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SIM-688 is a selective and orally active estrogen receptor inhibitor of NF-κB transcriptional activity (IC50 = 122 nM in HAECT-1 cells).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $152 | In Stock | |
5 mg | $378 | In Stock | |
10 mg | $612 | In Stock | |
25 mg | $1,220 | In Stock | |
50 mg | $1,960 | In Stock |
Description | SIM-688 is a selective and orally active estrogen receptor inhibitor of NF-κB transcriptional activity (IC50 = 122 nM in HAECT-1 cells). |
Targets&IC50 | NF-κB-luc:122 nM (in HAECT-1 cell), NF-κB: |
In vitro | SIM-688 displaces [3H]E2 from the ERα ligand-binding domain protein (C50=2.43 μM) and from the ERβ ligand-binding domain protein (IC50=1.5 μM)[1]. |
In vivo | SIM-688 (5 mg/kg per day, p.o.) inhibits pro-inflammatory genes including MHI, VCAM-1, RANTES, and TNF-α and induces the gene products and uterine wet weight. SIM-688 (0.3 mg/kg, p.o.) is active in the Lewis rat adjuvant-induced arthritis model [1]. |
Alias | SIM688 |
Molecular Weight | 556.62 |
Formula | C34H31F3N2O2 |
Cas No. | 796854-35-8 |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 90 mg/mL (161.7 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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