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G-1 (CAS 881639-98-1) LS-H26

GPR30 agonist
LS-H26-1 / 1 mg / $175
LS-H26-5 / 5 mg / $225
LS-H26-10 / 10 mg / $265
LS-H26-25 / 25 mg / $405
USA Shipment Only
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Description: GPR30 is a transmembrane G protein-coupled receptor (GPCR) localized to endoplasmic reticulum (ER) that binds estradiol with high affinity, activating multiple intracellular signaling pathways. G-1 is a nonsteroidal, high-affinity, selective agonist of GPR30 that binds with a Ki value of 11 nM. Competitive binding studies in endoplasmic reticulum alpha - (ER alpha -) and ER beta -expressing cells yielded Ki values for estradiol of 0.30 and 0.38 nM, respectively, with no substantial binding of G-1 at 1 µM. The discovery of G-1, a compound that does not bind classical ERs, should facilitate further physiological experiments to define the role of GPR30 in vivo. H26_ChemicalStructureImage.png
rel-1-[4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4S,5,9bS-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone
 
biochemical, chemical, agonist
LS-H26
881639-98-1
C21H18BrNO3
≥98%
A crystalline solid
 
CC(C1=CC([C@@](C=CC2)([H])[C@@]2([H])[C@H](C3=CC(OCO4)=C4C=C3Br)N5)=C5C=C1)=O
InChI=1S/C21H18BrNO3/c1-11(24)12-5-6-18-15(7-12)13-3-2-4-14(13)21(23-18)16-8-19-20(9-17(16)22)26-10-25-19/h2-3,5-9,13-14,21,23H,4,10H2,1H3/t13-,14+,21-/m1/s1
VHSVKVWHYFBIFJ-HKZYLEAXSA-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-1 is supplied as a crystalline solid. A stock solution may be made by dissolving the G-1 in an organic solvent purged with an inert gas. G-1 is soluble in organic solvents such as ethanol, DMSO, and dimethyl formamide (DMF). The solubility of G-1 in these solvents is approximately 1, 20, and 30 mg/ml, respectively. G-1 is sparingly soluble in aqueous buffers. For maximum solubility in aqueous buffers, G-1 should first be dissolved in DMF and then diluted with the aqueous buffer of choice. G-1 has a solubility of approximately 0.15 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. Revandar, C.M., Cimino, D.F., Sklar, L.A., et al. A transmembrane intracellular estrogen receptor mediates rapid cell signaling. Science 307, 1625-1630 (2005).
  2. Bologa, C.G., Revankar, C.M., Young, S.M., et al. Virtual and biomolecular screening converge on a selective agonist for GPR30. Nature Chemical Biology 2(4), 207-212 (2006).

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