产品
编 号：F756200
分子式：C31H28F5N7O6S
分子量：721.65
分子式：C31H28F5N7O6S
分子量：721.65
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CAS No: 2826273-90-7
产品详情
生物活性：
GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing.
体内研究：
GnRH-R antagonist 1 (30 mg/kg; p.o.; single daily for 7 days) has a good safety profile for oral administration.GnRH-R antagonist 1 (12 mg/kg; p.o.; single) shows favorable pharmacokinetic properties and high oral bioavailability with a F% value of 44.7%.GnRH-R antagonist 1 (12 mg/kg; p.o.; single) inhibits circulating testosterone levels in rats (lasts for more than 24 h).Animal Model:Adult Sprague-Dawley rats (200-250 g).
Dosage:30 mg/kg
Administration:Oral administration; single daily for 7 days.
Result:Showed no ames toxicity.
Animal Model:Adult Sprague-Dawley rats (200-250 g).
Dosage:1 mg/kg (for i.v.); 12 mg/kg (for p.o.)
Administration:Intravenous administration ;oral administration; single.
Result:Exhibited clear and significnt suppressive effects on circulating testosterone levels in rats, and the suppressive effects lasted for more than 24 h.1.19Pharmacokinetic Parameters of GnRH-R antagonist 1 in Adult Sprague-Dawley rats.IV (1 mg/kg) PO (12 mg/kg)
Tmax (h)-1.13
Cmax (nmol/L)3918.8920.1
AUCLast (nmol/L?h)1374.67370.6
CL (L/h/kg)1.05-
t1/2 (h)2.794.86
F (%)-44.7
体外研究：
GnRH-R antagonist 1 has a 140-fold higher cell permeability than Relugolix and exhibits favorable stability in human and mouse microsome.
GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeable GnRH-R antagonist with high binding affinity (IC50=0.57 nM) and potent in vitro antagonistic activity (IC50=2.18 nM). GnRH-R antagonist 1 can be used in studies of advanced prostate cancer and premature LH peaks preventing.
体内研究：
GnRH-R antagonist 1 (30 mg/kg; p.o.; single daily for 7 days) has a good safety profile for oral administration.GnRH-R antagonist 1 (12 mg/kg; p.o.; single) shows favorable pharmacokinetic properties and high oral bioavailability with a F% value of 44.7%.GnRH-R antagonist 1 (12 mg/kg; p.o.; single) inhibits circulating testosterone levels in rats (lasts for more than 24 h).Animal Model:Adult Sprague-Dawley rats (200-250 g).
Dosage:30 mg/kg
Administration:Oral administration; single daily for 7 days.
Result:Showed no ames toxicity.
Animal Model:Adult Sprague-Dawley rats (200-250 g).
Dosage:1 mg/kg (for i.v.); 12 mg/kg (for p.o.)
Administration:Intravenous administration ;oral administration; single.
Result:Exhibited clear and significnt suppressive effects on circulating testosterone levels in rats, and the suppressive effects lasted for more than 24 h.1.19Pharmacokinetic Parameters of GnRH-R antagonist 1 in Adult Sprague-Dawley rats.IV (1 mg/kg) PO (12 mg/kg)
Tmax (h)-1.13
Cmax (nmol/L)3918.8920.1
AUCLast (nmol/L?h)1374.67370.6
CL (L/h/kg)1.05-
t1/2 (h)2.794.86
F (%)-44.7
体外研究：
GnRH-R antagonist 1 has a 140-fold higher cell permeability than Relugolix and exhibits favorable stability in human and mouse microsome.
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