| Chemical Properties | Back Directory | [density ]
1.60±0.1 g/cm3(Predicted) | [storage temp. ]
2-8°C | [solubility ]
DMSO: 2mg/mL, clear | [form ]
powder | [pka]
12.47±0.40(Predicted) | [color ]
white to beige | [Optical Rotation]
[α]/D -120 to -100°, c =0.5 in chloroform-d |
| Hazard Information | Back Directory | [Uses]
BAY-784 is a gonadotropin releasing hormone receptor (GnRH-R) antagonist probe with IC50s of 21 and 24 nM for human and rat GnRH-R, respectively[1]. | [Biological Activity]
BAY-784 is an orally availablenon-toxicpotentand selective antagonist of human Gonadotropin-Releasing Hormone Receptor [hGnRH-R]which is potently active in other species including ratedogs and cynomolgus monkey. It partially lowered plasma luteinizing hormone levels in humans. BAY-784 exhibits favorable drug metabolism and pharmacokinetic (DMPK) profile thus is suitable for in vivo studies. | [in vivo]
BAY-784 (0.5, 3, 10, and 30 mg/kg; 24 hours; single p.o.) suppresses the plasma luteinizing hormone (LH) concentration in ovariectomized (OVX) rats in a dose-dependent manner[1]. | Animal Model: | OVX rats[1] | | Dosage: | 0.5, 3, 10, and 30 mg/kg (Pharmacokinetic Analysis) | | Administration: | Single p.o. | | Result: | ED50=4.5 mg/kg (4/8 h).
The t1/2=13-17 h, 18 h, and 7 h for male Wistar rat, female beagle, and female cynomolgus, respectively. |
| [References]
[1] GnRH-R Antagonist Probe BAY-784. |
|
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
|