An antagonist of the estrogen receptor GPER
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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
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
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    1 mg

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    10 mg

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    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).