SML3150

GSK5182

≥95% (HPLC)

• Synonym(s): (δZ)-δ-[[4-[2-(Dimethylamino)ethoxy]phenyl](4-hydroxyphenyl)methylene]benzenebutanol, 4-[(Z)-1-[4-(2-Dimethylaminoethyloxy)phenyl]-hydroxy-2-phenylpent-1-enyl]phenol, GSK 5182, GSK-5182
• Empirical Formula (Hill Notation): C₂₇H₃₁NO₃
• CAS Number: 877387-37-6
• Molecular Weight: 417.54
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD31922700
• Assay: ≥95% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear (Wramed)
• storage temp.: 2-8°C
• SMILES string: N(CCOc1ccc(cc1)\C(=C(\CCCO)/c3ccccc3)\c2ccc(cc2)O)(C)C
• InChI key: ZVSFNBNLNLXEFQ-RQZHXJHFSA-N

Description

Biochem/physiol Actions

GSK5182 is an orally available 4-hydroxy-tamoxifen (4-OHT) analog and a high affinity estrogen receptor-related receptor γ (ERRγ) inverse agonist (68% inhibition at 1 µM by reporter assay) with 25-fold reduced affinity and little antagonistic activity toward ERRα (No inhibition against 100 nM estradiol-induced reporter activity up to 1 µM). GSK5182 effectively inhibits ERRγ-dependent gene expression and biological functions both in cultures (1-10 µM) and in various animal studies in vivo (10-80 mg/kg i.p. or p.o. in rats and mice).

Orally available, selective estrogen receptor-related receptor γ (ERRγ) inverse agonist with in vitro and in vivo efficacy.

Safety Information

• pictograms: GHS08
• signalword: Danger
• hcodes: H360,H362
• pcodes: P202 - P260 - P263 - P264 - P270 - P308 + P313
• Hazard Classifications: Lact. - Repr. 1A
• Storage Class: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable