Morcamilast
Based on 1 Customer Validation
Morcamilast (ME3183) is a selective and orally active PDE4 inhibitor, with IC50s of 1.28 nM (PDE4A1A), 2.33 nM (PDE4B1), and 1.63 nM (PDE4D2) respectively. Morcamilast shows weak inhibition of PDEs other than PDE4s Morcamilast is an anti-inflammatory agent and inhibits LPS (HY-D1056)-induced release of TNF-α, IL-12/23p40, IL-23, and IL-17A in human PBMCs and T cells. Morcamilast has antipruritic effect and can be used in the study of psoriasis, atopic dermatitis, and other inflammatory diseases.
For research use only. We do not sell to patients.
- Purity: 98.92%
- CAS No.: 2231329-25-0
- Formula: C19H20F2N4O3S
- Molecular Weight:422.45
-
Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
-
Immunology/Inflammation Compound Library
HY-L007
-
Metabolism/Protease Compound Library
HY-L012
-
Anti-Cancer Compound Library
HY-L025
-
Clinical Compound Library
HY-L026
-
Drug Repurposing Compound Library
HY-L035
-
Differentiation Inducing Compound Library
HY-L038
-
Orally Active Compound Library
HY-L061
-
Anti-Alzheimer's Disease Compound Library
HY-L069
-
Neurodegenerative Disease-related Compound Library
HY-L086
-
Angiogenesis-Related Compound Library
HY-L088
-
Anti-Colorectal Cancer Compound Library
HY-L103
-
Antidepressant Compound Library
HY-L108
-
Cancer Stem Cells Compound Library
HY-L135
-
Pain-Related Compound Library
HY-L139
-
Metabolic Enzyme Compound Library
HY-L146
-
Autoimmune Disease Compound Library
HY-L156
-
Highly Selective Inhibitors Library
HY-L158
-
Cytokine Inhibitors Library
HY-L161
-
Multi-Target Compound Library
HY-L176
-
Radioprotector Library
HY-L178
-
Bioactive Compound Library Max
HY-L181
-
MCE Bioactive Compound Library
HY-L001V
-
Drug Repurposing Compound Library Plus
HY-L035P
-
Clinical Compound Library Plus
HY-L026P
-
Bioactive Compound Library
HY-L001
-
Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library
HY-L199
-
High-Throughput Bioactive Compound Library
HY-L205
Biological Activity
|
PDE4A1 1.28 nM (IC50) |
PDE4B1 2.33 nM (IC50) |
PDE4D2 1.63 nM (IC50) |
PDE10A2 453 nM (IC50) |
PDE2A 1810 nM (IC50) |
PDE3A 2950 nM (IC50) |
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
-
CAS No. 2231329-25-0
-
Appearance Solid
-
Molecular Weight 422.45
-
Formula C19H20F2N4O3S
-
Color White to off-white
-
SMILES
FC(F)(C(C)(C)O)OC1=C(N=C(O2)N3CC4CC(C3)N4)C2=C(C=C1)C5=NC=CS5
-
Synonyms
ME3183; PDE4-IN-14
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (236.71 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)
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: ≥ 5 mg/mL (11.84 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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: ≥ 5 mg/mL (11.84 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Please enter the basic information of animal experiments:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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.
Purity & Documentation
-
Data Sheet (276 KB)
-
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
-
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. 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 | 2.3671 mL | 11.8357 mL | 23.6714 mL | 59.1786 mL |
| 5 mM | 0.4734 mL | 2.3671 mL | 4.7343 mL | 11.8357 mL | |
| 10 mM | 0.2367 mL | 1.1836 mL | 2.3671 mL | 5.9179 mL | |
| 15 mM | 0.1578 mL | 0.7890 mL | 1.5781 mL | 3.9452 mL | |
| 20 mM | 0.1184 mL | 0.5918 mL | 1.1836 mL | 2.9589 mL | |
| 25 mM | 0.0947 mL | 0.4734 mL | 0.9469 mL | 2.3671 mL | |
| 30 mM | 0.0789 mL | 0.3945 mL | 0.7890 mL | 1.9726 mL | |
| 40 mM | 0.0592 mL | 0.2959 mL | 0.5918 mL | 1.4795 mL | |
| 50 mM | 0.0473 mL | 0.2367 mL | 0.4734 mL | 1.1836 mL | |
| 60 mM | 0.0395 mL | 0.1973 mL | 0.3945 mL | 0.9863 mL | |
| 80 mM | 0.0296 mL | 0.1479 mL | 0.2959 mL | 0.7397 mL | |
| 100 mM | 0.0237 mL | 0.1184 mL | 0.2367 mL | 0.5918 mL |
Powered by Bioz