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DG172 dihydrochloride PPAR antagonist

Cat.No.S0531

DG-172 dihydrochloride is a novel PPARβ/δ-selective antagonist with the IC50 of 27 nM.
DG172 dihydrochloride PPAR antagonist Chemical Structure

Chemical Structure

Molecular Weight: 455.22

Quality Control

Batch: S053101 DMSO]91 mg/mL]false]Water]44 mg/mL]false]Ethanol]23 mg/mL]false Purity: 99.17%
99.17

Chemical Information, Storage & Stability

Molecular Weight 455.22 Formula

C20H20BrN3.2ClH

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 1361504-77-9 -- Storage of Stock Solutions

Synonyms N/A Smiles CN1CCN(CC1)C2=CC=C(C=C2)C=C(C#N)C3=CC=CC=C3Br.Cl.Cl

Solubility

In vitro
Batch:

DMSO : 91 mg/mL (199.9 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 44 mg/mL

Ethanol : 23 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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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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Mechanism of Action

Targets/IC50/Ki
PPARβ/δ [1]
(in a competitive TR-FRET assay)
27 nM
In vitro

DG-172 dihydrochloride selectively inhibits the agonist-induced activity of PPARβ/δ, enhances transcriptional corepressor recruitment, and down-regulates transcription of the PPARβ/δ target gene Angptl4 in mouse myoblasts. [1]

References

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