2. Membrane Transporter/Ion Channel Neuronal Signaling
  3. GABA Receptor
  4. Saclofen

Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats.

For research use only. We do not sell to patients.

Saclofen Chemical Structure

Saclofen Chemical Structure

CAS No. : 125464-42-8

Size Price Stock Quantity
5 mg USD 150 In-stock
10 mg USD 240 In-stock
25 mg USD 550 In-stock
50 mg USD 850 In-stock
100 mg USD 1350 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 3 publication(s) in Google Scholar

Saclofen Related Antibodies

Top Publications Citing Use of Products

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Saclofen is an orally available competitive GABAB receptor antagonist with an IC50 of 7.8 μM, but it has a weaker antagonistic effect on GABAB1b and GABAB2 heterodimer recombinant receptors. Saclofen can inhibit the binding of baclofen (HY-B007) to rat cerebellar membranes and block the phase shifts in circadian rhythms caused by baclofen. Saclofen has also shown anti-inflammatory and analgesic effects in rats[1][2][3][4][5].

In Vitro

Saclofen (300 μM, 0-24 h) inhibits the phase changes in the circadian rhythm caused by baclofen in brain slices of the rat suprachiasmatic nucleus (SCN) [1].
Saclofen (0.1 μM-1 mM, 10 s) suppresses the increase in CHO intracellular calcium induced by GABA at high concentrations[2].
Saclofen inhibits the binding of baclofen to rat cerebellar membranes with an IC50 of 7.8 μM[3].

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

Saclofen Related Antibodies
In Vivo

Saclofen (5mg/mL, i.g., single dose) improves inflammation in rats induced by lipopolysaccharides[3].
Saclofen (1mg/mL, i.p., single dose) has analgesic effects in a rat pain model induced by acetic acid[4].

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

Animal Model: Adult male Wistar rats induced by lipopolysaccharide(LPS)[3]
Dosage: 5 mg/mL, single dose
Administration: i.g.
Result: Eliminated the hypotensive effect of lipopolysaccharide (LPS), restored mean arterial pressure (MAP), and reduced the increase of TNF-α and IL-6 induced by LPS.
Animal Model: Acetic acid -induced visceral pain by in rat[4]
Dosage: 1 mg/kg, single dose
Administration: Intraperitoneal injection (i.p.)
Result: Could prevent pain caused by the GABAB receptor agonist baclofen.
Molecular Weight

249.71

Formula

C9H12ClNO3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(CC(CN)C1=CC=C(Cl)C=C1)(O)=O
Shipping

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

H2O : 10 mg/mL (40.05 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0046 mL 20.0232 mL 40.0465 mL
5 mM 0.8009 mL 4.0046 mL 8.0093 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.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
=
Concentration
×
Volume
×
Molecular Weight *

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only.If necessary, please contact MedChemExpress (MCE).
Purity & Documentation

Purity: 99.87%

COA (252 KB) HNMR (242 KB) LCMS (88 KB)

Handling Instructions (2659 KB)
References

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
H2O 1 mM 4.0046 mL 20.0232 mL 40.0465 mL 100.1161 mL
5 mM 0.8009 mL 4.0046 mL 8.0093 mL 20.0232 mL
10 mM 0.4005 mL 2.0023 mL 4.0046 mL 10.0116 mL
15 mM 0.2670 mL 1.3349 mL 2.6698 mL 6.6744 mL
20 mM 0.2002 mL 1.0012 mL 2.0023 mL 5.0058 mL
25 mM 0.1602 mL 0.8009 mL 1.6019 mL 4.0046 mL
30 mM 0.1335 mL 0.6674 mL 1.3349 mL 3.3372 mL
40 mM 0.1001 mL 0.5006 mL 1.0012 mL 2.5029 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.

Saclofen Related Classifications

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:

Saclofen125464-42-8GABA ReceptorGamma-aminobutyric acid Receptorγ-Aminobutyric acid ReceptorBaclofenAnti-inflammatoryPain reliefCircadian rhythmCalcium increaseInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product Name

  

Salutation

Applicant Name *

 

Email Address *

Phone Number *

 

Organization Name *

Department *

 

Requested quantity *

Country or Region *

      

Remarks

Bulk Inquiry

Inquiry Information

Product Name:
Saclofen
Cat. No.:
HY-100813
Quantity:
MCE Japan Authorized Agent:

Customer Review

Thank You for Your Feedback!

Request for HNMR Report

Please fill out this form to request the QC report. We will send it to your Email address shortly.

Your information is safe with us. * Required Fields.

Product Name

  

Lot #

Applicant Name *

 

Email Address *

Phone Number

 

Department *

Organization Name *

 

Country or Region *

Remarks

Request for HNMR Report

We have received your request and will respond to you as soon as possible.