ACT-709478 (Synonyms: ACT-709478)
目录号: PL02095 纯度: ≥99%
CAS No. :1838651-58-3
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中文名称
ACT-709478
中文别名
N-(1-((5-氰基吡啶-2-基)甲基)-1H-吡唑-3-基)-2-(4-(1-(三氟甲基)环丙基)苯基)乙酰胺
英文名称
ACT-709478
英文别名
3Z7U1U8Z9E;N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)-phenyl)acetamide;N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)phenyl)acetamide;Unii-3Z7U1U8Z9E;ACT-709478
Cas No.
1838651-58-3
分子式
C22H18F3N5O
分子量
425.41
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ACT-709478 是一种口服有效的,可透过血脑屏障的选择性 T 型电压门控钙通道 (T-type calcium channel) 阻滞剂,可用于全身性癫痫的研究。
生物活性
ACT-709478 is a potent, selective, orally active, and brain penetrating T-type calcium channel blocker. ACT-709478 is used in the research of generalized epilepsies.
性状
Solid
IC50 & Target[1][2]
Cav1.2 2410 nM (IC50) CaV3.1
体外研究(In Vitro)
ACT-709478 (Compound 66b) blocks Cav3.1, Cav3.2, Cav3.3, Cav1.2 with IC50s of 6.4, 18, 7.5 and 2410 nM, respectively. ACT-709478 blocks recombinant channel hCav3.3 potently with marked voltage-dependency (Kr≈1500 nM and Ki≈20 nM). ACT-709478 blocks currents through hKv11.1-hERG channels with an IC50 of 5.5 μM.
ACT-709478 also inhibits P450 enzymes with IC50s of 14, 15, 22, 25, 51 and 52 μM for CYP2C8,CYP2D6 CYP2C9, CYP2C19, CYP3A4, and CYP2B6, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
ACT-709478 (Compound 66b, 100, 300 mg/kg, p.o., 12 hours) potently decreases the cumulative duration of absence-like seizures in mice. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Bezen?on O, et al. Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies. J Med Chem. 2017 Dec 14;60(23):9769-9789.
溶解度数据
In Vitro: DMSO : ≥ 125 mg/mL (293.83 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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