2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. ONO-7927846

ONO-7927846 是一种高效、具有口服有效性、选择性强且可透过血脑屏障的 TREK-1/TREK-2 双重抑制剂 (TREK-1 IC50= 0.11 μM，TREK-2 IC50= 0.29 μM)。 ONO-7927846 在 MK-801 (HY-15084B) 诱导的大鼠新物体识别 (NOR) 范式中表现出显著功效。ONO-7927846 可用于神经系统和认知障碍的相关研究。

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ONO-7927846

ONO-7927846 Chemical Structure

CAS No. : 2640753-27-9

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ONO-7927846 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ONO-7927846 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.11 μM, TREK-2 IC50= 0.29 μM). ONO-7927846 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-7927846 can be used for research on neurological and cognitive disorders[1].

IC50 & Target[1]

TREK-1

0.11 μM (IC50)

TREK-2

0.29 μM (IC50)

体外研究
(In Vitro)

ONO-7927846 (10 μM) 对腺苷 A3 (91%) 和钠通道位点 2 (56%) 表现出 >50% 的抑制作用；对 Cav1.2、HCN4、Kir2.1、Kv1.5、Kv4.3、Kir2.2 和 Nav1.5 的活性极低；并且对 hERG 具有功能性抑制作用，IC50 为 4.3 μM[1]。

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

ONO-7927846 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. Vss 2.7 L/kg
Rat 1 mg/kg i.v. CLplasma 6.1 mL/min/kg
Rat 1 mg/kg i.v. T1/2 5.5 h
Rat 1 mg/kg p.o. Cmax 162 ng/mL
Rat 1 mg/kg p.o. F 57 %
Dog 0.5 mg/kg i.v. T1/2 76 h
Dog 0.5 mg/kg i.v. CLplasma 1.5 mL/min/kg
Dog 0.5 mg/kg i.v. Vss 7.1 L/kg
Dog 1 mg/kg p.o. Cmax 263 ng/mL
Dog 1 mg/kg p.o. F 100 %
Cynomolgus Monkey 1 mg/kg i.v. T1/2 9.3 h
Cynomolgus Monkey 1 mg/kg i.v. CLplasma 6.5 mL/min/kg
Cynomolgus Monkey 1 mg/kg i.v. Vss 4.4 L/kg
Cynomolgus Monkey 1 mg/kg p.o. Cmax 260 L/kg
Cynomolgus Monkey 1 mg/kg p.o. F 89 %
体内研究
(In Vivo)

ONO-7927846 (0.03-3 mg/kg；口服；于 MK-801 注射前 3.5 小时给药) 在 MK-801 诱导的大鼠新物体识别模型中显示出强劲的功效[1]。
ONO-7927846 (56.6 mg/kg；口服；单次给药) 未在大鼠中引起显著的神经行为学改变[1]。

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

Animal Model: Male rats[1]
Dosage: 0.03, 0.1, 0.3, 1, and 3 mg/kg
Administration: P.O., 3.5 h pre-MK-801
Result: Improved recognition memory in male rats after MK-801 challenge. Significantly reversed the MK-801 deficit at 1 mg/kg。
分子量

497.92

Formula

C25H22ClF2N5O2
CAS 号
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

ONO-7927846 相关分类

  • 摩尔计算器

  • 稀释计算器

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质量   浓度   体积   分子量 *
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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ONO-79278462640753-27-9VU6024391ONO7927846ONO 7927846VU 6024391VU-6024391Potassium ChannelKcsApreclinical research toolsrobust efficacy-acyl piperidine pyrazolesion channel selectivityMK-801 challenge rat NOR paradigmOPTIMIZATION CNS penetrantKP family of potassium ion channelspotencyPK profilesTREK inhibitorsInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-179005
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