2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor Dopamine Receptor
  4. Sarizotan

Sarizotan  (Synonyms: EMD 128130)

製品番号: HY-100820 純度: 98.23%
COA 取扱説明書 Technical Support

Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively.

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Sarizotan

Sarizotan 構造式

CAS 番号 : 351862-32-3

容量 価格（税別） 在庫状況 数量
Solid or liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 275 在庫あり
Solution
10 mM * 1 mL in DMSO USD 275 在庫あり
Solid or liquid
5 mg $250 在庫あり
10 mg $380 在庫あり
25 mg $750 在庫あり
50 mg $1200 在庫あり
100 mg $1950 在庫あり
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

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Based on 1 publication(s) in Google Scholar

Other Forms of Sarizotan:

Sarizotan 関連抗体

Top Publications Citing Use of Products

5-HT Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
5-HT Receptor 5-HT1 Receptor 5-HT2 Receptor 5-HT3 Receptor 5-HT4 Receptor 5-HT5 Receptor 5-HT6 Receptor 5-HT7 Receptor

Dopamine Receptor アイソフォーム固有の製品をすべて表示:

すべてのアイソフォームを表示
Dopamine Receptor D1 Receptor D2 Receptor D3 Receptor D4 Receptor D5 Receptor

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製品説明

Sarizotan (EMD 128130) is an orally active serotonin 5-HT1A receptor and dopamine receptor agonist. Sarizotan (EMD 128130) exhibits IC50 values of 6.5 nM (rat 5-HT1A), 0.1 nM (human 5-HT1A), 15.1 nM (rat D2), 17 nM (human D2), 6.8 nM (human D3) and 2.4 nM (human D4.2), respectively[1].

IC50 & Target[1]

5-HT1A Receptor

6.5 nM (IC50, rat)

5-HT1A Receptor

 

5-HT1A Receptor

0.1 nM (IC50, human)

rD2 Receptor

15.1 nM (IC50, rat)

D3 Receptor

6.8 nM (IC50, human)

5-HT1B Receptor

600 nM (IC50, rat)

5-HT1D Receptor

500 nM (IC50, calf)

5-HT2A Receptor

960 nM (IC50, rat, agonist site)

5-HT2A Receptor

587 nM (IC50, human, antagonist site)

5-HT2B Receptor

108 nM (IC50, human)

5-HT2C Receptor

800 nM (IC50, pig)

5-HT3 Receptor

3500 nM (IC50, NG 108 cells)

5-HT5A Receptor

313 nM (IC50, human)

5-HT6 Receptor

3300 nM (IC50, human)

5-HT7 Receptor

10 nM (IC50, human)

hD4.2 Receptor

2.4 nM (IC50)

hD2 Receptor

17 nM (IC50)

体外実験

Sarizotan concentration-dependently inhibits the electrically-induced contractions with an IC50 value of 150 nM (Emax 40% at 1 mM) [1].

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

Sarizotan 関連抗体
体内実験

Sarizotan (3, 10 mg/kg, po) at the higher dose slightly decreases 5-HT in the striatum and its metabolite 5-HIAA in frontal cortex and hippocampus. Sarizotan (10 mg/kg, po) substantially increases the DA metabolites DOPAC and HVA in the striatum and frontal cortex[1].
Sarizotan represents a new approach for the treatment of extrapyramidal motor complications such as l-DOPA-induced dyskinesia in Parkinson’s disease[1].
Sarizotan (10 ng and 1 μg, local administration) attenuates levodopa-induced dyskinesias in 6-OHDA-lesioned rats[2].

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

Animal Model: Male Sprague-Dawley rats weighing 220-240 g (exhibiting a vigorous rotational response)[2].
Dosage: 1 ng, 10 ng and 1 μg in 0.3 μL solution.
Administration: Administered via an injection cannula inserted to the guide cannula through the STN (V -8.4 mm from skull) with the injection cannula connected to a 10-μL syringe and mounted on a microinfusion pump for 22 consecutive days.
Result: On day 23, the subthalamic administration of Sarizotan at the higher doses tested (10 ng and 1 μg) significantly decreased the total dyskinesia score in levodopa-treated rats in comparison with the rats treated only with levodopa (p<0.05, p<0.01, respectively).
臨床実験
分子量

348.41

分子式

C22H21FN2O
CAS 番号
Appearance

Viscous Liquid

Color

Colorless to light yellow

SMILES

FC1=CC=C(C2=CN=CC(CNC[C@H]3CCC4=CC=CC=C4O3)=C2)C=C1
輸送条件

Room temperature in continental US; may vary elsewhere.
保管条件
Pure form -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
溶剤 & 溶解度
体外: 

DMSO : 100 mg/mL (287.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8702 mL 14.3509 mL 28.7018 mL
5 mM 0.5740 mL 2.8702 mL 5.7404 mL
10 mM 0.2870 mL 1.4351 mL 2.8702 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.

  • Molarity Calculator

  • Dilution Calculator

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

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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

濃度 （開始）

C1

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体積 （開始）

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

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
純度とドキュメンテーション
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
DMSO 1 mM 2.8702 mL 14.3509 mL 28.7018 mL 71.7545 mL
5 mM 0.5740 mL 2.8702 mL 5.7404 mL 14.3509 mL
10 mM 0.2870 mL 1.4351 mL 2.8702 mL 7.1755 mL
15 mM 0.1913 mL 0.9567 mL 1.9135 mL 4.7836 mL
20 mM 0.1435 mL 0.7175 mL 1.4351 mL 3.5877 mL
25 mM 0.1148 mL 0.5740 mL 1.1481 mL 2.8702 mL
30 mM 0.0957 mL 0.4784 mL 0.9567 mL 2.3918 mL
40 mM 0.0718 mL 0.3588 mL 0.7175 mL 1.7939 mL
50 mM 0.0574 mL 0.2870 mL 0.5740 mL 1.4351 mL
60 mM 0.0478 mL 0.2392 mL 0.4784 mL 1.1959 mL
80 mM 0.0359 mL 0.1794 mL 0.3588 mL 0.8969 mL
100 mM 0.0287 mL 0.1435 mL 0.2870 mL 0.7175 mL
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Sarizotan 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:

Sarizotan351862-32-3EMD 128130EMD128130EMD-1281305-HT ReceptorDopamine ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorParkinson’sdiseaseDOPAdyskinesiaInhibitorinhibitorinhibit

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製品名:
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製品番号:
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