LY2119620
Based on 1 Customer Validation
LY2119620 is a high-affinity muscarinic M2/M4 receptor agonist.
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.74%
- CAS. Nr.: 886047-22-9
- Formel: C19H24ClN5O3S
- Molecular Weight:437.94
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Speicherung:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Protokoll
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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mAChR2 |
mAChR4 |
LY2119620 shows a modest allosteric agonism of 23.2±2.18% and 16.8±5.01% at the M2 and M4 receptors, respectively. Minimal allosteric agonism (<20%) is observed for LY2119620 at the M1, M3, and M5 receptors. The variable KB of LY2119620 for the allosteric binding site on the unoccupied receptor is found to be consistently about 1.9 to 3.4 μM. Results show a Bmax increase at the M2 receptor from 793±1.95 fmol/mg to 2850±162 fmol/mg upon addition of 10 μM LY2119620, and about a 5-fold increase in Bmax at the M4 receptor, 284±18.3 fmol/mg to 1340±42.2 fmol/mg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS. Nr. 886047-22-9
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Appearance Solid
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Molecular Weight 437.94
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Formel C19H24ClN5O3S
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Color White to light yellow
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SMILES
NC1=C(C(NC2CC2)=O)SC3=C1C(C)=C(Cl)C(OCC(N4CCN(C)CC4)=O)=N3
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Lösungsmittel & Löslichkeit
DMSO : 67.5 mg/mL (154.13 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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 (5.71 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.
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.
Protokoll
[3H]LY2119620 equilibrium binding is achieved by incubating 15 µg membranes, orthosteric ligand (100 µM), and various concentrations of [3H]LY2119620 (0.2 to 60 nM) for 1 hour at 25°C. The specific binding versus time data are fit to a one-site specific binding model, and the Bmax and Kd for the allosteric molecule are calculated for each orthosteric ligand[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Reinheit & Dokumentation
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Data Sheet (272 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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Handling Instructions (2659 KB)
Verweise
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2834 mL | 11.4171 mL | 22.8342 mL | 57.0854 mL |
| 5 mM | 0.4567 mL | 2.2834 mL | 4.5668 mL | 11.4171 mL | |
| 10 mM | 0.2283 mL | 1.1417 mL | 2.2834 mL | 5.7085 mL | |
| 15 mM | 0.1522 mL | 0.7611 mL | 1.5223 mL | 3.8057 mL | |
| 20 mM | 0.1142 mL | 0.5709 mL | 1.1417 mL | 2.8543 mL | |
| 25 mM | 0.0913 mL | 0.4567 mL | 0.9134 mL | 2.2834 mL | |
| 30 mM | 0.0761 mL | 0.3806 mL | 0.7611 mL | 1.9028 mL | |
| 40 mM | 0.0571 mL | 0.2854 mL | 0.5709 mL | 1.4271 mL | |
| 50 mM | 0.0457 mL | 0.2283 mL | 0.4567 mL | 1.1417 mL | |
| 60 mM | 0.0381 mL | 0.1903 mL | 0.3806 mL | 0.9514 mL | |
| 80 mM | 0.0285 mL | 0.1427 mL | 0.2854 mL | 0.7136 mL | |
| 100 mM | 0.0228 mL | 0.1142 mL | 0.2283 mL | 0.5709 mL |
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