G-1

G-1 - Names and Identifiers

Name	G-1
Synonyms	G-1 G-06710-1 1-((3aS,4R,9bR)-4-(6-bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethanone 1-((3aR,4S,9bS)-rel-4-(6-Bromobenzo[d][1,3]dioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl)ethanone (±)-1-[(3aR,4S,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone Ethanone, 1-[(3aR,4S,9bS)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-, rel-
CAS	881639-98-1

G-1 - Physico-chemical Properties

Molecular Formula	C21H18BrNO3
Molar Mass	412.28
Density	1.457±0.06 g/cm3(Predicted)
Boling Point	529.6±50.0 °C(Predicted)
Solubility	Soluble in DMSO
pKa	1.20±0.40(Predicted)
Storage Condition	Store at -20°C
Use	G-1 is a non-steroidal selective agonist of G protein-coupled receptor 30 (GPR30, G protein-coupled estrogen receptor 1, GPER) with a Ki value of 11 nM.

G-1 - Reference

Reference

1: Thomas P. Rapid steroid hormone actions initiated at the cell surface and the receptors that mediate them with an emphasis on recent progress in fish models. Gen Comp Endocrinol. 2012 Feb 1;175(3):367-83. doi: 10.1016/j.ygcen.2011.11.032. Epub 2011 Nov 29. Review. PubMed PMID: 22154643; PubMed Central PMCID: PMC3264783.
2: Revankar CM, Mitchell HD, Field AS, Burai R, Corona C, Ramesh C, Sklar LA, Arterburn JB, Prossnitz ER. Synthetic estrogen derivatives demonstrate the functionality of intracellular GPR30. ACS Chem Biol. 2007 Aug 17;2(8):536-44. Epub 2007 Jul 27. PubMed PMID: 17655271.
3: Song RX, Fan P, Yue W, Chen Y, Santen RJ. Role of receptor complexes in the extranuclear actions of estrogen receptor alpha in breast cancer. Endocr Relat Cancer. 2006 Dec;13 Suppl 1:S3-13. Review. PubMed PMID: 17259556.
4: Revankar CM, Cimino DF, Sklar LA, Arterburn JB, Prossnitz ER. A transmembrane intracellular estrogen receptor mediates rapid cell signaling. Science. 2005 Mar 11;307(5715):1625-30. Epub 2005 Feb 10. PubMed PMID: 15705806.

G-1 - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	2.426 ml	12.128 ml	24.255 ml
5 mM	0.485 ml	2.426 ml	4.851 ml
10 mM	0.243 ml	1.213 ml	2.426 ml
5 mM	0.049 ml	0.243 ml	0.485 ml

Last Update：2024-01-02 23:10:35

G-1 - In vitro study

G-1 is a nonsteroidal, high-affinity and selective agonist of GPR30 with a K I of 11 nM. Treatment with G-1 (10 μM and 100 μM) for 48 and 72 h significantly decreases cell proliferation (P<0.001). At 72 h, the IC 50 value for G-1 is calculated to be 20 μM. Treatment of A549 cells with G-1 at a concentration of 20 μM reveals a significant increase in apoptosis, consistent with its antiproliferative effect (P<0.001). Cell cycle analysis of H295R cells after 24 h of G-1 treatment demonstrates a cell cycle arrest in the G 2 phase. The presence of G-1 increases Bax expression while decreases Bcl-2.

Last Update：2024-04-10 22:29:15

G-1 - In vivo studies

The results at 14 days post-injury show that the Basso mouse scale (BMS) scores are significantly higher in the G-1 group compared with the other groups (P<0.05). The number of caspase-3-positive cells in the cross sections is counted, and G-1 group has fewer positive cells compare with the other groups (P<0.05), and there is no difference between the two groups (P>0.05). G-1 administration produces a statistically significant decrease in tumor volume from day 14 post treatment. Grafted tumors harvested after three-week treatment with G-1 show a significant decrease in tumor weight compare to vehicle treated animals.

Last Update：2024-04-10 22:29:15