An antagonist of the estrogen receptor GPER
Technical Support & Resources

Information provided in the product description is from published literature. Due to the nature of scientific experimentation, your results (e.g., selectivity and effective concentrations) or specific application for this product may differ. If you have questions about how this product fits your application, please contact our technical support staff.

Visit our FAQ

Contact Us

Toll Free Phone (USA and Canada Only): (888) 526-5351
Direct Phone: (734) 975-3888

Request Technical Support

Technical Support Request

To streamline the process attach the appropriate questionnaire to your inquiry.

Download IHC QuestionnaireDownload WB Questionnaire

View Our Privacy Statement for details on how we use and protect your data. In addition, this site is protected by hCaptcha and its Privacy Policy and Terms of Service apply.

G-15

Item No. 14673

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(3aS,4R,9bR)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
CAS Number
1161002-05-6
Molecular Formula
C19H16BrNO2
Formula Weight
370.2
Purity
≥95%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 30 mg/mlDMF:PBS (pH 7.2) (1:1): 0.5 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
207, 243, 293 nm
SMILES
BrC1=CC2=C(OCO2)C=C1[C@@H]3NC(C=CC=C4)=C4[C@@]5([H])[C@]3([H])CC=C5
InChi Code
InChI=1S/C19H16BrNO2/c20-15-9-18-17(22-10-23-18)8-14(15)19-13-6-3-5-11(13)12-4-1-2-7-16(12)21-19/h1-5,7-9,11,13,19,21H,6,10H2/t11-,13-,19+/m0/s1
InChi Key
YOLTZIVRJAPVPH-MJLGCCKJSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
Recommended Products

Certificates of Analysis & Batch Specific Data

Provide batch numbers separated by commas to download or request available product inserts, QC sheets, certificates of analysis, data packs, and GC-MS data.

Download most recent Certificate of Analysis for this product

    1 mg

    $69

    Add

    5 mg

    $132

    Add

    10 mg

    $198

    Add

    25 mg

    $412

    Add
    Product Description

    G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens.1 It is thought to be involved in estrogen-sensitive cancers.1,2 GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth.1 G-15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM).3 It displays low affinity cross-reactivity with the classical estrogen receptor (ER), ERα, so that at doses greater than 1 µM it is capable of mediating limited ER-dependent transcriptional activity.4 G-15 antagonizes the anti-depressive effects of estrogen in vivo.3

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Filardo, E.J., and Thomas, P. Minireview: G protein-coupled estrogen receptor-1, GPER-1: Its mechanism of action and role in female reproductive cancer, renal and vascular physiology. Endocrinology 153(7), 2953-2962 (2012).

    2. Chevalier, N., Vega, A., Bouskine, A., et al. GPR30, the non-classical membrane G protein related estrogen receptor, is overexpressed in human seminoma and promotes seminoma cell proliferation. PLoS One 7(4), 34672 (2012).

    3. Dennis, M.K., Burai, R., Ramesh, C., et al. In vivo effects of a GPR30 antagonist. Nat. Chem. Biol. 5(6), 421-427 (2009).

    4. Dennis, M.K., Field, A.S., Burai, R., et al. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J. Steroid Biochem. Mol. Biol. 127(3-5), 358-366 (2011).

    Product Citations

    Yang, Y., Wang, Y., Zou, H., et al. GPER1 signaling restricts macrophage proliferation and accumulation in human hepatocellular carcinoma. Front. Immunol. 15, 10.3389/fimmu.2024.1481972 (2024).

    Li, N., Xu, N., Lin, Y., et al. Roles of testosterone and estradiol in mediation of acute neuroendocrine and electroencephalographic effects of sevoflurane during the sensitive period in rat. Front. Endocrinol. (Lausanne) 11, 545973 (2020).