G-36

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Cat.No. 4759 - G-36 | C22H22BrNO2 | CAS No. 1392487-51-2
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% (HPLC)
Datasheet
Citations
Reviews
Literature
Pathways

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 (IC50 = 112 nM). Structural analog of G-1 (Cat. No. 3577).

Technical Data

M. Wt 412.33
Formula C22H22BrNO2
Storage Store at -20°C
Purity ≥99% (HPLC)
CAS Number 1392487-51-2
PubChem ID 73755224
InChI Key QTOCPACSSHFGOY-ZCCHDVMBSA-N
Smiles BrC1=CC4=C(OCO4)C=[C@@]1[C@@H]2NC(C=CC(C(C)C)=C5)=C5[C@@]3([H])[C@@]([H])2CC=C3

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 41.23 100

Preparing Stock Solutions

The following data is based on the product molecular weight 412.33. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.43 mL 12.13 mL 24.25 mL
5 mM 0.49 mL 2.43 mL 4.85 mL
10 mM 0.24 mL 1.21 mL 2.43 mL
50 mM 0.05 mL 0.24 mL 0.49 mL

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Product Datasheets

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

References are publications that support the biological activity of the product.

Prossnitz and Barton (2011) The G-protein-coupled estrogen receptor GPER in health and disease. Nat.Rev.Endocrinol. 7 715 PMID: 21844907

Dennis et al (2011) Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J.Steroid Biochem.Mol.Biol. 127 358 PMID: 21782022


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Keywords: G-36, G-36 supplier, G36, G-protein-coupled, estrogen, receptors, GPER, GPR30, antagonists, selective, Estrogen, (GPER), Receptors, 4759, Tocris Bioscience

Citations for G-36

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* or download your copy today!

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GPCR

GPCR Product Listing

A collection of over 450 products for G protein-coupled receptors, the listing includes research tools for the study of:

  • Rhodopsin-like Receptors
  • Secretin-like Receptors
  • Glutamate Receptors
  • Frizzled Receptors
  • GPCR Signaling

Pathways for G-36

Estrogen

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.