BAY 73-6691 - CAS 794568-92-6
Catalog number:
794568-92-6
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C15H12ClF3N4O
Molecular Weight:
356.73
COA:
Inquire
Targets:
Phosphodiesterase (PDE)
Description:
BAY 73-6691 is a phosphodiesterase inhibitor selective for the PDE9A subtype under the development of Bayer. It selectively inhibits human PDE9 with IC50 value of 55 nM in vitro.BAY 73-6691 was developed for the treatment of Alzheimer's disease, but pre-clinical research is at an early stage.
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Purity:
98%
Appearance:
Off-white powder
Synonyms:
UNII-80ZTV3INTW; (R)-Bay-73-6691; 1-(2-Chlorophenyl)-6-[(2R)-3,3,3-trifluoro-2-methylpropyl]-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidine-4-one
Solubility:
DMSO: >20 mg/mL
Storage:
-20℃ Freezer
MSDS:
Inquire
Application:
Alzheimer's disease.
Quality Standard:
In-house standard
Shelf Life:
2 month in rt, long time
Quantity:
Milligrams-Grams
InChIKey:
FFPXPXOAFQCNBS-MRVPVSSYSA-N
InChI:
1S/C15H12ClF3N4O/c1-8(15(17,18)19)6-12-21-13-9(14(24)22-12)7-20-23(13)11-5-3-2-4-10(11)16/h2-5,7-8H,6H2,1H3,(H,21,22,24)/t8-/m1/s1
Canonical SMILES:
C[C@H](Cc1[nH]c(=O)c2cnn(c2n1)c3ccccc3Cl)C(F)(F)F
Current Developer:
Originator Bayer
1.Phosphodiesterase-9 (PDE9) inhibition with BAY 73-6691 increases corpus cavernosum relaxations mediated by nitric oxide-cyclic GMP pathway in mice.
da Silva FH1, Pereira MN, Franco-Penteado CF, De Nucci G, Antunes E, Claudino MA. Int J Impot Res. 2013 Mar-Apr;25(2):69-73. doi: 10.1038/ijir.2012.35. Epub 2012 Oct 4.
Phosphodiesterase-9 (PDE9) specifically hydrolyzes cyclic GMP, and was detected in human corpus cavernosum. However, no previous studies explored the selective PDE9 inhibition with BAY 73-6691 in corpus cavernosum relaxations. Therefore, this study aimed to characterize the PDE9 mRNA expression in mice corpus cavernosum, and investigate the effects of BAY 73-6691 in endothelium-dependent and -independent relaxations, along with the nitrergic corpus cavernosum relaxations. Male mice received daily gavage of BAY 73-6691 (or dimethylsulfoxide) at 3 mg kg(-1) per day for 21 days. Relaxant responses to acetylcholine (ACh), nitric oxide (NO) (as acidified sodium nitrite; NaNO2 solution), sildenafil and electrical-field stimulation (EFS) were obtained in corpus cavernosum in control and BAY 73-6691-treated mice. BAY 73-6691 was also added in vitro 30 min before construction of concentration-responses and frequency curves. PDE9A and PDE5 mRNA expression was detected in the mice corpus cavernosum in a similar manner.
2.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.
Li J1, Liu CN2, Wei N3, Li XD4, Liu YY4, Yang R4, Jia YJ4. Brain Res. 2016 Apr 9. pii: S0006-8993(16)30204-9. doi: 10.1016/j.brainres.2016.04.011. [Epub ahead of print]
Alzheimer's disease (AD) is accompanied by enhanced oxidative stress and excess free radicals. Phosphodiesterase 9 inhibitors (PDE-9Is) showed memory improving effects in many pharmacological deficit models. However, whether BAY 73-6691 (a selective PDE-9I) may attenuate the oxidative stress during the development of AD is still unclear. For this purpose, primary cultures of SH-SY5Y cells were incubated with 20μM beta-amyloid25-35 (Aβ25-35), followed by exposure to different concentrations (50, 100, 150 and 200μg/ml) of BAY 73-6691. Furthermore, the antioxidant effect of BAY 73-6691 was evaluated in mice subjected to intracerebroventricular injection of Aβ25-35 (day 0) and treatment with BAY 73-6691 by intraperitoneal injection once daily (days 1-10). Our results elucidated that treatment with BAY 73-6691 attenuated the Aβ25-35-induced cytotoxicity and oxidative stress in SH-SY5Y cells. In vivo, BAY 73-6691 protected Aβ25-35-induced oxidative damage in hippocampus, associated with the attenuation of impairments in hippocampal neurons.
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