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G-36

4759 Datasheet / COA / SDS
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4759/10
4759/50
Estrogen and Related Receptor Antagonists Small Molecule
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Description: Selective GPER antagonist

Chemical Name: (±)-(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-8-(1-methylethyl)-3H-cyclopenta[c]quinoline

Purity: ≥99%

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Biological Activity

Antagonist of GPER; selectively inhibits estrogen-mediated activation of PI3-K by GPER, but not by ERα. Also inhibits estrogen-mediated calcium mobilization (IC 50 = 112 nM). Structural analog of G-1 (Cat. No. 3577).

Technical Data

M.Wt:
412.33
Formula:
C22H22BrNO2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥99%
Storage:
Store at -20°C
CAS No:
1392487-51-2

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.

Background References

  1. The G-protein-coupled estrogen receptor GPER in health and disease.
    Prossnitz and Barton
    Nat.Rev.Endocrinol., 2011;7:715
  2. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity.
    Dennis et al.
    J.Steroid Biochem.Mol.Biol., 2011;127:358

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VersaClone cDNA Plasmids

Human GPER/GPR30 (NP_001496) VersaClone cDNA

RDC0352

Mouse GPER/GPR30 (NP_084047) VersaClone cDNA

RDC0390

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