An ERRγ inverse agonist
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GSK5182

Item No. 19097

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
δZ-[[4-[2-(dimethylamino)ethoxy]phenyl](4-hydroxyphenyl)methylene]-benzenebutanol
CAS Number
877387-37-6
Molecular Formula
C27H31NO3
Formula Weight
417.5
Purity
≥95%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Sparingly soluble: 1-10 mg/mlEthanol: Slightly soluble: 0.1-1 mg/ml
SMILES
OC1=CC=C(/C(C2=CC=C(OCCN(C)C)C=C2)=C(CCCO)/C3=CC=CC=C3)C=C1
InChi Code
InChI=1S/C27H31NO3/c1-28(2)18-20-31-25-16-12-23(13-17-25)27(22-10-14-24(30)15-11-22)26(9-6-19-29)21-7-4-3-5-8-21/h3-5,7-8,10-17,29-30H,6,9,18-20H2,1-2H3/b27-26-
InChi Key
ZVSFNBNLNLXEFQ-RQZHXJHFSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    1 mg

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    5 mg

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    10 mg

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    25 mg

    $372

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    GSK5182 is an inverse agonist of estrogen-related receptor γ (ERRγ; IC50 = 77 nM in a reporter assay) and a derivative of (Z)-4-hydroxy tamoxifen (Item No. 14854).1 It selectively binds to ERRγ over ERα, ERRα, and ERRβ (IC50s = 0.11, 2, >10, and >10 µM, respectively). GSK5182 enhances radioiodine uptake and membrane localization of the sodium/iodide symporter (NIS) in BHT-101 and CAL-62 anaplastic thyroid cancer cells.2 It inhibits osteoclastogenesis induced by RANKL and macrophage colony-stimulating factor (M-CSF) in primary mouse bone marrow-derived macrophages (BMDMs) and induces apoptosis in osteoclasts when used at a concentration of 10 µM.3 GSK5182 (10 µM) inhibits fibrinogen secretion induced by the cannabinoid 1 (CB1) receptor agonist ACEA (arachidonoyl 2'-chloroethylamide; Item No. 91054) in AML12 hepatocytes.4 In vivo, GSK5182 (40 mg/kg) decreases blood glucose levels in a pyruvate tolerance test in a mouse model of high-fat diet-induced obesity.5

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kim, J., Song, J., Ji, H.D., et al. Discovery of potent, selective, and orally bioavailable estrogen-related receptor-γ inverse agonists to restore the sodium iodide symporter function in anaplastic thyroid cancer. J. Med. Chem. 62(4), 1837-1858 (2019).

    2. Singh, T.D., Jeong, S.Y., Lee, S.W., et al. Inverse agonist of estrogen-related receptor γ enhances sodium iodide symporter function through mitogen-activated protein kinase signaling in anaplastic thyroid cancer cells. J. Nucl. Med. 56(11), 1690-1696 (2015).

    3. Kim, H.J., Yoon, H.J., Lee, D.K., et al. The estrogen-related receptor γ modulator, GSK5182, inhibits osteoclast differentiation and accelerates osteoclast apoptosis. BMB Rep. 54(5), 266-271 (2021).

    4. Zhang, Y., Kim, D.K., Jung, Y.S., et al. Inverse agonist of ERRγ reduces cannabinoid receptor type 1-mediated induction of fibrinogen synthesis in mice with a high-fat diet-intoxicated liver. Arch. Toxicol. 92(9), 2885-2896 (2018).

    5. Kim, D.K., Gang, G.T., Ryu, D., et al. Inverse agonist of nuclear receptor ERRγ mediates antidiabetic effect through inhibition of hepatic gluconeogenesis. Diabetes 62(9), 3093-3102 (2013).