2. GPCR/G Protein
  3. GnRH Receptor
  4. GnRH-R antagonist 1

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。

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GnRH-R antagonist 1 Chemical Structure

GnRH-R antagonist 1 Chemical Structure

CAS No. : 2826273-90-7

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GnRH-R antagonist 1 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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[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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

GnRH-R antagonist 1 相关抗体:
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.
1.19 Pharmacokinetic 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/L•h) 1374.6 7370.6
CL (L/h/kg) 1.05 -
t1/2 (h) 2.79 4.86
F (%) - 44.7
分子量

721.65

Formula

C31H28F5N7O6S
CAS 号
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.
纯度 & 产品资料
参考文献

GnRH-R antagonist 1 相关分类

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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GnRH-R antagonist 12826273-90-7GnRH ReceptorGonadotropin releasing hormone receptorGNRHRpremature LH peaksCaco-2 cellsrelugolixadvanced prostate cancerInhibitorinhibitorinhibit

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