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  • HOME
  • ABOUT
    • About
    • Why INDIGO
    • Key Personnel
      • Board of Directors & Advisors
      • Management
  • PRODUCTS
    • Assays
    • Ortholog Assays
    • Growth Factor Receptors
    • In Vitro Toxicology Platform
    • MDR1 / Human P-Glycoprotein
    • Gene Expression
    • NASH Nuclear Receptors For Research
    • Disease States
    • Live Cell Multiplex
    • Custom Assay Development
  • TECHNICAL
    • Nuclear Receptor Profiling & Panels
    • Assay Kit Platform & Formats
    • FAQ
    • Discovery Toxicology
    • upcyte® Hepatocytes
    • Technical Manuals & Product Listing
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    • Scientific Whitepapers from INDIGO
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    • Scientific Posters
    • INDIGO Press Releases
    • INDIGO in the News

Rheum rhaponticum Root Extract Improves Vasomotor Menopausal Symptoms and Estrogen-Regulated Targets in Ovariectomized Rat Model

ABSTRACT Ovarian insufficiency and ovariectomy are characterized by deregulated heat loss mechanisms. Unlike hormone therapy, ERr 731 (a standardized botanical extract of Siberian rhubarb Rheum rhaponticum L. high in rhaponticin) acts like a selective estrogen receptor modulator for ERβ receptors and may offer a higher degree of safety while maintaining the desired efficacy profile. InRead More

Filed Under: New Publications Tagged With: ERa, ERb, estrogen, estrogen receptor, estrogen receptor beta, Estrogen receptor α

Intramolecular [2+2] Photocycloaddition of Altrenogest: Confirmation of Product Structure, Theoretical Mechanistic Insight, and Bioactivity Assessment

ABSTRACT While studying the environmental fate of potent endocrine-active steroid hormones, we observed the formation of an intramolecular [2+2] photocycloaddition product (2) with a novel hexacyclic ring system following photolysis of altrenogest (1). The structure and absolute configuration were established by X-ray diffraction analysis. Theoretical computations identified a barrierless two-step cyclization mechanism for the formationRead More

Filed Under: New Publications Tagged With: androgen receptor, AR, endocrine-active steroid hormones, er, estrogen receptor, pregnane x receptor, PXR

Mechanism and therapeutic window of a genistein nanosuspension to protect against hematopoietic-acute radiation syndrome

ABSTRACT There are no FDA-approved drugs that can be administered prior to ionizing radiation exposure to prevent hematopoietic–acute radiation syndrome (H-ARS). A suspension of synthetic genistein nanoparticles was previously shown to be an effective radioprotectant against H-ARS when administered prior to exposure to a lethal dose of total body radiation. Here we aimed to determineRead More

Filed Under: New Publications Tagged With: ER beta, ERb, ERβ, estrogen receptor, H-ARS, hematopoietic-acute radiation syndrome, radiation, radioprotectant

Benzothiophene estrogen receptor modulators: Patent Application

ABSTRACT This invention is a benzothiophene estrogen receptor modulator or its pharmaceutically acceptable salt or a pharmaceutically acceptable composition thereof to treat an estrogen-related medical disorder. To view the rest of the patent application click HERE. Patent Application Number: 15/893295 Filing Date: 09 February 2018 Publication Date: 19 February 2019 Applicant & Assignee information: G1Read More

Filed Under: New Publications Tagged With: estrogen receptor, estrogen receptor modulator

Synthesis and evaluation of 4-cycloheptylphenols as selective Estrogen receptor-β agonists (SERBAs)

ABSTRACT A short and efficient route to 4-(4-hydroxyphenyl)cycloheptanemethanol was developed, which resulted in the preparation of a mixture of 4 stereoisomers. The stereoisomers were separated by preparative HPLC, and two of the stereoisomers identified by X-ray crystallography. The stereoisomers, as well as a small family of 4-cycloheptylphenol derivatives, were evaluated as estrogen receptor-beta agonists. The lead compound, 4-(4-hydroxyphenyl)cycloheptanemethanol was selective for activatingRead More

Filed Under: New Publications Tagged With: cancer, drug development, estrogen receptor, estrogen receptor agonist, SERBA

Evaluation of estrogenic potential by herbal formula, HPC 03 for in vitro and in vivo

ABSTRACT HPC 03 is herbal formula that consists of extracts from Angelica gigas, Cnidium officinale Makino and Cinnamomum cassia Presel. The present study evaluated the estrogenic potential of HPC 03 by using in vitro and in vivo models. The regulatory mechanisms of HPS 03 in estrogen-dependent MCF-7 cells were assessed. HPC 03 induced the proliferation of estrogen receptor-positive MCF-7 cells, andRead More

Filed Under: New Publications Tagged With: ERa, ERb, estrogen receptor, HPC 03, tamoxifen

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