GnRH-R antagonist 1 (化合物 21a) 是一种具有良好口服安全性和膜渗透性的GnRH-R拮抗剂，对GnRH-R有高结合亲和力 (IC50=0.57 nM) 和有效的体外拮抗活性 (IC50=2.18 nM)。GnRH-R antagonist 1 可用于晚期前列腺癌和预防过早 LH 高峰的研究。
| 生物活性 | GnRH-R antagonist 1 (compound 21a) is an orally safe and membrane-permeableGnRH-Rantagonist 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 prostatecancerand premature LH peaks preventing[1]. |
体外研究
(In Vitro) | GnRH-R antagonist 1 has a 140-fold higher cell permeability than Relugolix and exhibits favorable stability in human and mouse microsome[1].
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体内研究
(In Vivo) | GnRH-R antagonist 1 (30 mg/kg; p.o.; single daily for 7 days) has a good safety profile for oral administration[1].
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%[1].
GnRH-R antagonist 1 (12 mg/kg; p.o.; single) inhibits circulating testosterone levels in rats (lasts for more than 24 h)[1].
| Animal Model: | Adult Sprague-Dawley rats (200-250 g)[1]. | | 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)[1]. | | 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[1].
| IV (1 mg/kg) | PO (12 mg/kg) | | Tmax(h) | - | 1.13 | | Cmax(nmol/L) | 3918.8 | 920.1 | | AUCLast(nmol/Loh) | 1374.6 | 7370.6 | | CL (L/h/kg) | 1.05 | - | | t1/2(h) | 2.79 | 4.86 | | F (%) | - | 44.7 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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