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Indazole-Cl is a selective estrogen receptor modifier (SERM), a selective ERβ agonist with > 100-fold selectivity for ERβ over Erα. In a recent study reported in Cell, Indazole-Cl, but not structurally distinct ERβ-specific ligands DPN and ERB-041, blocked the expression of proinflammatory genes in microglia and astrocytes, repressing induction of factors that promote Th17 T cell differentiation and activation. Indazole-Cl is believed to bind to the ERβ that is part of an ADIOL-ERβ-CtBP transrepression pathway that mediates recruitment of CtBP corepressor complexes to AP-1-dependent promoters, repressing genes that amplify inflammatory responses and activate Th17 T cells. In studies of experimental autoimmune encephalitis (EAE), a mouse model of Multiple sclerosis, Indazole-Cl both prevented the development of EAE when given prophylactically and caused significant improvement of EAE when provided to mice after they exhibited symptoms of disease.
| Molecular Weight | 260.68 |
| Formula | C13H9ClN2O2 |
| CAS Number | 848142-62-1 |
| Solubility (25°C) | DMSO: ≥5 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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