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G-1

Cat. No. M4836
G-1 Structure
Synonym:

G1

Size Price Availability Quantity
1mg USD 45  USD50 In stock
5mg USD 82.8  USD92 In stock
10mg USD 131.4  USD146 In stock
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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
References

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.

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

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