产品介绍
Product Description
Biochem/physiol Actions
Orally active human gonadotropin releasing hormone (GnRH)/luteinizing hormone releasing hormone (LHRH) receptor (GnRHR, LHRHR) antagonist.
Elagolix is an orally active, potent, high-affinity human gonadotropin-releasing hormone (GnRH)/luteinizing hormone-releasing hormone (LH-RH) receptor (GnRHR, LHRHR) antagonist (Ki = 0.9 nM/human, 3.3 nM/monkey, 4.4 µM/rat) that effectively blocks GnRH-induced inositol phosphate production in RBL-1 hGnRH-R transfectants (IC50 = 1.5 nM against 6 nM GnRH). Oral administration in castrated male cynomolgus macaques effectively reduces circulating LH in a reversible manner in vivo (75% reduction 8h post 30 mg/kg p.o.).
Disclaimer
Hygroscopic
技术参数
Specifications
| Quality Level | 100 |
| assay | ≥98% (HPLC) |
| form | powder |
| storage condition | desiccated |
| color | white to beige |
| solubility | H2O: 2 mg/mL, clear |
| storage temp. | -10 to -25°C |
| SMILES string | CC1=C(C2=C(C(OC)=CC=C2)F)C(N(C(N1CC3=C(C=CC=C3F)C(F)(F)F)=O)C[C@@H](C4=CC=CC=C4)NCCCC(O[Na])=O)=O |
