2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. Potassium Channel iGluR
  4. Flupirtine

Flupirtine  (Synonyms: 氟吡汀; D 9998)

目录号: HY-17001A 纯度: 99.98%
COA 产品使用指南

摩尔计算器

Flupirtine(D 9998)是神经元钾通道开放剂，同时还能拮抗NMDA受体。

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Flupirtine Chemical Structure

Flupirtine Chemical Structure

CAS No. : 56995-20-1

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5 mg ￥500
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10 mg ￥800
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100 mg   询价  

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Other Forms of Flupirtine:

Flupirtine 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 1 篇科研文献

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AMPA Receptor NMDA Receptor Kainate Receptor

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Flupirtine(D 9998) is a selective neuronal potassium channel opener that also has NMDA receptor antagonist properties. IC50 Value: Target: Potassium channel; NMDA receptor in vitro: High concentrations of flupirtine antagonized inward currents to NMDA(200 microM) at -70 mV with an lC50 against steady-state responses of 182.1+/-12.1 microM. The effects of flupirtine were voltage-independent and not associated with receptor desensitization making actions within the NMDA receptor channel or at the glycine modulatory site unlikely. NMDA receptor antagonism probably has little relevance for the clinical efficacy of flupirtine as the concentrations needed were far higher than those achieved in clinical practice. However, the activation of a G-protein-regulated inwardly rectifying K+ channel was identified as an interesting molecular target site of flupirtine. In the next stage, the central nervous spectrum of action of experimental K+ channel openers (PCO) was considered. As far as they have been studied, experimental K+ channel openers display a spectrum of action comparable to that of flupirtine [1]. Therapeutic flupirtine concentrations (≤10 M) did not affect voltage-gated Na(+) or Ca(2+) channels, inward rectifier K(+) channels, nicotinic acetylcholine receptors, glycine or ionotropic glutamate receptors. Flupirtine shifted the gating of K(V)7 K(+) channels to more negative potentials and the gating of GABA(A) receptors to lower GABA concentrations [2]. Cell exposure to flupirtine decreased the amplitude of delayed rectifier K(+) current (I(K(DR))) with a concomitant raise in current inactivation in NSC-34 neuronal cells [4]. in vivo: Rats were trained to discriminate the novel analgesic flupirtine (10.0 mg/kg i.p., 10 min) from no drug under a two-choice fixed-ratio 5 shock-termination schedule. Flupirtine yielded a dose-response curve with an ED50 of 3.87 mg/kg. The opioid analgesics pentazocine, codeine and tramadol failed to produce flupirtine appropriate responding. The opioid antagonist naltrexone did not antagonize the discriminative effects of flupirtine [3]. Both morphine (ED = 0.74 mg/kg) and flupirtine (ED = 3.32 mg/kg) caused dose-related anti-hyperalgesia at doses that did not cause sedation [5]. Toxicity: Based on study-end data, hepatotoxicity was detected in 31% of patients receiving flupirtine for ≥ 6 weeks [6].

IC50 & Target

NMDA Receptor

 

Clinical Trial
分子量

304.32

Formula

C15H17FN4O2
CAS 号
性状

固体

颜色

Off-white to light yellow

中文名称

氟吡啶
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
细胞实验： 

DMSO 中的溶解度 : 125 mg/mL (410.75 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.2860 mL 16.4301 mL 32.8601 mL
5 mM 0.6572 mL 3.2860 mL 6.5720 mL
查看完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

  • 摩尔计算器

  • 稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
计算结果
工作液所需浓度 : mg/mL
纯度 & 产品资料
参考文献

Flupirtine 相关分类

完整储备液配制表

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时，请在6个月内使用，-20°C储存时，请在1个月内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.2860 mL 16.4301 mL 32.8601 mL 82.1504 mL
5 mM 0.6572 mL 3.2860 mL 6.5720 mL 16.4301 mL
10 mM 0.3286 mL 1.6430 mL 3.2860 mL 8.2150 mL
15 mM 0.2191 mL 1.0953 mL 2.1907 mL 5.4767 mL
20 mM 0.1643 mL 0.8215 mL 1.6430 mL 4.1075 mL
25 mM 0.1314 mL 0.6572 mL 1.3144 mL 3.2860 mL
30 mM 0.1095 mL 0.5477 mL 1.0953 mL 2.7383 mL
40 mM 0.0822 mL 0.4108 mL 0.8215 mL 2.0538 mL
50 mM 0.0657 mL 0.3286 mL 0.6572 mL 1.6430 mL
60 mM 0.0548 mL 0.2738 mL 0.5477 mL 1.3692 mL
80 mM 0.0411 mL 0.2054 mL 0.4108 mL 1.0269 mL
100 mM 0.0329 mL 0.1643 mL 0.3286 mL 0.8215 mL
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:

Flupirtine56995-20-1D 9998氟吡啶D9998D-9998Potassium ChanneliGluRKcsAIonotropic glutamate receptorsInhibitorinhibitorinhibit

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