产品
编 号：F332637
分子式：C27H24F3N3O3
分子量：495.49
分子式：C27H24F3N3O3
分子量：495.49
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价格
是否有货
10mM*1mL in DMSO
询价
询价
1mg
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5mg
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10mg
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结构图
CAS No: 352290-60-9
产品详情
生物活性：
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases.
体内研究：
NBI-42902 (10-100 mg/kg，口服或静脉注射) 显著抑制阉割猕猴的血清 LH 水平。Animal Model:Castrated macaques
Dosage:10, 40, 100 mg/kg
Administration:Oral administration (p.o.)
Result:Inhibited serum LH with dose dependent.Inhibited serum LH achieved maximum suppression, that was 62-68% of pretreatment baseline, at 4-8 h after administration.Exhibited no suppression of LH levels after 24 h treated with 10 or 40 mg/kg, but remained suppression at 100 mg/kg.
Animal Model:Castrated macaques
Dosage:10 mg/kg
Administration:Intravenous injection (i.v.)
Result:Inhibited serum LH achieved maximum suppression was 62-68% of pretreatment baseline between 4-8 h after administration, but exhibited no suppression after 24 h.
体外研究：
NBI-42902 (0-1000 nM) 对物种之间保守序列的变化非常敏感，抑制 GnRH 受体的 IC50 值分别为 0.79 nM (人)， 10 nM (猕猴)， 400 nM (狗) 和 200 nM (兔)。NBI-42902 (1 nM-1 μM， 1 分钟) 在 RBL 细胞中抑制 GnRH (4 nM) 诱导的 Ca2+ 通量，平均 IC50 值为 3.6 nM。NBI-42902 (1 nM-1 μM， 1 分钟) 在 RBL 细胞中竞争性抑制 GnRH (4 nM) 诱导的 IP 积累。NBI-42902 (1 nM-1 μM， 5 分钟) 完全阻断 CHO-GnRHR 细胞中 GnRH 刺激的 ERK1/2 磷酸化，IC50 值为 5.22 nM。
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79 nM, a Ki value of 0.56 nM, respectively. NBI-42902 inhibits GnRH-stimulated inositol phosphate (IP) accumulation, Ca2+ flux, and ERK1/2 activation. NBI-42902 inhibits serum luteinizing hormone (LH) in castrated male macaques. NBI-42902 can be used for research on sex-hormone-related diseases.
体内研究：
NBI-42902 (10-100 mg/kg，口服或静脉注射) 显著抑制阉割猕猴的血清 LH 水平。Animal Model:Castrated macaques
Dosage:10, 40, 100 mg/kg
Administration:Oral administration (p.o.)
Result:Inhibited serum LH with dose dependent.Inhibited serum LH achieved maximum suppression, that was 62-68% of pretreatment baseline, at 4-8 h after administration.Exhibited no suppression of LH levels after 24 h treated with 10 or 40 mg/kg, but remained suppression at 100 mg/kg.
Animal Model:Castrated macaques
Dosage:10 mg/kg
Administration:Intravenous injection (i.v.)
Result:Inhibited serum LH achieved maximum suppression was 62-68% of pretreatment baseline between 4-8 h after administration, but exhibited no suppression after 24 h.
体外研究：
NBI-42902 (0-1000 nM) 对物种之间保守序列的变化非常敏感，抑制 GnRH 受体的 IC50 值分别为 0.79 nM (人)， 10 nM (猕猴)， 400 nM (狗) 和 200 nM (兔)。NBI-42902 (1 nM-1 μM， 1 分钟) 在 RBL 细胞中抑制 GnRH (4 nM) 诱导的 Ca2+ 通量，平均 IC50 值为 3.6 nM。NBI-42902 (1 nM-1 μM， 1 分钟) 在 RBL 细胞中竞争性抑制 GnRH (4 nM) 诱导的 IP 积累。NBI-42902 (1 nM-1 μM， 5 分钟) 完全阻断 CHO-GnRHR 细胞中 GnRH 刺激的 ERK1/2 磷酸化，IC50 值为 5.22 nM。
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