| 产品描述: | Etripamil displays atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells. Etripamil is an antagonist of short-acting L-type calcium-channel. It has a rapid onset of action designed for intranasal administration. It is also used to treat Paroxysmal Supraventricular Tachycardia |
| 靶点: |
Calcium Channel |
| 体外研究: |
Etripamil displays atrioventricular nodal conduction and prolongs atrioventricular nodal refractory periods by inhibiting calcium ion influx through the calcium slow channels in the atrioventricular node cells. |
| 体内研究: |
Etripamil (0-0.3 mg/kg;静脉注射) 在清醒遥测食蟹猴中表现出剂量依赖性收缩压下降、心率增加和 PR间期增加。 Etripamil (1.9-5.7 mg/kg;鼻腔给药;每周一次;26 次给药) 不会引起食蟹猴的宏观或全身微观异常。 |
| 参考文献: |
1. Stambler BS, et al. Etripamil Nasal Spray for Rapid Conversion of Supraventricular Tachycardia to Sinus Rhythm. J Am Coll Cardiol. 2018 Jul 31;72(5):489-497. 2. Milestone Pharmaceuticals Announces USAN Approval of Generic Name “Etripamil” for its Phase 2 Clinical Development Product for the Treatment of Paroxysmal Supraventricular Tachycardia. |
| 溶解性: |
Soluble in Ethanol |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.21 ml |
11.048 ml |
22.095 ml |
| 5 mM |
0.442 ml |
2.21 ml |
4.419 ml |
| 10 mM |
0.221 ml |
1.105 ml |
2.21 ml |
| 50 mM |
0.044 ml |
0.221 ml |
0.442 ml |
|
| 注意: |
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