(Rac)-Minzasolmin
Based on 1 Customer Validation
(Rac)-Minzasolmin ((Rac)-UCB0599; NPT200-11) is a blood-brain barrier penetrated alpha-synuclein (ASYN) misfolding inhibitor. (Rac)-Minzasolmin acts on the early stage of ASYN aggregation process, by replacing the membrane-bound oligomers ASYN, allowing them to revert to the monomeric form, while preventing pathological aggregation. (Rac)-Minzasolmin effectively improves the ASYN deposition in the retina and the neuro-pathological indicators in two α-synuclein transgenic mouse models. (Rac)-Minzasolmin can be used for the studies of Parkinson's disease (PD) and dementia with Lewy bodies (DLB).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.87%
- CAS 番号: 1802518-63-3
- 分子式: C23H31N5OS
- 分子量:425.59
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保管条件:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
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溶剤 & 溶解度
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
α-synuclein アイソフォーム固有の製品をすべて表示
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生物活性
製品説明
IC50 & Target
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α-synuclein Aggregation |
Parmacokinetics
体内実験
(Rac)-Minzasolmin (0.5-5 mg/kg, i.p., a Monday-Friday daily for approximately 90 days) reduces alpha-synuclein pathology in cortex, reduced associated neuroinflammation (astrogliosis), normalized striatal levels of the dopamine transporter (DAT) and improved motor function[1].
(Rac)-Minzasolmin (10 mg/kg, p.o., single dose) is well-absorbed in C57BL/6 mice and distributes readily into brain tissue with the Tmax in plasma and brain is observed to be 0.50 and 0.25 hr, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Over expressing human alpha synuclein models established in GFP fusion protein transgenic mice of the PDNG78 strain[1]
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Dosage:5 mg/kg
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Administration:Intraperitoneal injection (i.p.), once daily for 3 months
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Result:Significantly reduced the overexpressing fused ASYN-eGFP (ASYN::GFP) deposits after 2 months of treatment.
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Animal Model:Line 61 transgenic mouse model overexpressing human wild type ASYN[1]
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Dosage:0.5, 1 and 5 mg/kg
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Administration:Intraperitoneal injection (i.p.), a Monday-Friday daily for approximately 90 days
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Result:Significantly improved the behavioral performance of transgenic mice in the circular beam walking test. Significantly reduced total ASYN and proteinase K-resistant ASYN in the cortical neuroglia and neurons. Significantly restored the TH in the striatum and increased the DAT in the striatum. Significantly reduced neuroinflammation in the cerebral cortex and hippocampus, and restored the number of neurons.
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 1802518-63-3
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性状 Solid
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分子量 425.59
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分子式 C23H31N5OS
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Color White to off-white
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SMILES
O=C(C1=CN=C(N2CCN(CC2)C)S1)NC(CCCC)CC3=CNC4=CC=CC=C34
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別名
(Rac)-UCB0599; NPT200-11
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -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 (234.97 mM; Need ultrasonic; 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. 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
体内:
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: ≥ 2.5 mg/mL (5.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (5.87 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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.
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.
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.
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.
純度とドキュメンテーション
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データシート (275 KB)
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SDS (252 KB)
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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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3497 mL | 11.7484 mL | 23.4968 mL | 58.7420 mL |
| 5 mM | 0.4699 mL | 2.3497 mL | 4.6994 mL | 11.7484 mL | |
| 10 mM | 0.2350 mL | 1.1748 mL | 2.3497 mL | 5.8742 mL | |
| 15 mM | 0.1566 mL | 0.7832 mL | 1.5665 mL | 3.9161 mL | |
| 20 mM | 0.1175 mL | 0.5874 mL | 1.1748 mL | 2.9371 mL | |
| 25 mM | 0.0940 mL | 0.4699 mL | 0.9399 mL | 2.3497 mL | |
| 30 mM | 0.0783 mL | 0.3916 mL | 0.7832 mL | 1.9581 mL | |
| 40 mM | 0.0587 mL | 0.2937 mL | 0.5874 mL | 1.4685 mL | |
| 50 mM | 0.0470 mL | 0.2350 mL | 0.4699 mL | 1.1748 mL | |
| 60 mM | 0.0392 mL | 0.1958 mL | 0.3916 mL | 0.9790 mL | |
| 80 mM | 0.0294 mL | 0.1469 mL | 0.2937 mL | 0.7343 mL | |
| 100 mM | 0.0235 mL | 0.1175 mL | 0.2350 mL | 0.5874 mL |
(Rac)-Minzasolmin 関連分類
HY-125287 関連分類
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