1160514-60-2
中文名称
1160514-60-2
英文名称
1-[4-[(2,3,3-Trichloro-1-oxo-2-propen-1-yl)amino]phenyl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylicacid
CAS
1160514-60-2
分子式
C16H11Cl3F3N3O3
分子量
456.63
MOL 文件
1160514-60-2.mol
1160514-60-2 结构式
基本信息
中文别名
吡喃 3化合物PYR3
化合物 T16687
英文别名
Pyr3TRPC3 Channel Inhibitor, Pyr3
TRPC3 Channel Inhibitor, Pyr3 - CAS 1160514-60-2 - Calbiochem
Ethyl-1-(4-(2,3,3-trichloroacrylamide)phenyl)-5-(trifluoromethyl)-1H-pyrazole-4-carboxylate
1-[4-(2,3,3-Trichloro-acryloylamino)-phenyl]-5-trifluoromethyl-1H-pyrazole-4-carboxylic acid ethyl ester
1-[4-[(2,3,3-Trichloro-1-oxo-2-propen-1-yl)amino]phenyl]-5-(trifluoromethyl)-1H-pyrazole-4-carboxylicacid
1H-Pyrazole-4-carboxylic acid, 1-[4-[(2,3,3-trichloro-1-oxo-2-propen-1-yl)amino]phenyl]-5-(trifluoromethyl)-, ethyl ester
物理化学性质
熔点151-153 °C(Solv: toluene (108-88-3))
沸点534.0±50.0 °C(Predicted)
密度1.54±0.1 g/cm3(Predicted)
储存条件-20°C储存
溶解度溶于DMSO（高达40mg/ml）。
酸度系数(pKa)9.97±0.70(Predicted)
形态粉末
颜色白色至米色
稳定性可在-20°C下的DMSO中的溶液储存长达3个月。
常见问题列表
生物活性
Pyr3 是 TRPC3 的选择性抑制剂，其对 TRPC3 介导的 Ca2+ 内流的 IC50 值为 700 nM。靶点
IC50: 700 nM (TRPC3).
体外研究
Pyr3 selectively and directly inhibits TRPC3 channels among TRPC family members. Application of Pyr3 inhibits TRPC3-mediated Ca 2+ influx in a dose-dependent manner with the IC 50 value of 700 nM. Pyr3 becomes apparent at 0.3 μM, and is almost complete at 3 μM. Interestingly, Ca 2+ influx is inhibited by Pyr3 in cells co-expressing TRPC3 plus TRPC6 but not in cells coexpressing TRPC1 plus TRPC5. The Ang II-induced NFAT translocation is suppressed by Pyr3, but weakly by Pyr2 in a concentration-dependent manner (IC 50 value was 0.05 μM for Pyr3 and 2 μM for Pyr2).