G7423

GSK3787

≥98% (HPLC), white to off-white, powder

• Synonym(e): 4-Chloro-N-(2-{[5-trifluoromethyl)-2-pyridyl]sulfonyl}ethyl)benzamide
• Empirische Formel (Hill-System): C₁₅H₁₂ClF₃N₂O₃S
• CAS-Nummer: 188591-46-0
• Molekulargewicht: 392.78
• NACRES: NA.77
• PubChem Substance ID: 329799963
• UNSPSC Code: 12352200
• MDL number: MFCD00099612
• Assay: ≥98% (HPLC)
• Form: powder
• Storage condition: desiccated

Eigenschaften

• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: powder
• storage condition: desiccated
• color: white to off-white
• solubility: DMSO: ≥10 mg/mL
• originator: GlaxoSmithKline
• storage temp.: 2-8°C
• SMILES string: O=S(C1=CC=C(C=N1)C(F)(F)F)(CCNC(C2=CC=C(Cl)C=C2)=O)=O
• InChI: 1S/C15H12ClF3N2O3S/c16-12-4-1-10(2-5-12)14(22)20-7-8-25(23,24)13-6-3-11(9-21-13)15(17,18)19/h1-6,9H,7-8H2,(H,20,22)
• InChI key: JFUIMTGOQCQTPF-UHFFFAOYSA-N

Beschreibung

Application

GSK3787 has been used to inhibit the role of peroxisome proliferator-activated receptor-delta (PPARδ), during the pre-implantation period of bovine embryonic development. It has also been used as a PPARδ-specific inhibitor in in vitro maturation (IVM) media to inhibit PPARδ.

Biochem/physiol Actions

GSK3787 is known to exhibit pharmacokinetic properties.

GSK3787 is an orally available selective irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) antagonist (pIC50=6.6) with no measurable affinity for hPPARR or hPPARγ (pIC50<5).

GSK3787 is an orally available selective irreversible Peroxisome Proliferator-Activated Receptor δ (PPARδ) antagonist (pIC50=6.6) with no measurable affinity for hPPARR or hPPARγ (pIC50<5). It acts by covalently modifying Cys249 within the ligand binding pocket, and has been shown to antagonize the induction of PPARδ-regulated target genes in skeletal muscle cells.

Features and Benefits

This compound is a featured product for Gene Regulation research. Click here to discover more featured Gene Regulation products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

This compound was developed by GlaxoSmithKline. To browse the list of other pharma-developed compounds and Approved Drugs/Drug Candidates, click here.

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• Was ist los?: WGK 3
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable