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BI-409306 PDE inhibitor

Cat.No.S0039

BI 409306 (SUB 166499) is a potent and selective inhibitor of human and rat PDE9A with mean IC50 of 65 nM and 168 nM, respectively. Treatment with BI 409306 increases brain cGMP levels, promotes long-term potentiation, and improves episodic and working memory performance in rodents.
BI-409306 PDE inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 311.34

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S003901 DMSO]62 mg/mL]false]Ethanol]4 mg/mL]false]Water]˂1 mg/mL]false Purity: 99.91%
99.91

Chemical Information, Storage & Stability

Molecular Weight 311.34 Formula

C16H17N5O2

 Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1189767-28-9 -- Storage of Stock Solutions

Synonyms SUB 166499 Smiles C1COCCC1N2C3=C(C=N2)C(=O)NC(=N3)CC4=CC=CC=N4

Solubility

In vitro
Batch:

DMSO : 62 mg/mL (199.13 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 4 mg/mL

Water : ˂1 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

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Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO
%
% Tween 80
% ddH2O
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Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
human PDE9A [1]
(Cell-free assay)
65 nM
rat PDE9A [1]
(Cell-free assay)
168 nM
References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03505151 Completed
Healthy
Boehringer Ingelheim
 April 27 2018 Phase 1
NCT03193307 Completed
Healthy
Boehringer Ingelheim
 June 29 2017 Phase 1
NCT03151499 Completed
Healthy
Boehringer Ingelheim
 May 30 2017 Phase 1
NCT02597998 Completed
Healthy
Boehringer Ingelheim
 September 15 2015 Phase 1

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