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

Saclofen  (Synonyms: サクロフェン)

製品番号: HY-100813 純度: 99.97%
COA 取扱説明書 Technical Support

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 構造式

CAS 番号 : 125464-42-8

容量 価格（税別） 在庫状況 数量
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in Water
ready for reconstitution
 USD 165 在庫あり
Solution
10 mM * 1 mL in Water USD 165 在庫あり
Solid
5 mg $150 在庫あり
10 mg $240 在庫あり
25 mg $460 在庫あり
50 mg $740 在庫あり
100 mg $1180 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

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Based on 5 publication(s) in Google Scholar

Other Forms of Saclofen:

Saclofen 関連抗体

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製品説明

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].

体外実験

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 関連抗体
体内実験

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.
分子量

249.72

分子式

C9H12ClNO3S
CAS 番号
Appearance

Solid

Color

White to off-white

SMILES

O=S(CC(CN)C1=CC=C(Cl)C=C1)(O)=O
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Powder -20°C 3 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

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
10 mM 0.4004 mL 2.0022 mL 4.0045 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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  • Dilution Calculator

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

一般には略語で表示されます：C1V1 = C2V2

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

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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).
純度とドキュメンテーション

純度: 99.97%

COA (252 KB)

取扱説明書 (2659 KB)
参考文献

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

  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

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

質量   濃度   体積   分子量 *
= × ×

The dilution calculator equation

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

一般には略語で表示されます：C1V1 = C2V2

濃度 （開始） × 体積 （開始） = 濃度 （終了） × 体積 （終了）
× = ×
C1   V1   C2   V2
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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