2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. BAY 73-6691

BAY 73-6691 ((R)-BAY 73-6691) est un inhibiteur de PDE9A qui est puissant, pénétrant dans le cerveau et sélectif.

BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor.

For research use only. We do not sell to patients.

BAY 73-6691 Chemical Structure

BAY 73-6691 Chemical Structure

CAS No. : 794568-92-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
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10 mM * 1 mL in DMSO USD 132 In-stock
Solid
5 mg USD 120 In-stock
10 mg USD 160 In-stock
25 mg USD 310 In-stock
50 mg USD 540 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of BAY 73-6691:

BAY 73-6691 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE BAY 73-6691

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  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

BAY 73-6691 ((R)-BAY 73-6691) is a potent, brain penetrant, and selective PDE9A inhibitor[1].

IC50 & Target

PDE9

 

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

BAY 73-6691 Related Antibodies
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

356.73

Formula

C15H12ClF3N4O
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1C2=C(N(C3=CC=CC=C3Cl)N=C2)NC(C[C@@H](C)C(F)(F)F)=N1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (280.32 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: 2.5 mg/mL (7.01 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (7.01 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.8032 mL 14.0162 mL 28.0324 mL 70.0810 mL
5 mM 0.5606 mL 2.8032 mL 5.6065 mL 14.0162 mL
10 mM 0.2803 mL 1.4016 mL 2.8032 mL 7.0081 mL
15 mM 0.1869 mL 0.9344 mL 1.8688 mL 4.6721 mL
20 mM 0.1402 mL 0.7008 mL 1.4016 mL 3.5041 mL
25 mM 0.1121 mL 0.5606 mL 1.1213 mL 2.8032 mL
30 mM 0.0934 mL 0.4672 mL 0.9344 mL 2.3360 mL
40 mM 0.0701 mL 0.3504 mL 0.7008 mL 1.7520 mL
50 mM 0.0561 mL 0.2803 mL 0.5606 mL 1.4016 mL
60 mM 0.0467 mL 0.2336 mL 0.4672 mL 1.1680 mL
80 mM 0.0350 mL 0.1752 mL 0.3504 mL 0.8760 mL
100 mM 0.0280 mL 0.1402 mL 0.2803 mL 0.7008 mL
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BAY 73-6691 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BAY 73-6691794568-92-6Phosphodiesterase (PDE)Inhibitorinhibitorinhibit

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