2. Phaclofen

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.

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Phaclofen Chemical Structure

Phaclofen Chemical Structure

CAS No. : 114012-12-3

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Phaclofen Related Antibodies

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Description

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]
In Vitro

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

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

Phaclofen Related Antibodies
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].

MedChemExpress (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.
Molecular Weight

249.63

Formula

C9H13ClNO3P
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

ClC1=CC=C(C(CN)CP(O)(O)=O)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

1M NaOH : 50 mg/mL (200.30 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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Purity & Documentation

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 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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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:

Phaclofen114012-12-3Inhibitorinhibitorinhibit

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