Leramistat
Based on 1 Customer Validation
Leramistat (HMC-C-01-A; MBS2320) is a mitochondrial complex 1 inhibitor, involving in cell metabolism immune metabolism regulation. Leramistat also inhibits ATP production in Thp1 human monocytes (IC50: 0.63 μM). Leramistat inhibits atopic dermatitis and other skin diseases autoimmune diseases, inflammatory diseases, cancer; and also inhibits osteoclast mediated disease.
For research use only. We do not sell to patients.
- Purity: 98.00%
- CAS No.: 1642602-54-7
- Formula: C20H21ClN2O3S
- Molecular Weight:404.91
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Storage:
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Biological Activity
Mitochondrial complex 1[1]
Leramistat has moderate stability in rat hepatocytes, with a half-life of 7 min, and in human hepatocytes, a half-life of 154 min[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1642602-54-7
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Appearance Solid
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Molecular Weight 404.91
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Formula C20H21ClN2O3S
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Color Off-white to light yellow
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SMILES
N#CC1=C(C2=CC=C(C=C2)S(N[C@H]3CC[C@](O)(CC3)C)(=O)=O)C=CC(Cl)=C1
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Synonyms
HMC-C-01-A; MBS2320
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
Solvent & Solubility
DMSO : 100 mg/mL (246.97 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 (protect from light, stored under nitrogen). 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 (protect from light, stored under nitrogen). 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: ≥ 2.5 mg/mL (6.17 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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)
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.
Purity & Documentation
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Data Sheet (272 KB)
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SDS (392 KB)
- English - EN (392 KB)
- Français - FR (392 KB)
- Deutsch - DE (392 KB)
- Norwegian - NO (392 KB)
- Español - ES (392 KB)
- Swedish - SV (392 KB)
- Italian - IT (392 KB)
- Korean - KR (392 KB)
- Portuguese - PT (392 KB)
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Handling Instructions (2659 KB)
References
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 (protect from light, stored under nitrogen). 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 | 2.4697 mL | 12.3484 mL | 24.6968 mL | 61.7421 mL |
| 5 mM | 0.4939 mL | 2.4697 mL | 4.9394 mL | 12.3484 mL | |
| 10 mM | 0.2470 mL | 1.2348 mL | 2.4697 mL | 6.1742 mL | |
| 15 mM | 0.1646 mL | 0.8232 mL | 1.6465 mL | 4.1161 mL | |
| 20 mM | 0.1235 mL | 0.6174 mL | 1.2348 mL | 3.0871 mL | |
| 25 mM | 0.0988 mL | 0.4939 mL | 0.9879 mL | 2.4697 mL | |
| 30 mM | 0.0823 mL | 0.4116 mL | 0.8232 mL | 2.0581 mL | |
| 40 mM | 0.0617 mL | 0.3087 mL | 0.6174 mL | 1.5436 mL | |
| 50 mM | 0.0494 mL | 0.2470 mL | 0.4939 mL | 1.2348 mL | |
| 60 mM | 0.0412 mL | 0.2058 mL | 0.4116 mL | 1.0290 mL | |
| 80 mM | 0.0309 mL | 0.1544 mL | 0.3087 mL | 0.7718 mL | |
| 100 mM | 0.0247 mL | 0.1235 mL | 0.2470 mL | 0.6174 mL |