Pergolide mesylate
Based on 1 publication(s) in Google Scholar
Pergolide mesylate (Pergolide methanesulfonate), an Ergoline derivative, is a potent and orally active dopamine D1 and D2 receptors agonist. Pergolide mesylate can be used for Parkinson's disease and hyperprolactinaemia research.
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- Purity: 99.98%
- CAS No.: 66104-23-2
- 화학식: C20H30N2O3S2
- 분자량:410.59
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
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- References
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Publications Citing Use of MedChemExpress (MCE) Pergolide mesylate
MoreAll Dopamine Receptor Isoforms
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Biological Activity
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Cell Line
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Type | Value | Description | References |
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| Pituitary gland cell | IC50 |
0.07 nM
Compound: pergolide mesylate
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Inhibitory activity against prolactin release in rat anterior pituitary cells
Inhibitory activity against prolactin release in rat anterior pituitary cells
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[PMID: 6834383] |
Pergolide (10 nM-50 μM) mesylate treatment dose-dependently inhibits H2O2-induced cell death in SH-SY5Y neuroblastoma cells, acting in very low concentrations (nanomolar range) and in very early stages of the neurotoxic intracellular process[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SH-SY5Y cells
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Concentration:0.01 μM, 0.1 μM, 0.5 μM, 1 μM, 5 μM, 10 μM, 50 μM
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Incubation Time:Pretreated for 2 hours
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Result:Dose-dependently inhibited H2O2-induced cell death in SH-SY5Y neuroblastoma cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar rats (200-250 g) induced with 6-hydroxydopamine (6-OHDA)[3]
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Dosage:0.3 mg/kg
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Administration:Intraperitoneal injection; daily; 11 days
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Result:A reduced number of working/reference memory errors was observed. And significant decreased of MDA level.
Chemical Information
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CAS No. 66104-23-2
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Appearance Solid
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분자량 410.59
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화학식 C20H30N2O3S2
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Color White to off-white
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SMILES
[H][C@@]1(N(CCC)C[C@H](CSC)C[C@@]12[H])CC3=CNC4=CC=CC2=C43.CS(=O)(O)=O
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Synonyms
Pergolide methanesulfonate; LY127809
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Publications (1)
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Journal Impact Factor
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Most Recent
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Nature
2023 Dec;624(7992):672-681. PMID: 37935376
용액&용해도
DMSO : 50 mg/mL (121.78 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (281 KB)
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SDS (479 KB)
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Handling Instructions (2659 KB)
References
[1]. S Franks, et al. Effectiveness of pergolide mesylate in long term treatment of hyperprolactinaemia. Br Med J (Clin Res Ed). 1983 Apr 9;286(6372):1177-9. [Content Brief]
[2]. Daniela Uberti, et al. Pergolide protects SH-SY5Y cells against neurodegeneration induced by H(2)O(2). Eur J Pharmacol. 2002 Jan 2;434(1-2):17-20. [Content Brief]
[3]. Alin Ciobica, et al. The effects of pergolide on memory and oxidative stress in a rat model of Parkinson's disease. J Physiol Biochem. 2012 Mar;68(1):59-69. [Content Brief]
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 (sealed storage, away from moisture). 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 | 2.4355 mL | 12.1776 mL | 24.3552 mL | 60.8880 mL |
| 5 mM | 0.4871 mL | 2.4355 mL | 4.8710 mL | 12.1776 mL | |
| 10 mM | 0.2436 mL | 1.2178 mL | 2.4355 mL | 6.0888 mL | |
| 15 mM | 0.1624 mL | 0.8118 mL | 1.6237 mL | 4.0592 mL | |
| 20 mM | 0.1218 mL | 0.6089 mL | 1.2178 mL | 3.0444 mL | |
| 25 mM | 0.0974 mL | 0.4871 mL | 0.9742 mL | 2.4355 mL | |
| 30 mM | 0.0812 mL | 0.4059 mL | 0.8118 mL | 2.0296 mL | |
| 40 mM | 0.0609 mL | 0.3044 mL | 0.6089 mL | 1.5222 mL | |
| 50 mM | 0.0487 mL | 0.2436 mL | 0.4871 mL | 1.2178 mL | |
| 60 mM | 0.0406 mL | 0.2030 mL | 0.4059 mL | 1.0148 mL | |
| 80 mM | 0.0304 mL | 0.1522 mL | 0.3044 mL | 0.7611 mL | |
| 100 mM | 0.0244 mL | 0.1218 mL | 0.2436 mL | 0.6089 mL |
Pergolide mesylate Related Classifications
HY-13720A Related Classifications
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