Item № 10008933
CAS № 881639-98-1
Purity ≥98%
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1 mg $25.00 $0.00
5 mg $94.00 $0.00
10 mg $150.00 $0.00
25 mg $344.00 $0.00

Pricing updated 2016-02-06. Prices are subject to change without notice.

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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.1 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 α- (ERα-) and ERβ-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.2 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.

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Technical Information
Formal Name rel-1-[4-(6-bromo-1,3-benzodioxol-5-yl)-3aR,4S,5,9bS-tetrahydro-3H-cyclopenta[c]quinolin-8-yl]-ethanone
CAS Number 881639-98-1
Molecular Formula C21H18BrNO3
Formula Weight 412.3
Purity ≥98%
Formulation A crystalline solid
λmax 210, 242, 329 nm
SMILES CC(C1=CC([C@@](C=CC2)([H])[C@@]2([H])[C@H](C3=CC(OCO4)=C4C=C3Br)N5)=C5C=C1)=O
InChI Code 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

WARNING - This product is not for human or veterinary use.

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Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
Stability 2 years
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References & Background Reading
Product Description References

1. Revankar, 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. Nat Chem Biol 2(4) 207-212 (2006).

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