|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|CsnPharm

CAS No.: 1838651-58-3

N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)phenyl)acetamide Catalog No. CSN24052

Synonyms: ACT-709478

ACT-709478 is a potent, selective, orally-bioavailable and brain penetrant T-type calcium channel blocker with IC50 of 6.4, 18, and 7.5 nM for Cav3.1, Cav3.2, and Cav3.3 channels respectively.

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400-920-2911

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技术信息

生物活性

描述T-type calcium channels (TTCCs) belong to the family of thelow-voltage-activated calcium channels. These channels are the products of three genes, CACNA1G, CACNA1H, and CACNA1I, yielding the Ca_v3.1, Ca_v3.2, and Ca_v3.3 channels, respectively. ACT-709478 blocked hCa_v3.3 potently but with marked voltage-dependency (K_r ≈ 1500 nM and K_i ≈ 20 nM). ACT-709478 blocked currents through hK_v11.1-hERG channels with an IC₅₀ of 5.5 μM. In WAG/Rij rats, 10 mg/kg po of ACT-709478 significantly decreased the cumulative duration of absence-like seizures over the next 12 h period by 93%, compared to a matched vehicle group. ACT-709478 completely suppressed the absence-type seizures over the first 6 h following administration. In the AGS model of juvenile DBA/2J mice, ACT-709478 showed a significant decrease of the seizure severity at a dose of 100 mg/kg po^[1]. Ascending single oral doses of 1-400 mg ACT-709478 were administered to sequential groups of eight subjects. ACT-709478 exhibited good tolerability and safety after single-dose administration^[2].
参考文献

[1] Bezençon O, Heidmann B, Siegrist R, 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;60(23):9769‐9789
[2] Richard M, Kaufmann P, Kornberger R, Dingemanse J. First-in-man study of ACT-709478, a novel selective triple T-type calcium channel blocker. Epilepsia. 2019;60(5):968‐978

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3507 mL
- 11.7534 mL
- 23.5067 mL
- 5 mM
- 0.4701 mL
- 2.3507 mL
- 4.7013 mL
- 10 mM
- 0.2351 mL
- 1.1753 mL
- 2.3507 mL

技术信息

CAS号

1838651-58-3

储存条件

粉末: Inert atmosphere,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H18F3N5O

运输

蓝冰

分子量

425.41

别名

ACT-709478

溶解度

DMSO	320.0 mg/mL (752.2 mM)
Water	insoluble

动物实验配方

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N-(1-((5-Cyanopyridin-2-yl)methyl)-1H-pyrazol-3-yl)-2-(4-(1-(trifluoromethyl)cyclopropyl)phenyl)acetamide Catalog No. CSN24052

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