2. Sarizotan

Sarizotan  (Synonyms: EMD 128130)

Cat. No.: HY-100820 Purity: 98.74%
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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 Chemical Structure

Sarizotan Chemical Structure

CAS No. : 351862-32-3

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Solid or liquid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 275 In-stock
Solution
10 mM * 1 mL in DMSO USD 275 In-stock
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5 mg USD 250 In-stock
10 mg USD 380 In-stock
25 mg USD 750 In-stock
50 mg USD 1200 In-stock
100 mg USD 1950 In-stock
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Sarizotan Related Antibodies

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Description

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].

In Vitro

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 Related Antibodies
In Vivo

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).
Clinical Trial
Molecular Weight

348.41

Formula

C22H21FN2O
CAS No.
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
Shipping

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

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

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This equation is commonly abbreviated as: C1V1 = C2V2

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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
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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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-128130Inhibitorinhibitorinhibit

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