G-1
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 2015-09-02. Prices are subject to change without notice.

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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.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
InChI Key VHSVKVWHYFBIFJ-HKZYLEAXSA-N

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

Shipping & Storage
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
Stability 2 years
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Additional Information

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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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