| Bioactivity | 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[1]. |
| Invitro | 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)[1]。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[1]。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[1]。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[1]。 Western Blot Analysis[1] Cell Line: |
| In Vivo | 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[1]。 Animal Model: |
| Name | NBI-42902 |
| CAS | 352290-60-9 |
| Formula | C27H24F3N3O3 |
| Molar Mass | 495.49 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Struthers RS, et al. Pharmacological characterization of a novel nonpeptide antagonist of the human gonadotropin-releasing hormone receptor, NBI-42902. Endocrinology. 2007 Feb;148(2):857-67. |
NBI-42902
CAS: 352290-60-9 F: C27H24F3N3O3 W: 495.49
NBI-42902 is an orally active, potent functional and competitive antagonist of GnRH receptor with an IC50 value of 0.79
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