2. Metabolic Enzyme/Protease
  3. Phosphodiesterase (PDE)
  4. BAY-7081

BAY-7081 is a potent, selective, orally active and soluble cyanopyridone-based PDE9A inhibitor with an IC50 of 15 nM.

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

BAY-7081 Chemical Structure

BAY-7081 Chemical Structure

CAS No. : 3036022-06-4

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Based on 1 publication(s) in Google Scholar

BAY-7081 Related Antibodies

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  • Biological Activity

  • Purity & Documentation

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  • Customer Review

Description

BAY-7081 is a potent, selective, orally active and soluble cyanopyridone-based PDE9A inhibitor with an IC50 of 15 nM[1].

IC50 & Target[1]

PDE9A

15 nM (IC50)

In Vivo

BAY-7081 (0.3 or 1.0 mg/kg; i.v. or p.o.) shows good in vivo PK properties[1].

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

Animal Model: Wistar rats and dogs[1]
Dosage: 0.3 or 1.0 mg/kg
Administration: Intravenous injection or oral (Pharmacokinetic Analysis)
Result: PK Profile of PDE9A Inhibitor BAY-7081 in Selected Speciesa[1]
species CLbb [L h–1 kg–1] VSSc [L kg–1] MRTd [h] Fe [%]
Rat 2.4 4.5 1.9 61
Dog 0.9 3.0 4.0 80

a Values were derived by intravenous (dose 0.3 mg/kg) and oral (dose 1.0 mg/kg) administration of solutions in either plasma 99% + DMSO 1% (rat iv) or EtOH/PEG400/H2O (dog iv, rat and dog po) vehicles.
bBlood clearance.
cVolume of distribution at steady state.
dMean residence time after iv application.
eOral bioavailability.
Molecular Weight

362.90

Formula

C19H27ClN4O
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(N(CC2)CCC32CC3)C4=C(NC1=O)C(CCC)CNC4.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMSO : 33.33 mg/mL (91.84 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.7556 mL 13.7779 mL 27.5558 mL
5 mM 0.5511 mL 2.7556 mL 5.5112 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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

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C2

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

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mg/kg

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g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation
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, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.7556 mL 13.7779 mL 27.5558 mL 68.8895 mL
5 mM 0.5511 mL 2.7556 mL 5.5112 mL 13.7779 mL
10 mM 0.2756 mL 1.3778 mL 2.7556 mL 6.8890 mL
15 mM 0.1837 mL 0.9185 mL 1.8371 mL 4.5926 mL
20 mM 0.1378 mL 0.6889 mL 1.3778 mL 3.4445 mL
25 mM 0.1102 mL 0.5511 mL 1.1022 mL 2.7556 mL
30 mM 0.0919 mL 0.4593 mL 0.9185 mL 2.2963 mL
40 mM 0.0689 mL 0.3444 mL 0.6889 mL 1.7222 mL
50 mM 0.0551 mL 0.2756 mL 0.5511 mL 1.3778 mL
60 mM 0.0459 mL 0.2296 mL 0.4593 mL 1.1482 mL
80 mM 0.0344 mL 0.1722 mL 0.3444 mL 0.8611 mL
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BAY-7081 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-70813036022-06-4BAY7081BAY 7081Phosphodiesterase (PDE)heart failurePDE9AInhibitorinhibitorinhibit

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