|1-(3,4-二氟苯基)-3-(3-甲基-1-苯基-1H-吡唑-5-基)脲|CsnPharm

CAS No.: 1443246-62-5

ML 297 Catalog No. CSN25288

Synonyms: VU 0456810;CID 56642816

ML 297 is a potent and selective GIRK1/2 activator, with an EC50 of 0.16 μM.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述G protein‐gated inwardly rectifying K⁺ (K_ir3, also known as GIRK) channels modulate cell excitability, and have been implicated in a number of crucial physiological processes. ML 297 (VU 0456810) is a potent and selective GIRK1/2 (K_ir3.1/3.2) channel activator, with EC₅₀ values of 0.16 and 1.8 μM for GIRK1/2 and GIRK1/4, respectively. ML 297 is potential for the treatment of epilepsy^[1]. ML297 showed concentration-dependent efficacy when tested on cells expressing GIRK1/2 with a measured potency of ∼160 nM. In the ML297-treated (60 mg/kg) animals, there was an immediate decrease in locomotor activity compared to the control group. Furthermore, when compared to the vehicle-treated animals, the ML297-treated (60 mg/kg) group showed a modest (14%) decrease in performance on the rotarod suggesting ML297's effects on generalized locomotor activity may be mediated through sedation. In a maximal electroshock (MES) model of epilepsy in mice, ML297 (60 mg/kg) caused a robust increase in the latency of seizure onset equivalent to that observed with a 150 mg/kg dose of the known antiepileptic, sodium valproate. Moreover, ML297 (60 mg/kg) showed a highly significant ability to both prevent convulsions (p = 0.006) and prevent fatality of the PTZ (pentylenetetrazol) treatment (p = 0.001) with most of the animals treated with ML297 experiencing neither convulsions nor death^[2].
参考文献

[1] Wen W, Wu W, Romaine IM, et al. Discovery of 'molecular switches' within a GIRK activator scaffold that afford selective GIRK inhibitors. Bioorg Med Chem Lett. 2013;23(16):4562-4566
[2] Kaufmann K, Romaine I, Days E, et al. ML297 (VU0456810), the first potent and selective activator of the GIRK potassium channel, displays antiepileptic properties in mice. ACS Chem Neurosci. 2013;4(9):1278-1286

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
- 3.0458 mL
- 15.2292 mL
- 30.4585 mL
- 5 mM
- 0.6092 mL
- 3.0458 mL
- 6.0917 mL
- 10 mM
- 0.3046 mL
- 1.5229 mL
- 3.0458 mL

技术信息

CAS号

1443246-62-5

储存条件

粉末: Sealed in dry,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H14F2N4O

运输

蓝冰

分子量

328.32

别名

VU 0456810;CID 56642816

溶解度

DMSO	66.0 mg/mL (201.0 mM)
Water	Insoluble
Ethanol	15.0 mg/mL (45.7 mM)

动物实验配方

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ML 297 Catalog No. CSN25288

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