Etalocib (LY293111, VML295) is a small-molecule benzofuran derivative originally developed as a leukotriene B4 receptor antagonist and later identified as a peroxisome proliferator-activated receptor gamma (PPARγ) agonist. It exhibits anti-inflammatory and anticancer properties. In preclinical models, Etalocib has shown nanomolar potency in inhibiting LTB4 binding to its receptor (IC₅₀ ≈ 5–10 nM) and demonstrates significant PPARγ activation at micromolar concentrations (EC₅₀ ≈ 1–5 µM). Antitumor activity has been observed in various cancer cell lines, including pancreatic and colon cancer, with reported GI₅₀ values ranging from ~0.5 to 5 µM.
MedKoo Cat#: 201310
Name: Etalocib free acid
CAS#: 161172-51-6 (free base)
Chemical Formula: C33H32FNaO6
Exact Mass: 285.3032
Molecular Weight: 566.59
Elemental Analysis: C, 69.95; H, 5.69; F, 3.35; Na, 4.06; O, 16.94
| Solvent | mg/mL | mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 98.5 | 173.85 |
The following data is based on the product molecular weight 566.59 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
