APD597

Synonyms: JNJ-38431055

APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).

APD597 Chemical Structure

APD597 Chemical Structure

CAS: 897732-93-3

Purity & Quality Control

Batch: S011001 DMSO] 96 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.98%
99.98

Choose Selective GPR Inhibitors

Biological Activity

Description APD-597 (JNJ-38431055) is a potent and selective G protein-coupled receptor 119 (GPR119) agonist with EC50 of 46 nM for hGPR119 and an inhibitor of Cytochrome P450 2C9 (CYP2C9) with IC50 of 5.8 μM. APD-597 (JNJ-38431055) is developed for treating Type 2 diabetes (T2D).
Targets
hGPR119 [1]
(Cell-free assay)
CYP2C9 [1]
(Cell-free assay)
46 nM(EC50) 5.8 μM
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT00910923 Completed Diabetes Mellitus Type 2 Johnson & Johnson Pharmaceutical Research & Development L.L.C. November 2008 Phase 1

Chemical lnformation & Solubility

Molecular Weight 479.55 Formula

C21H29N5O6S

CAS No. 897732-93-3 SDF --
Smiles CC1=C(C=CC(=N1)S(=O)(=O)C)NC2=C(C(=NC=N2)OC3CCN(CC3)C(=O)OC(C)C)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 96 mg/mL ( (200.18 mM); Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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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.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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