DG172 dihydrochloride

SKU: orb1299475

Description

DG172 dihydrochloride is a potent and selective PPARβ/δ antagonist with an IC50 of 27 nM. It is a valuable research tool for investigating the role of this nuclear receptor in metabolic diseases, inflammation, and cancer in both cellular and animal models.

Research Area

Metabolism Research, Molecular Biology

Key Properties

• CAS Number: 1361504-77-9
• MW: 455.2
• Purity: 99.87% (May vary between batches)
• Formula: C₂₀H₂₂BrCl₂N₃
• SMILES: Cl.Cl.CN1CCN(CC1)c1ccc(\C=C(/C#N)c2ccccc2Br)cc1
• Target: PPAR
• Solubility: H2O:14.29 mg/mL (31.39 mM)

Bioactivity

• Target IC50:
  PPARβ/δ:27 nM
• In Vitro:
  DG172 is a novel PPARβ/δ-selective ligand showing high binding affinity (IC(50) = 27 nM) and potent inverse agonistic properties. DG172 selectively inhibited the agonist-induced activity of PPARβ/δ, enhanced transcriptional corepressor recruitment, and down-regulated transcription of the PPARβ/δ target gene Angptl4 in mouse myoblasts (IC(50) = 9.5 nM). Importantly, DG172 was bioavailable after oral application to mice with peak plasma levels in the concentration range of its maximal inhibitory potency, suggesting that 37 will be an invaluable tool to elucidate the functions and therapeutic potential of PPARβ/δ.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Inhibitor, inhibit, DG 172, DG 172 Dihydrochloride, DG172, DG-172, DG172 (dihydrochloride), DG172 dihydrochloride, DG172 Dihydrochloride, DG-172 dihydrochloride, DG-172 Dihydrochloride, PPAR, Peroxisome proliferator-activated receptors

Compound Identifiers

PubChem CID

57342888