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G-1

Cayman Chemical Item Number 10008933

(CAS 881639-98-1)

G-1 (CAS 881639-98-1)

See more	Receptor Biochemistry (59) Steroids (37) Endocrinology (335)

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 K_i value of 11 nM. Competitive binding studies in ERα- and ERβ-expressing cells yielded K_i 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.

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).

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
Formulation	A crystalline solid
Purity	≥98%
λ_max	210, 242, 329 nm
Stability	2 years
Storage	-20°C
Shipping	Room temperature in continental US; may vary elsewhere
SMILES	Copy SMILES to clipboard CC(C1=CC([C@@](C=CC2)([H])[C@@]2([H])[C@H](C3=CC(OCO4)=C4C=C3Br)N5)=C5C=C1)=O

Background Reading

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).

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).

G-1 is available in the following screening library:

Bio-active Lipid I Screening Library (96-Well)

Size	Price	Quantity	Subtotal
1 mg	$17.00		$0.00
5 mg	$77.00		$0.00
10 mg	$136.00		$0.00
50 mg	$595.00		$0.00
Bulk	Contact
		Cart Total	$0.00

Pricing updated 2012-02-12. Prices are subject to change without notice.

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G-1