GSK2193874游离态
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- CAS号:
- 1336960-13-4
- 英文名:
- 3-([1,4′-Bipiperidin]-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide
- 英文别名:
- GSK2193874;GSK2193874 >=98% (HPLC);GSK 2193874; GSK2193874;TRPV4 antagonist GS2193874;GSK2193874,inhibit,GSK 2193874,Transient receptor potential channels,GSK-2193874,Inhibitor,TRP Channel;3-([1,4′-Bipiperidin]-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide;3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-(3-(trifluoromethyl)phenyl)quinoline-4-carboxamide;4-Quinolinecarboxamide, 3-([1,4'-bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-
- 中文名:
- GSK2193874游离态
- 中文别名:
- GSK2193874游离态;化合物GSK2193874;GSK 2193874,TRPV4拮抗剂;3-([1,4′-联哌啶]-1′-基甲基)-7-溴-N-(1-苯基环丙基)-2-[3-(三氟甲基)苯基]-4-喹啉甲酰胺;3-([1,4'-联吡啶基]-1'-基甲基)-7-溴-N-(1-苯基环丙基)-2-(3-(三氟甲基)苯基)喹啉-4-甲酰胺
- CBNumber:
- CB62751087
- 分子式:
- C37H38BrF3N4O
- 分子量:
- 691.62
- MOL File:
- 1336960-13-4.mol
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GSK2193874游离态化学性质
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沸点:
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737.8±60.0 °C(Predicted)
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密度:
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1.43±0.1 g/cm3(Predicted)
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储存条件:
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room temp
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溶解度:
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DMSO: soluble10mg/mL, clear
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酸度系数(pKa):
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12.82±0.20(Predicted)
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形态:
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powder
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颜色:
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white to beige
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GSK2193874游离态性质、用途与生产工艺
GSK2193874是一种具有口服活性的、有效的、选择性transient receptor potential vanilloid 4 (TRPV4)阻滞剂,对hTRPV4和rTRPV4的IC50分别为0.04和0.002 μM。
Target | Value |
rTRPV4
(Cell-free assay)
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0.002 μM
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hTRPV4
(Cell-free assay)
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0.04 μM
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GSK2193874拮抗TRP通道,对靶点的抑制作用相对对TRPV1、TRPA1、TRPC3、TRPC6和TRPM8的作用来说更具有选择性。用GSK2193874处理人脐静脉内皮细胞(HUVECs)可浓度依赖性地阻止细胞收缩以及抑制由GSK1016790激活TRPV4所导致的细胞脱离。
在大鼠和犬类中检测GSK2193874的药代动力学,发现在慢性动物模型中,GSK2193874具有适于口服途径的半衰期和其他特性。(在大鼠中:iv CL = 7.3 mL/min/kg, po t1/2 = 10 h, %F =31;在狗中:iv CL = 6.9 mL/min/kg, po t1/2 = 31 h, %F = 53)。除此之外,在大鼠中,当GSK2193874浓度高达30 mg/kg时,对血压或心率没有作用。在一些心衰模型中,GSK2193874能够改善肺功能。在急性和慢性心衰模型中,GSK2193874的预处理可抑制肺水肿的形成并增强动脉氧合。GSK2193874能够维持内皮细胞的完整性、抑制内皮TRPV4电流,在离体肺和心衰模型中保护肺部免于肺水肿形成。
GSK2193874游离态
上下游产品信息
上游原料
下游产品
更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
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2024/04/30 | HY-100720 | GSK2193874游离态 GSK2193874 | 1336960-13-4 | 5mg | 770元 |
2024/04/30 | HY-100720 | GSK2193874游离态 GSK2193874 | 1336960-13-4 | 10mM * 1mLin DMSO | 1172元 |
1336960-13-4, GSK2193874游离态 相关搜索:
- 合成有机化合物配体
- C37H38BrF3N4O
- GSK 2193874,TRPV4拮抗剂
- 3-([1,4'-联吡啶基]-1'-基甲基)-7-溴-N-(1-苯基环丙基)-2-(3-(三氟甲基)苯基)喹啉-4-甲酰胺
- 3-([1,4′-联哌啶]-1′-基甲基)-7-溴-N-(1-苯基环丙基)-2-[3-(三氟甲基)苯基]-4-喹啉甲酰胺
- GSK2193874游离态
- 化合物GSK2193874
- 1336960-13-4
- 3-([1,4'-Bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-(3-(trifluoromethyl)phenyl)quinoline-4-carboxamide
- GSK2193874,inhibit,GSK 2193874,Transient receptor potential channels,GSK-2193874,Inhibitor,TRP Channel
- GSK2193874 >=98% (HPLC)
- 4-Quinolinecarboxamide, 3-([1,4'-bipiperidin]-1'-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-
- GSK 2193874; GSK2193874
- TRPV4 antagonist GS2193874
- GSK2193874
- 3-([1,4′-Bipiperidin]-1′-ylmethyl)-7-bromo-N-(1-phenylcyclopropyl)-2-[3-(trifluoromethyl)phenyl]-4-quinolinecarboxamide