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GPR30 agonist G-1

Chemical Structure : GPR30 agonist G-1

CAS No.: 881639-98-1

GPR30 agonist G-1 (Tespria)

Catalog No.: PC-60270Not For Human Use, Lab Use Only.

GPER/GPR30 agonist G-1 (Tespria) is potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

GPER/GPR30 agonist G-1 (Tespria) is potent and selective GPER/GPR30 agonist with Ki of 11 nM, EC50 of 2 nM.
GPER/GPR30 agonist G-1 displays no activity at ERα and ERβ at concentrations up to 10 uM.
GPER/GPR30 agonist G-1 increases cytosolic Ca2+ and inhibits migration of SKBr3 cells and MCF-7 cells in response to chemoattractants with IC50 of 0.7 and 1.6 nM respectively.
GPER/GPR30 agonist G-1 induces cell cycle arrest, DNA damage and cell death by the activation of the intrinsic apoptotic mechanism in H295R cells.

Physicochemical Properties

M.Wt 412.28
Formula C21H18BrNO3
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(±)-1-[(3aR*,4S*,9bS*)-4-(6-Bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]- ethanone

References

1. Wang C, et al. Mol Endocrinol. 2008 Mar;22(3):636-48.

2. Chimento A, et al. Oncotarget. 2015 Aug 7;6(22):19190-203.

3. Ahola TM, et al. Endocrinology. 2002 Sep;143(9):3376-84.

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