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BAY 73-6691

  Cat. No.:  DC11661  
Chemical Structure
794568-92-6
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More than 5000 active chemicals with high quality for research!
Field of application
BAY 73-6691 is a drug developed by Bayer for the treatment of Alzheimer's disease. It was the first compound developed that acts as a phosphodiesterase inhibitor selective for the PDE9A subtype.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 794568-92-6
Chemical Name: 4H-Pyrazolo[3,4-d]pyrimidin-4-one,1-(2-chlorophenyl)-1,5-dihydro-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-
Synonyms: LogP;1-(2-chlorophenyl)-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-2H-pyrazolo[3,4-d]pyrimidin-4-one;4H-Pyrazolo[3,4-d]pyrimidin-4-one,1-(2-chlorophenyl)-1,5-dihydro-6-[(2R)-3,3,3-trifluoro-2-met...;BAY 73-6691;4H-Pyrazolo[3,4-d]pyrimidin-4-one,1-(2-chlorophenyl)-1,5-dihydro-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-
SMILES: FC([C@@H](CC1=NC(=O)C2C(N(C3=CC=CC=C3Cl)NC=2)=N1)C)(F)F
Formula: C15H12ClF3N4O
M.Wt: 356.730192184448
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description: BAY 73-6691 is a potent, selective brain penetrant PDE9A inhibitor.
Target: PDE9A[1]
In Vivo: 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].
In Vitro: 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].
Cell Assay: 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 Administration: 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.
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
2018-0101
2018-0101
Cat. No. Product name Field of application
DC73764 CRD733 CRD733 (ASP4901) is a potent, selective cGMP-specific PDE9 (phosphodiesterase 9) inhibitor.
DC71683 Lodenafil Lodenafil (Hydroxyhomosildenafil) is a potent phosphodiesterase type 5 (PDE5) inhibitor for the treatment of erectile dysfunction (ED).
DC70239 BAY 2666605 BAY2666605 is a potent, small molecule PDE3A-SLFN12 complex inducer with EC50 of 7 nM.BAY2666605 triggers the formation of a complex of two proteins called SLFN12 and PDE3A. This complex drive cancer cells into cell death by a mechanism called apoptosis.
DC48226 ONO-8430506 ONO-8430506 is an orally bioavailable and potent autotaxin (ATX)/ENPP2 inhibitor with the IC90 of 100 nM for ATX activity in mouse plasma.
DC47989 FPFT-2216 FPFT-2216, a “molecular glue” compound, degrades phosphodiesterase 6D (PDE6D), zinc finger transcription factors Ikaros (IKZF1), Aiolos (IKZF3), and casein kinase 1α (CK1α). FPFT-2216 can be used for the research of cancer and inflammatory disease.
DC42521 MBCQ MBCQ is a potent and selective the type V phosphodiesterase (PDE V; PDE5) inhibitor with an IC50 of 19 nM. MBCQ has IC50s >100 µM for PDE1, PDE2, PDE3, and PDE4, respectively. MBCQ dilates coronary arteries via potent and specific inhibition of cGMP-PDE.
DC40977 DSR-141562 DSR-141562 is a novel, orally active, and selective brain-penetrant phosphodiesterase 1 (PDE1) inhibitor. DSR-141562 shows preferential selectivity for human PDE1B with an IC50 of 43.9 nM, and the IC50 values for human PDE1A and 1C are 97.6 and 431.8 nM, respectively. DSR-141562 can be used for the study of positive symptoms, negative symptoms and cognitive impairments associated with schizophrenia.
DC40378 MR-L2 MR-L2 is a reversible and noncompetitive allosteric activator of long-isoform phosphodiesterase-4 (PDE4), activates representative PDE4 long-isoform variants (PDE4A4, PDE4B1, PDE4C3, PDE4D5). MR-L2 suppresses PGE2-induced MDCK cell cyst formation with an EC50 of 1.2 μM.
DC28378 THPP-1 THPP-1, a SGC chemical probe, is a potent and orally bioavailable phosphodiesterase 10A (PDE10A) inhibitor, with Ki values of 1 nM and 1.3 nM for human and rat PDE10A, respectively. THPP-1 has excellent pharmacokinetic properties in preclinical species.
DC28354 (E/Z)HA-155 (E/Z)HA-155 is a potent and selective autotaxin (ATX) inhibitor with an IC50 of 5.7 nM.
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