808756-71-0

• 常用中文名：N-(5-叔丁基茚满-1-基)-N-(1H-吲唑-4-基)脲
• 常用英文名：ABT-102
• CAS号：808756-71-0
• 分子式：C₂₁H₂₄N₄O
• 分子量：348.44
• 相关类别： 信号通路 跨膜转运 TRP频道
• 发布时间：2019-01-12 17:17:41
• 更新时间：2025-08-25 15:26:19
• ABT-102 是一种有效且高度选择性的 Vanilloid Receptor (TRPV1) 受体拮抗剂。ABT-102 有效且可逆地增加热痛阈值并减少阈上口腔/皮肤热痛。ABT-102 可减少炎症、骨癌、术后和骨关节炎疼痛模型中动物的伤害性反应。

名称

• 中文名: N-(5-叔丁基茚满-1-基)-N-(1H-吲唑-4-基)脲
• 英文名: 1-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-3-(1H-indazol-4-yl)urea
• 中文别名: N-(5-叔丁基茚满-1-基)-N'-(1H-吲唑-4-基)脲
• 英文别名: N-[(1R)-5-tert-butyl-2,3-dihydro-1H-inden-1-yl]-N'-1H-indazol-4-ylurea; (R)-1-(5-tert-butylindan-1-yl)-3-(1H-indazol-4-yl); ABT-102

物化性质

• 密度: 1.24 g/cm3
• 沸点: 529.5ºC at 760 mmHg
• 分子式: C₂₁H₂₄N₄O
• 分子量: 348.44
• 闪点: 274.1ºC
• 精确质量: 348.19500
• PSA: 69.81000
• LogP: 5.13330
• 储存条件: 2-8°C

生物活性

• 描述: ABT-102 是一种有效且高度选择性的 Vanilloid Receptor (TRPV1) 受体拮抗剂。ABT-102 有效且可逆地增加热痛阈值并减少阈上口腔/皮肤热痛。ABT-102 可减少炎症、骨癌、术后和骨关节炎疼痛模型中动物的伤害性反应。
• 相关类别:
  信号通路 >> 跨膜转运 >> TRP频道
  研究领域 >> 癌症
  研究领域 >> 炎症/免疫
• 靶点:

  TRPV1

• 参考文献:

  [1]. Lukin K, et al. Development of a Large Scale Asymmetric Synthesis of Vanilloid Receptor (TRPV1) Antagonist ABT-102. Organic Process Research & Development, 2007, 11(3):578-584.

  [2]. Rowbotham MC, et al. Oral and cutaneous thermosensory profile of selective TRPV1 inhibition by ABT-102 in a randomized healthy volunteer trial. Pain. 2011 May;152(5):1192-1200.

合成路线

952734-48-4 ~% 808756-71-0

文献：Lukin, Kirill A.; Hsu, Margaret Chi-Ping; Fernando, Dilinie P.; Kotecki, Brian J.; Leanna, Marvin R. Patent: US2007/244178 A1, 2007 ; Location in patent: Page/Page column 14 ;

808756-69-6 ~% 808756-71-0

文献：Gomtsyan, Arthur; Bayburt, Erol K.; Schmidt, Robert G.; Surowy, Carol S.; Honore, Prisca; Marsh, Kennan C.; Hannick, Steven M.; McDonald, Heath A.; Wetter, Jill M.; Sullivan, James P.; Jarvis, Michael F.; Faltynek, Connie R.; Lee, Chih-Hung Journal of Medicinal Chemistry, 2008 , vol. 51, # 3 p. 392 - 395

253185-03-4 ~% 808756-71-0

文献：Lukin, Kirill; Hsu, Margaret C.; Chambournier, Gilles; Kotecki, Brian; Venkatramani; Leanna Organic Process Research and Development, 2007 , vol. 11, # 3 p. 578 - 584

28547-33-3 ~% 808756-71-0

文献：Lukin, Kirill; Hsu, Margaret C.; Chambournier, Gilles; Kotecki, Brian; Venkatramani; Leanna Organic Process Research and Development, 2007 , vol. 11, # 3 p. 578 - 584

4600-86-6 ~% 808756-71-0

文献：Lukin, Kirill; Hsu, Margaret C.; Chambournier, Gilles; Kotecki, Brian; Venkatramani; Leanna Organic Process Research and Development, 2007 , vol. 11, # 3 p. 578 - 584

935680-90-3 ~% 808756-71-0

文献：Lukin, Kirill; Hsu, Margaret C.; Chambournier, Gilles; Kotecki, Brian; Venkatramani; Leanna Organic Process Research and Development, 2007 , vol. 11, # 3 p. 578 - 584

735330-50-4 934593-36-9 ~% 808756-71-0

文献：Lukin, Kirill; Hsu, Margaret C.; Chambournier, Gilles; Kotecki, Brian; Venkatramani; Leanna Organic Process Research and Development, 2007 , vol. 11, # 3 p. 578 - 584

上下游产品

上游产品  6
808756-69-6 28547-33-3 4600-86-6 935680-90-3
735330-50-4 934593-36-9
下游产品  0