholar.)
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