GSK-3787, PPARd antagonist

Product Details

Formal Name: 4-Chloro-N-(2-{[5-(trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide

Molecular Formula: C₁₅H₁₂ClF₃N₂O₃S

Formula Weight: 392.80

CAS Number: 188591-46-0

Purity: >98%

Formulation: powder

Solubility: Soluble in DMSO (up to 30 mg/ml).

Storage: -20°C

Stability: ≥ 1 year.

Applications

PPARd antagonist

Functions

Selective and irreversible antagonist of peroxisome proliferator-activated receptor beta/delta (PPARβ/δ) (plC50 = 6.6), but not PPARα or ɣ. It covalently binds to Cys 249 in the PPARβ/δ binding site1. When applied topically, GSK-3787 showed efficacy against an inflammatory skin disease resembling psoriasis in mice. Suppresses colorectal cancer tumorigenesis in Apc(δ580) mice.

Application Procedures

First dissolved in DMSO (up to 30 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Documents

• Datasheet (PDF)
• MSDS (PDF)