G-1

Cayman Chemical Item Number 10008933

(CAS 881639-98-1)

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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.

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%
λmax 210, 242, 329 nm
Stability 2 years
Storage -20°C
Shipping Room temperature in continental US; may vary elsewhere
SMILES
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CC(C1=CC([C@@]​(C=CC2)​([H]​)​[C@@]​2([H]​)​[C@H]​(C3=CC(OCO4)​=C4C=C3Br)​N5)​=C5C=C1)​=O
InCHI Code
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​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
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VHSVKVWHYFBIFJ-HKZYLEAXSA-N

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G-1 is available in the following screening library:

Size Price Quantity Subtotal
1 mg $25.00 $0.00
5 mg $94.00 $0.00
10 mg $150.00 $0.00
25 mg $344.00 $0.00
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Cart Total $0.00

Pricing updated 2015-07-02. Prices are subject to change without notice.

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Warning This product is not for human or veterinary use.

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Cayman Chemical was formed over thirty years ago by demonstrating the value of naturally growing gorgonian corals as a renewable, economically viable source of prostaglandins. Today we operate our business knowing that we owe our start to the renewable resources our environment had provided. As Cayman Chemical continues to grow we consistently evaluate our business processes to ensure we are operating at the highest environmental standards.

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Ann Arbor, Michigan 48108 USA

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