A selective antagonist of the estrogen receptor GPER
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G-36

Item No. 14397

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
(4S)-rel-4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4,5,9bS-tetrahydro-8-(1-methylethyl)-3H-cyclopenta[c]quinoline
CAS Number
1392487-51-2
Molecular Formula
C22H22BrNO2
Formula Weight
412.3
Purity
≥98%
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
206, 243, 293 nm
SMILES
BrC1=CC2=C(OCO2)C=C1[C@@H]3NC(C=CC(C(C)C)=C4)=C4[C@@]5([H])[C@]3([H])CC=C5
InChi Code
InChI=1S/C22H22BrNO2/c1-12(2)13-6-7-19-16(8-13)14-4-3-5-15(14)22(24-19)17-9-20-21(10-18(17)23)26-11-25-20/h3-4,6-10,12,14-15,22,24H,5,11H2,1-2H3/t14-,15+,22-/m1/s1
InChi Key
QTOCPACSSHFGOY-ZCCHDVMBSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $36

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    5 mg

    $128

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    10 mg

    $203

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    50 mg

    $920

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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-36 is a cell-permeable non-steroidal antagonist of GPER, inhibiting activation by either 17β-estradiol (Item No. 10006315) or the GPER-selective agonist LNS 8801 (Item No. 10008933) (IC50 = 112 and 165 nM, respectively).3 It has no detectable binding activity to either ERα or ERβ.3 G-36 blocks the activation of PI3K or calcium mobilization triggered by estrogen through GPER and it suppresses ERK activation by estrogen or LNS 8801 but not by EGF.3 G-36 can be used in combination with GPER-selective agonists, like LNS 8801, to distinguish the roles of GPER from those of ERα and ERβ in complex biological systems.3,4

    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., 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).

    4. Brailoiu, G.C., Arterburn, J.B., Oprea, T.I., et al. Bradycardic effects mediated by activation of G protein-coupled estrogen receptor in rat nucleus ambiguus. Exp. Physiol. 98(3), 679-691 (2013).