1. Membrane Transporter/Ion Channel
  2. Potassium Channel
  3. ONO-9517601

ONO-9517601 是一种高效、具有口服活性、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 = 0.067 μM,TREK-2 IC50 = 0.23 μM)。ONO-9517601 在 MK-801 (HY-15084B) 诱导的大鼠新物体识别 (NOR) 模型中表现出显著功效。ONO-9517601 可用于神经系统和认知障碍的研究。

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ONO-9517601

ONO-9517601 Chemical Structure

CAS No. : 2640753-22-4

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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

ONO-9517601 is a potent, orally active, selective and CNS penetrant dual TREK-1/TREK-2 inhibitor (TREK-1 IC50= 0.067 μM, TREK-2 IC50= 0.23 μM). ONO-9517601 displays robust efficacy in an MK-801 (HY-15084B) challenge rat novel object recognition (NOR) paradigm. ONO-9517601 can be used for research on neurological and cognitive disorders[1].

IC50 & Target[1]

TREK-1

0.067 μM (IC50)

TREK-2

0.23 μM (IC50)

体外研究
(In Vitro)

ONO-9517601 (10 μM) 抑制腺苷 A3 (98%) 和 DAT (78%),对 Cav1.2、HCN4、Kir2.1、Kv1.5、Kv4.3、KCNQ1/E1 和 Nav1.5 的活性极低,对 TASK-1、TASK-2、THIK-1 和 TRESK 没有显著影响,并且以 6.7 μM 的 IC50 阻断 hERG[1]

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

药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 1 mg/kg i.v. CLplasma 30.0 mL/min/kg
Rat 1 mg/kg i.v. Vss 2.2 L/kg
Rat 1 mg/kg i.v. T1/2 1.0 h
Rat 1 mg/kg p.o. Cmax 80 ng/mL
Rat 1 mg/kg p.o. F 40 %
Cynomolgus Monkey 1 mg/kg p.o. Cmax 152 ng/mL
Cynomolgus Monkey 1 mg/kg p.o. F 34 %
Cynomolgus Monkey 1 mg/kg i.v. Vss 2.1 L/kg
Cynomolgus Monkey 1 mg/kg i.v. T1/2 3.3 h
Cynomolgus Monkey 1 mg/kg i.v. CLplasma 13.3 mL/min/kg
Dog 1 mg/kg p.o. Cmax 315 ng/mL
Dog 1 mg/kg p.o. F 97 %
Dog 1 mg/kg i.v. CLplasma 1.9 mL/min/kg
Dog 1 mg/kg i.v. Vss 5.9 L/kg
Dog 1 mg/kg i.v. T1/2 56 h
体内研究
(In Vivo)

ONO-9517601 (0.1-30 mg/kg,口服,在 MK-801 注射前 3.5 小时给药) 可改善 MK-801 诱导的认知功能障碍模型中大鼠的识别记忆[1]
ONO-9517601 (56.6 mg/kg,口服,单次给药) 不会引起大鼠产生显著的神经行为学异常[1]

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

Animal Model: Male rats[1]
Dosage: 0.1, 0.3, 1, 3, 10, 30 mg/kg
Administration: p.o., 3.5 h pre-MK-801
Result: Significantly reversed the MK-801 deficit at 1, and 3 mg/kg. Improved recognition memory in rats.
分子量

461.94

Formula

C25H24ClN5O2

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
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  • 稀释计算器

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Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

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× = ×
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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.

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产品名称:
ONO-9517601
目录号:
HY-179004
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