Orphan Nuclear Receptor

Orphan nuclear receptor ligands act on nuclear receptors cloned before a natural ligand was known. The term dates from 1988, when estrogen-related receptors were identified by sequence similarity to the estrogen receptor. Many further superfamily members were found this way, as a 1995 review of the second decade of nuclear receptor research describes. Liver receptor homolog 1 (LRH-1, NR5A2) regulates development, metabolism and steroidogenesis. ML-180 is an LRH-1 inverse agonist, LRH-1 agonist-2 activates the receptor, and RJW100 activates LRH-1 together with steroidogenic factor 1 (SF-1). MI-883 activates and CINPA1 inhibits the constitutive androstane receptor (CAR). The set is mixed and also lists compounds for unrelated targets, such as splicing factor 3B subunit 1 (SF3B1).

6 Items

  • SB-423562 hydrochloride
    Cat. No.
    A59497

    SB-423562 hydrochloride

    SB-423562 hydrochloride is a potent calcium-sensing receptor (CaR) antagonist. It exhibits strong inhibitory effects on CaR signaling, making it a valuable tool for investigating calcium homeostasis and related metabolic disorders. This compound is particularly applicable in osteoporosis research, providing insights into bone density regulation and potential therapeutic interventions.

    25 mg
    $2,035.00
    50 mg
    $2,610.00
    All 3 sizes
  • BIM5078
    Cat. No.
    A85353

    BIM5078

    BIM5078 is an antagonist of hepatocyte nuclear factor 4α (HNF4α), which effectively inhibits the expression of target genes regulated by HNF4α. This compound has been shown to repress insulin promoter activity, making it a valuable tool for studying the roles of HNF4α in metabolic disorders. BIM5078 is utilized in research focusing on cancer and diabetes, contributing to the understanding of these diseases at a molecular level.

    5 mg
    $150.00
    10 mg
    $250.00
    All 4 sizes
  • BI-6015
    Cat. No.
    A85357

    BI-6015

    BI-6015 is an antagonist of hepatocyte nuclear factor 4α (HNF4α), effectively inhibiting the expression of HNF4α target genes. By repressing insulin promoter activity, it serves as a valuable tool for studying the regulatory mechanisms governed by HNF4α. BI-6015 is applicable in research focused on cancer and diabetes, providing insights into metabolic and oncogenic pathways.

    2 mg
    $30.00
    5 mg
    $45.00
    All 7 sizes
  • 7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene
    Cat. No.
    A85363

    7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene

    7-[4-(2-Piperidinyl)ethoxy]benzoyl Raloxifene is an LRH-1 antagonist, exhibiting an IC50 of 3.1 μM. This compound is valuable for studying the role of LRH-1 in various biological processes, including lipid metabolism and endocrine signaling. Its pharmacological properties make it a suitable tool for investigating potential therapeutic targets in metabolic diseases and hormone-related conditions.

    5 mg
    $230.00
    10 mg
    $380.00
    All 5 sizes
  • LRH-1 antagonist-1
    Cat. No.
    A85373

    LRH-1 antagonist-1

    LRH-1 antagonist-1 is a selective antagonist of Liver Receptor Homolog-1 (LRH-1) with a Kd of 1.8 μM. This compound effectively inhibits the transcriptional activity of LRH-1, leading to reduced expression of G0S2 and subsequent inhibition of proliferation in LRH-1-positive cancer cells. It is suitable for research applications in pancreatic, colon, and breast cancer studies, where targeting LRH-1 may provide valuable insights into tumor growth and progression.

    Out of stock

    All 3 sizes
  • LRH-1 antagonist-1 dihydrochloride
    Cat. No.
    A85376

    LRH-1 antagonist-1 dihydrochloride

    LRH-1 antagonist-1 dihydrochloride is a selective antagonist of Liver Receptor Homolog-1 (LRH-1), exhibiting a Kd of 1.8 μM. This compound effectively inhibits the transcriptional activity of LRH-1, leading to a decrease in the expression of G0S2. Furthermore, it demonstrates the ability to suppress the proliferation of LRH-1-positive cancer cells, making it a valuable tool for research in pancreatic, colon, and breast cancer.

    Out of stock

    All 3 sizes

6 Items

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