85175-67-3
85175-67-3 結(jié)構(gòu)式
基本信息
中文別名
扎替雷定 英文別名
ZatebradineUL-FS-49 free base
UL-FS-49CL free base
2H-3-Benzazepin-2-one, 3-[3-[[2-(3,4-dimethoxyphenyl)ethyl]methylamino]propyl]-1,3,4,5-tetrahydro-7,8-dimethoxy-
所屬類別
生物化工：激動劑抑制劑物理化學性質(zhì)
沸點612.5±55.0 °C(Predicted)
密度1.115±0.06 g/cm3(Predicted)
儲存條件Sealed in dry,2-8°C
溶解度DMSO : ≥ 50 mg/mL (109.51 mM)
酸度系數(shù)(pKa)8.99±0.50(Predicted)
形態(tài)Oil
顏色Light brown to brown
扎替雷定價格(試劑級)
| 報價日期 | 產(chǎn)品編號 | 產(chǎn)品名稱 | CAS號 | 包裝 | 價格 |
| 2024/11/08 | HY-13422A | 扎替雷定 Zatebradine | 85175-67-3 | 5mg | 700元 |
| 2024/11/08 | HY-13422A | 扎替雷定 Zatebradine | 85175-67-3 | 10mM * 1mLin DMSO | 703元 |
| 2024/11/08 | HY-13422A | 扎替雷定 Zatebradine | 85175-67-3 | 10mg | 1100元 |
常見問題列表
生物活性
Zatebradine (UL-FS-49 (free base); UL-FS-49CL (free base)) 是一種高效的 HCN Channel 抑制劑，其 IC50 值為 1.96 μM。Zatebradine 會阻止通過人類 HCN1，HCN2，HCN3 和 HCN4 通道的緩慢內(nèi)向電流，其 IC50 值分別為 1.83 μM，2.21 μM，1.90 μM 和 1.88 μM。
.靶點
IC50: 1.96 μM ( HCN channels )
體外研究
The use-dependent blockade by Zatebradine of the cardiac pacemaker current from rabbit sino-atrial node cells has an apparent K d of 480 nM.
體內(nèi)研究
Zatebradine (0-20 mg/kg; intraperitoneal injection; for 30 minutes; male C57/Bl6-mice) reduces the heart rate dose-dependently from 600 to 200 bpm with ED 50 value of 1.8 mg/kg and induces increasing arrhythmia.
| Animal Model: | Male C57/Bl6-mice |
| Dosage: | 0 mg/kg, 0.1 mg/kg, 1 mg/kg, 10 mg/kg, 20 mg/kg |
| Administration: | Intraperitoneal injection; for 30 minutes |
| Result: | Observed acute blood glucose reduction, dose-dependently reduced glycated hemoglobin, significantly prevented the decrease of IRI levels at doses of 3 and 10 mg/kg, and no difference in food intake or body weight. |