ICA 069673
| 中文名称 | ICA 069673 |
|---|---|
| 中文同义词 | 化合物ICA069673;N-(2-氯-5-嘧啶基)-3,4-二氟苯甲酰胺;ICA 069673,KV7.2 / KV7.3通道开启器 |
| 英文名称 | ICA 069673 |
| 英文同义词 | ICA 069673;N-(2-Chloro-5-pyrimidinyl)-3,4-difluorobenzamide;ICA069673;ICA-069673;Benzamide, N-(2-chloro-5-pyrimidinyl)-3,4-difluoro-;ICA-069673 >=98% (HPLC);Potassium Channel,ICA 069673,ICA-069673,KcsA,inhibit,Inhibitor;N-(2-Chloropyrimidin-5-yl)-3,4-difluorobenzamide |
| CAS号 | 582323-16-8 |
| 分子式 | C11H6ClF2N3O |
| 分子量 | 269.63 |
| EINECS号 | |
| 相关类别 | Selective KCNQ2/Q3 potassium channel opener. |
| Mol文件 | 582323-16-8.mol |
| 结构式 |  |
ICA 069673 性质
| 沸点 | 358.9±37.0 °C(Predicted) |
|---|---|
| 密度 | 1.539±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,Room Temperature |
| 溶解度 | DNF:30.0(最大浓度 mg/mL);111.26(最大浓度 mM) DMSO:36.24(最大浓度 mg/mL);134.4(最大浓度 mM) 乙醇:30.25(最大浓度 mg/mL);112.18(最大浓度 mM) |
| 形态 | 粉末 |
| 酸度系数(pKa) | 9.47±0.70(Predicted) |
| 颜色 | 白色至米白色 |
ICA 069673 (compound 51) 是一种口服活性、有效的 KCNQ2/Q3 potassium channel 的选择性激活剂，其对KCNQ2/Q3和KCNQ3/Q5的EC50值分别为0.69 μM和14.3 μM。
| Target | Value |
|
KCNQ2/Q3
(Cell-free assay) | 0.69 μM(EC50) |
|
KCNQ3/Q5
(Cell-free assay) | 14.3 μM(EC50) |
ICA-069673 is found to be 20-fold selective for KCNQ2/Q3 over KCNQ3/Q5 and has no measurable activity against a panel of cardiac ion channels (IC 50 values > 30 μM for hERG, Nav1.5, L type channels, and KCNQ1) as well as no activity on GABA(A) gated channels at 10 μM. ICA-069673 exhibits much stronger effects on KCNQ2 channels, including a large hyperpolarizing shift of the voltage-dependence of activation, an 2-fold enhancement of peak current and pronounced subtype specificity for KCNQ2 over KCNQ3. Based on ICA73 sensitivity of chimeric constructs of the transmembrane segments of KCNQ2 and KCNQ3, this drug appears to interact with the KCNQ2 voltage sensor (S1-S4).
安全信息
| 更新日期 | 产品编号 | 产品名称 | CAS号 | 包装 | 价格 |
|---|---|---|---|---|---|
| 2024/04/30 | HY-101396 | ICA 069673 ICA-069673 | 582323-16-8 | 5mg | 770元 |
| 2024/04/30 | S0144 | ICA 069673 ICA 069673 | 582323-16-8 | 5mg | 779.46元 |