Catalog No.S4896 Synonyms: NBI-56418, ABT-620
Molecular Weight(MW): 653.57
Elagolix Soidum is a potent, selective, orally active, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with Kd value of 54 pM. Concentration at 10 μM shows no significant activity on ion channels, enzymes, and transporters (inhibition <50%).
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|Description||Elagolix Soidum is a potent, selective, orally active, non-peptide antagonist of the gonadotropin-releasing hormone receptor (GnRHR) with Kd value of 54 pM. Concentration at 10 μM shows no significant activity on ion channels, enzymes, and transporters (inhibition <50%).|
Elagolix displays high affinity in a competition binding assay for hGnRH-R (Ki = 0.90 nM) and low CYP3A4 inhibition (IC50 = 56 μM). It is a slowly disassociating antagonist exhibiting very high affinity (KD = 54 pM) and insurmountable antagonism. Elagolix is highly selective at hGnRH-R, its wider receptor selectivity is tested at a concentration of 10 μM in a panel of radioligand binding assays for 100 off-target receptors, ion channels, enzymes, and transporters, and significant activity is not observed (inhibition <50%). It does not stimulate histamine release from cultured rat peritoneal mast cells. Elagolix lacks the necessary high binding affinity to the rat GnRH receptor (Ki = 4400 nM) and it possesses high affinity at the monkey GnRH receptor (Ki = 3.3 nM).
|In vivo||Oral administration of Elagolix suppresses luteinizing hormone in castrated macaques. Elagolix shows good efficacy in suppressing luteinizing hormone in monkeys and exhibits high oral bioavailability in dogs (~100% when dosed via oral gavage at 50 mg/kg).|
|In vitro||DMSO||100 mg/mL (153.0 mM)|
|Water||100 mg/mL (153.0 mM)|
|Ethanol||100 mg/mL (153.0 mM)|
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