2. Membrane Transporter/Ion Channel
  3. Potassium Channel
  4. IDOR-1104-0086

IDOR-1104-0086 是一种口服有效、可穿过血脑屏障的 Kv7 potassium channel 开放剂，其 EC50 为 210 nM。IDOR-1104-0086 对 hERG 通道表现出强选择性，其 IC20 为 25 μM。IDOR-1104-0086 在两种啮齿动物癫痫模型中均表现出疗效，且耐受性良好。IDOR-1104-0086 可用于癫痫研究。

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IDOR-1104-0086

IDOR-1104-0086 Chemical Structure

CAS No. : 2756581-81-2

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IDOR-1104-0086 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

IDOR-1104-0086 is an orally active Kv7 potassium channel opener with an EC50 of 210 nM that can cross blood-brain barrier. IDOR-1104-0086 displays strong selectivity against the hERG channel with an IC20 of 25 μM. IDOR-1104-0086 exhibits efficacy in two rodent models of epilepsy and a favorable tolerability profile. IDOR-1104-0086 can used for the study of epilepsy[1].

IC50 & Target[1]

Kv7

250 nM (EC50)

体外研究
(In Vitro)

IDOR-1104-0086 (Compound 31) 可有效抑制大鼠原代皮层神经元-星形胶质细胞共培养体系中的病理性钙振荡，IC50 分别为 188 nM (急性) 和 228 nM (20 分钟)[1]。

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

IDOR-1104-0086 相关抗体:
药代动力学
(Parmacokinetics)[1]
Species Dose Route Indicator value
Rat 10 mg/kg p.o. AUC 10300 ng·h/mL
Rat 1 mg/kg i.v. CL 9.3 mL/min/kg
Rat 10 mg/kg p.o. Cmax 1100 ng/mL
Rat 1 mg/kg i.v. Vd 1.8 L/kg
Rat 10 mg/kg p.o. Tmax 0.17 h
Rat 1 mg/kg i.v. T1/2 2.8 h
Rat 10 mg/kg p.o. F 19 %
体内研究
(In Vivo)

IDOR-1104-0086 (Compound 31)（10-30 mg/kg，口服，单剂量) 可有效渗透啮齿动物脑组织，给药后 1 小时脑组织与血浆非结合性脑组织比值 ([B/P]u) > 127%，在 AGS 小鼠模型中几乎完全抑制全身性强直阵挛性癫痫发作，并在大鼠点燃模型中导致癫痫发作强度呈剂量依赖性降低[1]。

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

Animal Model: Audiogenic seizure-sensitive model of generalized convulsive seizures established in male juvenile DBA/2J mice (22-24 days old)[1]
Dosage: 10 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Induced almost full protection from the generalized tonic-clonic seizure in the AGS mouse model.
Animal Model: Amygdala-kindling rat Model established in adult male Wistar rats (body weight 300-350g)[1]
Dosage: 10 and 30 mg/kg
Administration: Oral administration (p.o.), single dose
Result: Displayed the inhibition of the bilateral forelimb clonus and facial myoclonic twitches without behavioral side effects.
分子量

334.28

Formula

C15H15F5N2O
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

IDOR-1104-0086 相关分类

  • 摩尔计算器

  • 稀释计算器

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  • 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:

IDOR-1104-00862756581-81-2Potassium ChannelKcsAPhenotypic ScreeningCa2? Oscillation AssayEpilepsyMice modelRat modelInhibitorinhibitorinhibit

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产品名称：
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目录号：
HY-175668
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