product name
GSK1016790A, ≥98% (HPLC)
质量水平
检测方案
≥98% (HPLC)
形式
solid
颜色
white
溶解性
DMSO: >10 mg/mL
创始人
GlaxoSmithKline
储存温度
−20°C
SMILES字符串
CC(C)C[C@H](NC(=O)c1cc2ccccc2s1)C(=O)N3CCN(CC3)C(=O)[C@H](CO)NS(=O)(=O)c4ccc(Cl)cc4Cl
InChI
1S/C28H32Cl2N4O6S2/c1-17(2)13-21(31-26(36)24-14-18-5-3-4-6-23(18)41-24)27(37)33-9-11-34(12-10-33)28(38)22(16-35)32-42(39,40)25-8-7-19(29)15-20(25)30/h3-8,14-15,17,21-22,32,35H,9-13,16H2,1-2H3,(H,31,36)/t21-,22-/m0/s1
InChI key
IVYQPSHHYIAUFO-VXKWHMMOSA-N
应用
GSK1016790A可用于：
- 刺激非洲爪蟾卵母细胞中瞬时受体电位香草素亚型4 (TRPV4)介导的电流
- 刺激人视网膜毛细血管内皮细胞(HRCEC)中钙2+ 水平的测定
- 研究TRPV4通道在脑出血(ICH)后脑损伤中的作用
- 触发牛髓核细胞或Hanks′平衡盐溶液中TRPV4通道
生化/生理作用
GSK1016790A是一种新型强效TRPV4通道激动剂。TRP超家族的TRPV4（瞬时受体电位香草素4）成员涉及许多生理过程。GSK1016790A诱导钙2+流入表达HEK细胞（EC50值分别为18和2.1纳米的小鼠和人TRPV4中，并在1纳米以上的浓度下诱导TRPV4全细胞电流的剂量依赖性激活。它的效力是4a-PDD（货号P8014）的300倍。
特点和优势
该化合物由GlaxoSmithKline开发。要浏览其他药物开发化合物和批准的药物/候选药物列表，单击此处。
WGK
WGK 1
闪点(°F)
Not applicable
闪点(°C)
Not applicable
TRPV4 regulates migration and tube formation of human retinal capillary endothelial cells
Wen L, et al.
BMC Ophthalmology, 18(1), 38-38 (2018)
When size matters: transient receptor potential vanilloid 4 channel as a volume-sensor rather than an osmo-sensor
Toft-Bertelsen TL, et al.
The Journal of Physiology, 595(11), 3287-3302 (2017)
TRPV4 channels stimulate Ca2+-induced Ca2+ release in mouse neurons and trigger endoplasmic reticulum stress after intracerebral hemorrhage
Shen J, et al.
Brain Research Bulletin, 146, 143-152 (2019)
Sandip M Swain et al.
The Journal of biological chemistry, 296, 100171-100171 (2020-12-11)
The ion channels Piezo1 and TRPV4 have both, independently, been implicated in high venous pressure- and fluid shear stress-induced vascular hyperpermeability in endothelial cells. However, the mechanism by which Piezo1 and TRPV4 channels execute the same function is poorly understood.
Reduced tissue osmolarity increases TRPV4 expression and pro-inflammatory cytokines in intervertebral disc cells
Walter BA, et al.
European Cells & Materials, 32, 123-123 (2016)
商品
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