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

Saclofen is an orally active and a competitive GABAB receptor antagonist with an IC50 of 7.8 μM. Saclofen has weak antagonistic effects on GABAB1b and GABAB2 heterodimeric recombinant receptors. Saclofen inhibits the binding of Baclofen (HY-B0007) to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts, and exhibits anti-inflammatory and analgesic effects in rats.

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Saclofen

Saclofen 화학구조

CAS No. : 125464-42-8

사이즈 가격 재고 수량
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
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Solution
10 mM * 1 mL in Water 해외재고보유
Solid
5 mg 해외재고보유
10 mg 해외재고보유
25 mg 해외재고보유
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200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 5 publication(s) in Google Scholar

Other Forms of Saclofen:

Saclofen Related Antibodies

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  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

Saclofen is an orally active and a competitive GABAB receptor antagonist with an IC50 of 7.8 μM. Saclofen has weak antagonistic effects on GABAB1b and GABAB2 heterodimeric recombinant receptors. Saclofen inhibits the binding of Baclofen (HY-B0007) to rat cerebellar membranes and blocks Baclofen-induced circadian phase shifts, and exhibits 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 (50 μg/10 μL/rat, i.c.) 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: 50 μg/10 μL/rat
Administration: i.c.
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.
분자량

249.72

화학식

C9H12ClNO3S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=S(CC(CN)C1=CC=C(Cl)C=C1)(O)=O
선적

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

H2O : 10 mg/mL (40.04 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 4.0045 mL 20.0224 mL 40.0448 mL
5 mM 0.8009 mL 4.0045 mL 8.0090 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.

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

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

This equation is commonly abbreviated as: C1V1 = C2V2

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C2

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V2

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

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순도&문서

Purity: 99.97%

SDS (394 KB)

COA (252 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 4.0045 mL 20.0224 mL 40.0449 mL 100.1121 mL
5 mM 0.8009 mL 4.0045 mL 8.0090 mL 20.0224 mL
10 mM 0.4004 mL 2.0022 mL 4.0045 mL 10.0112 mL
15 mM 0.2670 mL 1.3348 mL 2.6697 mL 6.6741 mL
20 mM 0.2002 mL 1.0011 mL 2.0022 mL 5.0056 mL
25 mM 0.1602 mL 0.8009 mL 1.6018 mL 4.0045 mL
30 mM 0.1335 mL 0.6674 mL 1.3348 mL 3.3371 mL
40 mM 0.1001 mL 0.5006 mL 1.0011 mL 2.5028 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.

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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

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상품명:
Saclofen
Cat. No.:
HY-100813
수량:
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