A GnRH receptor antagonist
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AG-045572

Item No. 42244

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
5-[(5,6,7,8-tetrahydro-3,5,5,8,8-pentamethyl-2-naphthalenyl)methyl]-N-(2,4,6-trimethoxyphenyl)-2-furancarboxamide
CAS Number
263847-55-8
Molecular Formula
C30H37NO5
Formula Weight
491.6
Purity
≥98%
Formulation
A solid
Solubility(Learn about Variance in Solubility)
DMSO: Soluble: ≥10 mg/mlEthanol: Soluble: ≥10 mg/ml
SMILES
CC1(CCC(C)(C2=CC(C)=C(CC3=CC=C(C(NC4=C(OC)C=C(OC)C=C4OC)=O)O3)C=C12)C)C
InChi Code
InChI=1S/C30H37NO5/c1-18-13-22-23(30(4,5)12-11-29(22,2)3)15-19(18)14-20-9-10-24(36-20)28(32)31-27-25(34-7)16-21(33-6)17-26(27)35-8/h9-10,13,15-17H,11-12,14H2,1-8H3,(H,31,32)
InChi Key
IPEMCIBPDYCJLO-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $43

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    5 mg

    $194

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    10 mg

    $344

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    50 mg

    $752

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    Product Description

    AG-045572 is a nonpeptide antagonist of the gonadotropin-releasing hormone (GnRH) receptor (Kis = 6, 2.2, and 3.8 nM for the human, mouse, and rat receptors, respectively).1 It is selective for the GnRH receptor over a panel of 43 receptors, ion channels, and enzymes at 1 µM. AG-045572 prevents GnRH-induced increases in inositol phosphate production in HEK293 cells expressing the human GnRH receptor (KB = 25 nM). Oral or intravenous administration of AG-045572 decreases plasma luteinizing hormone (LH) levels in castrated rats. It inhibits GnRH-A-induced increases in plasma LH and testosterone levels in non-castrated rats when administered at a dose of 20 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Anderes, K.L., Luthin, D.R., Castillo, R., et al. Biological characterization of a novel, orally active small molecule gonadotropin-releasing hormone (GnRH) antagonist using castrated and intact rats. J. Pharmacol. Exp. Ther. 305(2), 688-695 (2003).