ML381
Based on 1 Customer Validation
ML381 (VU0488130) is a highly selective, central nervous system penetrant mAChR M5 orthogonal antagonist (IC50 = 450 nM; Ki = 340 nM). ML381 is unstable in rat plasma and can be mainly used as a molecular probe for in vitro and electrophysiological studies.
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- Pureté : 99.87%
- CAS No.: 1623481-80-0
- Formule: C21H21N3O4
- Masse moléculaire:379.41
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Stockage:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
Description
IC50 & Target
IC50: 450 nM (mAChR M5)[1].
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Sprague-Dawley rat[1].
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Dosage:0.2 mg/kg
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Administration:Intravenous injection; single.
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Result:
1.19 Pharmacokinetic Parameters of ML381 in Sprague-Dawley rat[1].
*Kp value was determined at 0.25 h following a 0.2 mg/kg IV dose (n=2).IV (0.2 mg/kg) Hepatic microsomal CLint (mL min-1 kg-1) 770 Predicted CLhep (mL min-1 kg-1) 64 fubrain 0.14 Cbrain/Cplasma (Kp*) 0.58
Chemical Information
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CAS No. 1623481-80-0
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Appearance Oil
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Masse moléculaire 379.41
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Formule C21H21N3O4
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Color Colorless to light yellow
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SMILES
O=C(C1=NOC(COC2=CC=CC(C(C)=O)=C2)=C1)N(C)[C@H](C3=NC=CC=C3)C
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Synonyms
VU0488130
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (263.57 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 (6.59 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 (6.59 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.
Pureté et documentation
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Fiche technique (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instruction de manipulation (2659 KB)
Références
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 |
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| DMSO | 1 mM | 2.6357 mL | 13.1784 mL | 26.3567 mL | 65.8918 mL |
| 5 mM | 0.5271 mL | 2.6357 mL | 5.2713 mL | 13.1784 mL | |
| 10 mM | 0.2636 mL | 1.3178 mL | 2.6357 mL | 6.5892 mL | |
| 15 mM | 0.1757 mL | 0.8786 mL | 1.7571 mL | 4.3928 mL | |
| 20 mM | 0.1318 mL | 0.6589 mL | 1.3178 mL | 3.2946 mL | |
| 25 mM | 0.1054 mL | 0.5271 mL | 1.0543 mL | 2.6357 mL | |
| 30 mM | 0.0879 mL | 0.4393 mL | 0.8786 mL | 2.1964 mL | |
| 40 mM | 0.0659 mL | 0.3295 mL | 0.6589 mL | 1.6473 mL | |
| 50 mM | 0.0527 mL | 0.2636 mL | 0.5271 mL | 1.3178 mL | |
| 60 mM | 0.0439 mL | 0.2196 mL | 0.4393 mL | 1.0982 mL | |
| 80 mM | 0.0329 mL | 0.1647 mL | 0.3295 mL | 0.8236 mL | |
| 100 mM | 0.0264 mL | 0.1318 mL | 0.2636 mL | 0.6589 mL |
ML381 Related Classifications
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