1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. GABA Receptor
  3. Phaclofen

Phaclofen 是一种选择性 GABAB receptor 拮抗剂。Phaclofen 是一种外周和中央的 baclofen 拮抗剂。酞氯芬在确定中枢和外周 GABA 和 (-)-baclofen 相互作用的 bicuculline-insensitive 受体的生理意义方面可能是一种潜在的化合物。

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Phaclofen Chemical Structure

Phaclofen Chemical Structure

CAS No. : 114012-12-3

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1 mg ¥2350
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5 mg ¥5200
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Customer Review

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Phaclofen is a selective GABAB receptor antagonist. Phaclofen is a peripheral and central baclofen antagonist. Phaclofen maybe a potential compound in determining the physiological significance of central and peripheral bicuculline-insensitive receptors with which GABA and (-)-baclofen interact[1][2].

IC50 & Target

GABAB receptor[1]

体外研究
(In Vitro)

The GABAB antagonist phaclofen (500 µM) partly prevents the effect of 1 µM of (R+) baclofen[5].

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

体内研究
(In Vivo)

Phaclofen (2 mg/kg; i.p) shows that fewer neuropeptide Y-like immunoreactive fibers are detected in the stimulated cuneate nucleus[4].
Phaclofen (2 mg/kg; s.c) antagonizes the effects of 6 mg/kg R(+) baclofen in dorsal striatum[5].
Phaclofen (100 nmol; intrathecal injection) antagonizes the depressant effect of baclofen. Phaclofen (100 nmol) is devoid of stimulatory or depressant effects on spinal reflexes[3].

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

Animal Model: Sprague–Dawley rats (180–250 g)[4]
Dosage: 2 mg/kg
Administration: I.p.
Result: Fewer neuropeptide Y-like immunoreactive fibers were detected in the stimulated cuneate nucleus.
Animal Model: Male Wistar rats (280–320 g)[5]
Dosage: 2 mg/kg
Administration: S.c.
Result: Antagonized the effects of 6 mg/kg R(+) baclofen in dorsal striatum.
分子量

249.63

Formula

C9H13ClNO3P

CAS 号
性状

固体

颜色

White to off-white

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

1M NaOH 中的溶解度 : 50 mg/mL (200.30 mM; 超声助溶)

DMSO 中的溶解度 : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.0059 mL 20.0296 mL 40.0593 mL
5 mM 0.8012 mL 4.0059 mL 8.0119 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。-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

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

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。-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
1M NaOH 1 mM 4.0059 mL 20.0296 mL 40.0593 mL 100.1482 mL
5 mM 0.8012 mL 4.0059 mL 8.0119 mL 20.0296 mL
10 mM 0.4006 mL 2.0030 mL 4.0059 mL 10.0148 mL
15 mM 0.2671 mL 1.3353 mL 2.6706 mL 6.6765 mL
20 mM 0.2003 mL 1.0015 mL 2.0030 mL 5.0074 mL
25 mM 0.1602 mL 0.8012 mL 1.6024 mL 4.0059 mL
30 mM 0.1335 mL 0.6677 mL 1.3353 mL 3.3383 mL
40 mM 0.1001 mL 0.5007 mL 1.0015 mL 2.5037 mL
50 mM 0.0801 mL 0.4006 mL 0.8012 mL 2.0030 mL
60 mM 0.0668 mL 0.3338 mL 0.6677 mL 1.6691 mL
80 mM 0.0501 mL 0.2504 mL 0.5007 mL 1.2519 mL
100 mM 0.0401 mL 0.2003 mL 0.4006 mL 1.0015 mL
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产品名称:
Phaclofen
目录号:
HY-100798
需求量: