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G-15 (CAS 1161002-05-6) LS-H105

GPER antagonist
LS-H105-1 / 1 mg / $195
LS-H105-5 / 5 mg / $225
LS-H105-10 / 10 mg / $265
LS-H105-25 / 25 mg / $375
USA Shipment Only
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Description: G protein-coupled estrogen receptor (GPER), or GPR30, specifically binds natural and man-made estrogens. It is thought to be involved in estrogen-sensitive cancers. GPER knockout mice are fertile, although they exhibit thymic atrophy, impaired glucose tolerance, and altered bone growth. G-15 is a cell-permeable non-steroidal antagonist of GPER (Ki = 20 nM). It displays low affinity cross-reactivity with the classical estrogen receptor (ER), ER alpha, so that at doses greater than 1 µM it is capable of mediating limited ER-dependent transcriptional activity. G-15 antagonizes the anti-depressive effects of estrogen in vivo. H105_ChemicalStructureImage.png
(3aS,4R,9bR)-4-(6-bromo-1,3-benzodioxol-5-yl)-3a,4,5,9b-tetrahydro-3H-cyclopenta[c]quinoline
 
biochemical, chemical, antagonist
LS-H105
1161002-05-6
C19H16BrNO2
≥95%
A crystalline solid
 
BrC1=CC2=C(OCO2)C=C1[C@@H]3NC(C=CC=C4)=C4[C@@]5([H])[C@]3([H])CC=C5
InChI=1S/C19H16BrNO2/c20-15-9-18-17(22-10-23-18)8-14(15)19-13-6-3-5-11(13)12-4-1-2-7-16(12)21-19/h1-5,7-9,11,13,19,21H,6,10H2/t11-,13-,19+/m0/s1
YOLTZIVRJAPVPH-MJLGCCKJSA-N
Shipped Ambient, store at -20°C, ≥ 2 years shelf life.
This product is for research use only. Not for administration to humans, or for human or veterinary diagnostic or therapeutic use.
Data Sheet DataSheet    SDS SDS
Related Products: GPER1 / GPR30 related products

Usage Information

G-15 is supplied as a crystalline solid. A stock solution may be made by dissolving the G-15 in the solvent of choice. G-15 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF), which should be purged with an inert gas. The solubility of G-15 in these solvents is approximately 1, 20, and 30 mg/ml, respectively. G-15 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, G-15 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. G-15 has a solubility of approximately 0.5 mg/ml in a 1:1 solution of DMF:PBS (pH 7.2) using this method. We do not recommend storing the aqueous solution for more than one day.

References:
  1. Filardo, E.J. and Thomas, P. Minireview: G protein-coupled estrogen receptor-1, GPER-1: Its mechanism of action and role in female reproductive cancer, renal and vascular physiology. Endocrinology 153(7), 2953-2962 (2012).
  2. Chevalier, N., Vega, A., Bouskine, A., et al. GPR30, the non-classical membrane G protein related estrogen receptor, is overexpressed in human seminoma and promotes seminoma cell proliferation. PLoS One 7(4), 34672 (2012).
  3. Dennis, M.K., Burai, R., Ramesh, C., et al. In vivo effects of a GPR30 antagonist. Nat. Chem. Biol. 5(6), 421-427 (2009).
  4. Dennis, M.K., Field, A.S., Burai, R., et al. Identification of a GPER/GPR30 antagonist with improved estrogen receptor counterselectivity. J. Steroid Biochem. Mol. Biol. 127(3-5), 358-366 (2011).

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