1173435-64-7

• 常用中文名：BMS-665053
• 常用英文名：BMS-665053
• CAS号：1173435-64-7
• 分子式：C₁₆H₁₄Cl₃F₂N₃O₂
• 分子量：424.65700
• 相关类别： 信号通路 G 蛋白偶联受体/G 蛋白 CRFR
• 发布时间：2017-10-04 18:50:38
• 更新时间：2024-01-05 19:43:07
• BMS-665053 是一种促肾上腺皮质激素释放因子 1 (CRF1) 受体拮抗剂 (IC50 = 1.0 nM)。 BMS-665053)11 是人 Y-79 视网膜母细胞瘤细胞中 CRF 刺激的环磷酸腺苷 (cAMP) 产生的有效抑制剂 (IC50 = 4.9 nM)[1]。

名称

• 英文名: 5-Chloro-1-[(1S)-1-cyclopropylethyl]-3-{[2,6-dichloro-4-(difluoro methoxy)phenyl]amino}-2(1H)-pyrazinone
• 英文别名: 1-Boc-D-Pyroglutamic acid ethyl ester; Ethyl Boc-D-pyroglutamate; Ethyl N-Boc-D-pyroglutamate

物化性质

• 分子式: C₁₆H₁₄Cl₃F₂N₃O₂
• 分子量: 424.65700
• 精确质量: 423.01200
• PSA: 59.38000
• LogP: 4.94140

生物活性

• 描述: BMS-665053 是一种促肾上腺皮质激素释放因子 1 (CRF1) 受体拮抗剂 (IC50 = 1.0 nM)。 BMS-665053)11 是人 Y-79 视网膜母细胞瘤细胞中 CRF 刺激的环磷酸腺苷 (cAMP) 产生的有效抑制剂 (IC50 = 4.9 nM)[1]。
• 相关类别:
  信号通路 >> G 蛋白偶联受体/G 蛋白 >> CRFR
  研究领域 >> 神经疾病
• 参考文献:

  [1]. Jianqing Li, et al. An Efficient, Direct Bis-ortho-chlorination of 4-(Difluoromethoxy)aniline and Its Application to the Synthesis of BMS-665053, a Potent and Selective Pyrazinone-Containing Corticotropin-Releasing Factor-1 Receptor Antagonist. Organic Process Research & Development, 16, 156-159.

合成路线

1173434-71-3 ~% 1173435-64-7

文献：Li, Jianqing; Smith, Daniel; Krishnananthan, Subramaniam; Hartz, Richard A.; Dasgupta, Bireshwar; Ahuja, Vijay; Schmitz, William D.; Bronson, Joanne J.; Mathur, Arvind; Barrish, Joel C.; Chen, Bang-Chi Organic Process Research and Development, 2012 , vol. 16, # 1 p. 156 - 159

1173434-78-0 ~% 1173435-64-7

文献：Li, Jianqing; Smith, Daniel; Krishnananthan, Subramaniam; Hartz, Richard A.; Dasgupta, Bireshwar; Ahuja, Vijay; Schmitz, William D.; Bronson, Joanne J.; Mathur, Arvind; Barrish, Joel C.; Chen, Bang-Chi Organic Process Research and Development, 2012 , vol. 16, # 1 p. 156 - 159

591-35-5 ~% 1173435-64-7

文献：Li, Jianqing; Smith, Daniel; Krishnananthan, Subramaniam; Hartz, Richard A.; Dasgupta, Bireshwar; Ahuja, Vijay; Schmitz, William D.; Bronson, Joanne J.; Mathur, Arvind; Barrish, Joel C.; Chen, Bang-Chi Organic Process Research and Development, 2012 , vol. 16, # 1 p. 156 - 159

22236-10-8 ~% 1173435-64-7

文献：Li, Jianqing; Smith, Daniel; Krishnananthan, Subramaniam; Hartz, Richard A.; Dasgupta, Bireshwar; Ahuja, Vijay; Schmitz, William D.; Bronson, Joanne J.; Mathur, Arvind; Barrish, Joel C.; Chen, Bang-Chi Organic Process Research and Development, 2012 , vol. 16, # 1 p. 156 - 159

50590-08-4 ~% 1173435-64-7

文献：Li, Jianqing; Smith, Daniel; Krishnananthan, Subramaniam; Hartz, Richard A.; Dasgupta, Bireshwar; Ahuja, Vijay; Schmitz, William D.; Bronson, Joanne J.; Mathur, Arvind; Barrish, Joel C.; Chen, Bang-Chi Organic Process Research and Development, 2012 , vol. 16, # 1 p. 156 - 159

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