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Clofilium phosphate  (Synonyms: 磷酸氯非铵; LY 150378)

目录号: HY-105439A
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Clofilium phosphate (LY 150378) 是一种抗心律失常/抗纤颤剂。Clofilium phosphate 可显著延长犬心脏浦肯野纤维的动作电位时程与有效不应期、提升室颤阈值，能降低折返性心律失常风险，部分室颤可自行转复为窦性心律。Clofilium phosphate 可用于心室颤动、心律失常及室性快速性心律失常的相关研究。

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Clofilium phosphate

Clofilium phosphate Chemical Structure

CAS No. : 68379-03-3

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Clofilium phosphate 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Clofilium phosphate (LY 150378) is an antiarrhythmic/antifibrillatory agent. Clofilium phosphate significantly prolongs the action potential duration and effective refractory period of canine cardiac Purkinje fibers, increases the ventricular fibrillation threshold, reduces the risk of reentrant arrhythmias, and enables spontaneous conversion of some ventricular fibrillation episodes to sinus rhythm. Clofilium phosphate is applicable to research related to ventricular fibrillation, arrhythmias, and ventricular tachyarrhythmias[1][2][3].

体外研究
(In Vitro)

Clofilium phosphate 可选择性延长正常犬浦肯野纤维的动作电位时程和有效不应期[1]。
Clofilium phosphate (30-100 nM) 可延长犬乳头肌和心室游离壁细胞的动作电位时程，但在测试浓度下对心房肌的 APD 无影响[1]。
Clofilium phosphate (30-10 nM; at least 1 h) 可选择性延长离体正常犬浦肯野纤维的动作电位时程与不应期，且不会显著改变膜反应性、传导速度或舒张期去极化速率；在基础周期更长的情况下，以及高浓度下的去极化纤维中，其 APD 延长作用更显著[2]。
Clofilium phosphate (0.01-10 μM; 30 min) 可强效延长离体犬心脏浦肯野纤维的 APD95，其 C20APD95 值为 0.26 μM，在 10 μM 时 APD95 最大升高 39 ± 8%[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clofilium phosphate 相关抗体:
体内研究
(In Vivo)

Clofilium phosphate (0.5-1.0 µmole/kg；静脉注射；输注 30 分钟) 可剂量依赖性地提高麻醉杂种犬的心室颤动阈值[1]。
Clofilium phosphate (10 mg/kg；皮内注射) 可使麻醉健康杂种犬的左心室功能性不应期延长至少 12%[3]。
Clofilium phosphate (0.1-10 mg/kg；静脉注射) 可在 70% 患有 24 小时陈旧性心肌梗死的麻醉杂种犬中预防程序性电刺激诱发的室性心动过速[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: mongrel (adult, 8-15 kg, pentobarbital-anesthetized, electrical stimulation-induced ventricular fibrillation model)[1]
Dosage: 0.5 µmole/kg; 1.0 µmole/kg
Administration: i.v.; infused over 30 minutes
Result: Increased mean ventricular fibrillation threshold (VFT) by 98% from pre-drug values at 0.5 µmole/kg.
Induced spontaneous conversion of ventricular fibrillation (VF) to normal sinus rhythm in 8% of episodes (2 out of 25), with VF lasting an average of 8.5 seconds at 0.5 µmole/kg.
Increased mean VFT by 205% from pre-drug values at 1.0 µmole/kg, with this increase significant at all post-infusion time periods.
Induced spontaneous conversion of VF to normal sinus rhythm in 22% of episodes (5 out of 23), with VF lasting an average of 8.5 seconds at 1.0 µmole/kg.
Produced significantly higher VFT at the 4th post-infusion determination (≈240 minutes after end of infusion) than at the first three post-infusion determinations for both doses.
分子量

435.97

Formula

C21H39ClNO4P
CAS 号
中文名称

磷酸氯非铵
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

Clofilium phosphate 相关分类

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Keywords:

Clofilium68379-03-3LY 150378磷酸氯非铵LY150378LY-150378Drug DerivativeDrug derivativecanine cardiac tissuesatrial muscle cellsnormal sinus rhythmventricular tachyarrhythmiasventricular fibrillationanesthetized dogsventricular tachycardiacardiac arrhythmiasacute myocardial infarctionInhibitorinhibitorinhibit

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