Free shipping on all orders over $ 500


Cat. No. M4836
G-1 Structure


Size Price Availability Quantity
1mg USD 45  USD50 In stock
5mg USD 82.8  USD92 In stock
10mg USD 131.4  USD146 In stock
Free Delivery on orders over USD 500 Bulk Inquiry?

Quality Control
Biological Activity

G-1 profoundly inhibited MCF-7 cell growth, potentially via p53 and p21 induction. Further, flow cytometry showed that G-1 blocked MCF-7 cell cycle progression at the G(1) phase.G-1 inhibits the production of lipopolysaccharide (LPS)-induced cytokines such as TNF-alpha and IL-6 in a dose-dependent manner in human primary macrophages and in a murine macrophage cell line. In vivo, G-1 is able to reduce the severity of disease in both active and passive EAE models of multiple sclerosis in SJL mice and that this effect is concomitant with a G-1-mediated decrease in proinflammatory cytokines, including IFN-gamma and IL-17, in immune cells harvested from these mice. The effect of G-1 appears indirect, as the GPR30 agonist did not directly influence IFN-gamma or IL-17 production by purified T cells. These data indicate that G-1 may represent a novel therapeutic agent for the treatment of chronic autoimmune, inflammatory diseases. G-1 was able to induce both c-fos expression and proliferation in the ERalpha-negative/GPR30-positive SKBR3 breast cancer cells, the requirement for ERalpha expression in GPR30/EGFR signaling may depend on the specific cellular context of different tumor types.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 412.28
Formula C21H18BrNO3
CAS Number 881639-98-1
Purity >99%
Solubility DMSO: ≥ 40 mg/mL (Need ultrasonic)
Storage at -20°C

The G protein-coupled receptor GPR30 inhibits proliferation of estrogen receptor-positive breast cancer cells.
Ariazi EA, et al. Cancer Res. 2010 Feb 1;70(3):1184-94. PMID: 20086172.

Beneficial role of the GPR30 agonist G-1 in an animal model of multiple sclerosis.
Blasko E, et al. J Neuroimmunol. 2009 Sep 29;214(1-2):67-77. PMID: 19664827.

G protein-coupled receptor 30 (GPR30) mediates gene expression changes and growth response to 17beta-estradiol and selective GPR30 ligand G-1 in ovarian cancer cells.
Albanito L, et al. Cancer Res. 2007 Feb 15;67(4):1859-66. PMID: 17308128.

Related Estrogen Receptor Products

27-Hydroxycholesterol is a selective estrogen receptor modulator, and it is also an agonist of the liver X receptor.

SAR439859 (Amcenestrant)

SAR439859 (Amcenestrant) is an orally active, nonsteroidal and selective degrader of estrogen receptor, it is also a potent antagonist of ER with EC50 of 0.2 nM for ERα degradation.


4-Hydroxytamoxifen is a selective estrogen receptor modulator.

Methylpiperidino pyrazole

Methylpiperidino pyrazole (MPP) is an agonist for estrogen receptor α and lacks any ligand functionality with estrogen receptor (ER)β.

Endoxifen E-isomer hydrochloride

Endoxifen E-isomer hydrochloride is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM).

Abmole Inhibitor Catalog 2017

Keywords: G-1, G1 supplier, Estrogen Receptor, inhibitors

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.