中文名 | ICA-069673 |
英文名 | ICA-069673 |
别名 | 化合物ICA069673 N-(2-氯-5-嘧啶基)-3,4-二氟苯甲酰胺 |
英文别名 | ICA069673 ICA-069673 ICA 069673 N-(2-Chloro-5-pyrimidinyl)-3,4-difluorobenzamide Benzamide, N-(2-chloro-5-pyrimidinyl)-3,4-difluoro- |
CAS | 582323-16-8 |
化学式 | C11H6ClF2N3O |
分子量 | 269.63 |
密度 | 1.539±0.06 g/cm3(Predicted) |
沸点 | 358.9±37.0 °C(Predicted) |
溶解度 | DMSO : ≥ 34 mg/mL (126.10 mM) |
酸度系数 | 9.47±0.70(Predicted) |
存储条件 | Sealed in dry,Room Temperature |
体外研究 | 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). |
参考资料 展开查看 | 1: Provence A, Malysz J, Petkov GV. The Novel KV7.2/KV7.3 Channel Opener ICA-069673 Reveals Subtype-Specific Functional Roles in Guinea Pig Detrusor Smooth Muscle Excitability and Contractility. J Pharmacol Exp Ther. 2015 Sep;354(3):290-301. doi: 10.1124/jpet.115.225268. Epub 2015 Jun 18. PubMed PMID: 26087697; PubMed Central PMCID: PMC4538873. 2: Vicente-Baz J, Lopez-Garcia JA, Rivera-Arconada I. Effects of novel subtype selective M-current activators on spinal reflexes in vitro: Comparison with retigabine. Neuropharmacology. 2016 Oct;109:131-8. doi: 10.1016/j.neuropharm.2016.05.025. Epub 2016 Jun 2. PubMed PMID: 27263036. 3: Brueggemann LI, Haick JM, Cribbs LL, Byron KL. Differential activation of vascular smooth muscle Kv7.4, Kv7.5, and Kv7.4/7.5 channels by ML213 and ICA-069673. Mol Pharmacol. 2014 Sep;86(3):330-41. doi: 10.1124/mol.114.093799. Epub 2014 Jun 18. PubMed PMID: 24944189; PubMed Central PMCID: PMC4152906. 4: Wang AW, Yang R, Kurata HT. Sequence determinants of subtype-specific actions of KCNQ channel openers. J Physiol. 2017 Feb 1;595(3):663-676. doi: 10.1113/JP272762. Epub 2016 Sep 23. PubMed PMID: 27506413; PubMed Central PMCID: PMC5285613. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 3.709 ml | 18.544 ml | 37.087 ml |
5 mM | 0.742 ml | 3.709 ml | 7.417 ml |
10 mM | 0.371 ml | 1.854 ml | 3.709 ml |
5 mM | 0.074 ml | 0.371 ml | 0.742 ml |
微信搜索化工百科或扫描下方二维码,添加化工百科小程序,随时随地查信息!