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G-36

Cat. No. 4759 3 Citations Submit a Review Datasheet / COA / SDS
Pricing Availability   Qty
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 (3)
Reviews
Pathways (1)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for G-36

G-36 is an 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).

Compound Libraries for G-36

G-36 is also offered as part of the Tocriscreen 2.0 Max. Find out more about compound libraries available from Tocris.

Technical Data for G-36

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.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility Data for G-36

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

Preparing Stock Solutions for G-36

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

Select a batch to recalculate based on the batch molecular weight:
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

Molarity Calculator

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Product Datasheets for G-36

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References for G-36

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

If you know of a relevant reference for G-36, please let us know.

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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

3 Citations for G-36

Citations are publications that use Tocris products. Selected citations for G-36 include:

Bin et al (2020) G-protein-coupled estrogen receptor activation upregulates interleukin-1 receptor antagonist in the hippocampus after global cerebral ischemia: implications for neuronal self-defense. J Neuroinflammation 17 45 PMID: 32007102

Jing et al (2023) Anti-Inflammatory Actions of G-Protein-Coupled Estrogen Receptor 1 (GPER) and Brain-Derived Estrogen Following Cerebral Ischemia in Ovariectomized Rats. Biology (Basel) 12 PMID: 36671793

Meseke et al (2018) Distal Dendritic Enrichment of HCN1 Channels in Hippocampal CA1 Is Promoted by Estrogen, but Does Not Require Reelin. Eneuro 5 PMID: 30406178

Do you know of a great paper that uses G-36 from Tocris? Please let us know.

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Pathways for G-36

Estrogen Signaling Pathway

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.