1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. Bay 60-7550

Bay 60-7550  (Synonyms: BAY 607550)

Cat. No.: HY-14992 Purity: 98.14%
COA Handling Instructions

Bay 60-7550 is a potent and selective PDE2 inhibitor with a Ki of 3.8 nM.

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

Bay 60-7550 Chemical Structure

Bay 60-7550 Chemical Structure

CAS No. : 439083-90-6

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Customer Review

Based on 4 publication(s) in Google Scholar

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View All Phosphodiesterase (PDE) Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Bay 60-7550 is a potent and selective PDE2 inhibitor with a Ki of 3.8 nM.

IC50 & Target

PDE2

 

In Vitro

Bay 60-7550 (1 μM) increases cGMP in the neuronal cultures compared with control [F(6,14)=12.97, p<0.05 for Bay 60-7550]. Bay 60-7550 in the presence of NMDA (30 μM) results in further increases in cGMP compared with NMDA alone. The NMDA receptor antagonist MK-801 (10 μM) blocks both Bay 60-7550+NMDA-induced elevation in cGMP in neuronal cultures[1]. Compared with untreated control cells, proliferation of PASMCs from IPAH patients is significantly reduced by BAY 60-7550 (1 μM)[2].

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

In Vivo

The PDE2 inhibitors Bay 60-7550 (1 mg/kg) reverses restraint stress-induced alterations in behavior, resulting in increased percentages of open-arm entries and open-arm time compared with the vehicle + restraint stress condition. In nonstressed mice, Bay 60-7550 produces a dose-dependent increase in percentages of open-arm entries and open-arm time compared with the vehicle-treated group; significant increases are observed at a dose of 3 mg/kg. In nonstressed mice, Bay 60-7550 increases, in a dose-dependent manner, the number of head-dips and time spent head-dipping, compared with vehicle-treated mice; significant increases are observed at doses of 1 and 3 mg/kg[1].

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

Molecular Weight

476.57

Formula

C27H32N4O4

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1N=C(NN2C1=C(N=C2[C@@H](CCCC3=CC=CC=C3)[C@@H](C)O)C)CC4=CC=C(C(OC)=C4)OC

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 : ≥ 33.3 mg/mL (69.87 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 2.0983 mL 10.4916 mL 20.9833 mL
5 mM 0.4197 mL 2.0983 mL 4.1967 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    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

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

    Solubility: ≥ 2.5 mg/mL (5.25 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    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.
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
Kinase Assay
[1]

COS-7 cells are maintained in complete DMEM (containing 10% fetal calf serum, 100 units/mL penicillin G, 100 mg/mL streptomycin, and 400 μM L-alanyl-L-glutamine) at 37°C in 5% CO2 atmosphere. A PDE2 expression plasmid is introduced into COS-7 cells using the FuGENE6 transfection reagent. Cells are lysed in solubilization buffer (275 mM NaCl, 1.5 mM MgCl2, 2 mM EGTA, 2% Triton X, 20% glycerol, and 40 mM Tris-HCl), and the cell lysates are used in the immunoprecipitation procedures. A protein A-agarose bead slurry (100 μL) is washed three times with ice-cold phosphate-buffered saline (100 mM NaCl, 2.7 mM KCl, 10.6 mM Na2HPO4, and 1.6 mM NaH2PO4) and mixed with the 5 μg of PDE2 antibody and 100 μL (2 μg/μL) of the lysate sample and rotated overnight at 4°C. The bead/sample mixture is then centrifuged at 1000g to separate the beads from the supernatant. The beads are resuspended in 100 μL of ice-cold lysis buffer (20 mM Tris, pH 7.4, 140 mM NaCl, 0.75 mM MgCl2, 1 mM EGTA, 1% Triton X-100, and 20% glycerol, containing protease and phosphatase inhibitors) to elute the PDE2 for use in the enzyme activity assays. The PDE2 activity assay is done. The recombinant PDE2 enzyme derived from COS-7 cell expression and diluted in KHEM buffer (50 mM KCl, 50 mM HEPES, 10 mM EGTA, and 1.9 mM MgCl2, pH 7.2) is mixed with different concentrations of PDE2 inhibitors (Bay 60-7550, ND7001, and EHNA) and [3H]cGMP/cGMP (5 μM) as the substrate. The mixture is then incubated for 30 min at 37°C (100 μL of reaction volume). To convert the [3H]GMP to [3H]guanosine, samples are incubated with snake venom from Crotalus atrox for 30 min at 37°C. The samples are then vortexed with a freshly prepared slurry of Dowex/water/ethanol [1:1:1, v/v] and then centrifuged for 10 min. [3H]Guanosine in the supernatant is then quantified by liquid scintillation counting. Bay 60-7550 is dissolved in dimethyl sulfoxide, EHNA is dissolved in distilled water, and ND7001 is dissolved in ethanol as 10 mM stocks and then diluted for use in assays with 20 mM Tris, pH 7.4; final concentrations of the respective solvents did not affect the assay. IC50 values at a single substrate concentration are determined by nonlinear regression analysis of the log concentration-response curves for each PDE2 inhibitor; Ki values are calculated[1].

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

Cell Assay
[2]

Growth of human distal pulmonary artery smooth muscle cells isolated from patients with idiopathic pulmonary arterial hypertension (IPAH) or control cells from adults undergoing transplant or lung resection for suspected malignancy, are monitored following treatment with BAY 60-7550 (1 μM), ANP (1 μM), DETA-NONOate (10 μM), or Treprostinil (1 μM), alone or in combination[2].

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

Animal Administration
[1]

Mice[1]
Male ICR mice weighing 28 to 35 g are used. Bay 60-7550 (0.5, 1, and 3 mg/kg), ND7001 (0.5, 1.0, and 3 mg/kg), Detanonoate (0.5 mg/kg), L-NAME (50 mg/kg), or Diazepam (1 mg/kg) is administered after restraint stress and 30 min before behavioral testing. Mice also are treated with Bay 60-7550 (3 mg/kg), ND7001 (3 mg/kg), Detanonoate, (0.5 mg/kg), L-NAME (50 mg/kg), or diazepam (1 mg/kg) in the absence of restraint stress; drugs are administered 30 min before the behavioral tests. Bay 60-7550 shows 50-fold selectivity for PDE2 compared with PDE1, 100-fold compared with PDE5, and greater than 200-fold compared with the other PDE families. ND7001 exhibits at 1east 100-fold selectivity for inhibition of PDE2 relative to other PDE families. For antagonism tests to assess the role of cGMP signaling in the behavioral effects of the PDE2 inhibitors, ODQ, an inhibitor of soluble guanylyl cyclase (20 mg/kg), is administered 20 min before Bay 60-7550 or ND7001.

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 2.0983 mL 10.4916 mL 20.9833 mL 52.4582 mL
5 mM 0.4197 mL 2.0983 mL 4.1967 mL 10.4916 mL
10 mM 0.2098 mL 1.0492 mL 2.0983 mL 5.2458 mL
15 mM 0.1399 mL 0.6994 mL 1.3989 mL 3.4972 mL
20 mM 0.1049 mL 0.5246 mL 1.0492 mL 2.6229 mL
25 mM 0.0839 mL 0.4197 mL 0.8393 mL 2.0983 mL
30 mM 0.0699 mL 0.3497 mL 0.6994 mL 1.7486 mL
40 mM 0.0525 mL 0.2623 mL 0.5246 mL 1.3115 mL
50 mM 0.0420 mL 0.2098 mL 0.4197 mL 1.0492 mL
60 mM 0.0350 mL 0.1749 mL 0.3497 mL 0.8743 mL
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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.

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