An antagonist of ERα (IC50 = 52.4 nM)

Ridaifen-B – 10 mg

Brand:
Cayman
CAS:
886465-70-9
Storage:
-20
UN-No:
Non-Hazardous - /

Ridaifen-B is an antagonist of estrogen receptor α (ERα; IC50 = 52.4 nM), an inverse agonist of cannabinoid (CB) receptor 2 (CB2; Ki = 43.7 nM), and a derivative of tamoxifen (Item No. 13258).{42930} It is selective for CB2 over CB1 receptors (Ki = 732 nM).{42931} Ridaifen-B was designed to be cytotoxic to cancer cells independent of ER binding; it inhibits growth of ER-positive and ER-negative cells in a panel of 39 cancer cell lines (GI50s = 0.20-2.14 µM).{42932} It induces apoptosis and autophagy in ER-negative Jurkat cells when used at a concentration of 0.4 µM.{42933} Ridaifen-B decreases nitric oxide (NO) production and protein levels of IL-1α and IL-6 in LPS-stimulated RAW 264.7 cells when used at a concentration of 1 µM.{42931}  

 

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Description

An antagonist of ERα (IC50 = 52.4 nM), an inverse agonist of CB2 (Ki = 43.7 nM), and a derivative of tamoxifen; selective for CB2 over CB1 receptors (Ki = 732 nM); designed to be cytotoxic to cancer cells independent of ER binding; it inhibits growth of ER-positive and ER-negative cells in a panel of 39 cancer cell lines (GI50s = 0.20-2.14 µM); induces apoptosis and autophagy in ER-negative Jurkat cells at 0.4 µM; decreases NO production and protein levels of IL-1α and IL-6 in LPS-stimulated RAW 264.7 cells at 1 µM

Formal name: 1,1′-[(2-phenyl-1-buten-1-ylidene)bis(4,1-phenyleneoxy-2,1-ethanediyl)]bis-pyrrolidine

Synonyms: 

Molecular weight: 510.7

CAS: 886465-70-9

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Receptor Pharmacology|Antagonists||Product Type|Biochemicals|Receptor Pharmacology|Inverse Agonists||Research Area|Cancer|Autophagy||Research Area|Cancer|Cell Death|Apoptosis||Research Area|Cell Biology|Cell Signaling|Nitric Oxide Signaling||Research Area|Immunology & Inflammation|Innate Immunity||Research Area|Neuroscience|Cannabinoid Research|CB1 & CB2 Receptors

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