Fulacimstat
Based on 2 publication(s) in Google Scholar
Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.
For research use only. We do not sell to patients.
- Purity: 99.86%
- CAS No.: 1488354-15-9
- Formula: C23H16F3N3O6
- Molecular Weight:487.38
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Fulacimstat
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Biological Activity
IC50: 4 nM (human chymase enzyme), 3 nM (hamster chymase enzyme)[1][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. 1488354-15-9
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Appearance Solid
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Molecular Weight 487.38
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Formula C23H16F3N3O6
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Color White to off-white
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SMILES
O=C(N(C1=CC=C(N2C)C(OC2=O)=C1)C=C(C(O)=O)C3=O)N3[C@H]4C5=CC=CC(C(F)(F)F)=C5CC4
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Synonyms
BAY1142524
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (2)
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Journal Impact Factor
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Most Recent
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J Med Entomol
Mouse chymase mast cell protease-4 facilitates blood feeding of Aedes aegypti (Diptera: Culicidae) mosquitoes. [Abstract]2025 Oct 21:tjaf137. PMID: 41117697 -
Solvent & Solubility
DMSO : 50 mg/mL (102.59 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.
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 (5.13 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: ≥ 0.5 mg/mL (1.03 mM); Clear solution
This protocol yields a clear solution of ≥ 0.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (5.0 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:
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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.
Purity & Documentation
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Data Sheet (275 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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, 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 |
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| DMSO | 1 mM | 2.0518 mL | 10.2589 mL | 20.5179 mL | 51.2947 mL |
| 5 mM | 0.4104 mL | 2.0518 mL | 4.1036 mL | 10.2589 mL | |
| 10 mM | 0.2052 mL | 1.0259 mL | 2.0518 mL | 5.1295 mL | |
| 15 mM | 0.1368 mL | 0.6839 mL | 1.3679 mL | 3.4196 mL | |
| 20 mM | 0.1026 mL | 0.5129 mL | 1.0259 mL | 2.5647 mL | |
| 25 mM | 0.0821 mL | 0.4104 mL | 0.8207 mL | 2.0518 mL | |
| 30 mM | 0.0684 mL | 0.3420 mL | 0.6839 mL | 1.7098 mL | |
| 40 mM | 0.0513 mL | 0.2565 mL | 0.5129 mL | 1.2824 mL | |
| 50 mM | 0.0410 mL | 0.2052 mL | 0.4104 mL | 1.0259 mL | |
| 60 mM | 0.0342 mL | 0.1710 mL | 0.3420 mL | 0.8549 mL | |
| 80 mM | 0.0256 mL | 0.1282 mL | 0.2565 mL | 0.6412 mL | |
| 100 mM | 0.0205 mL | 0.1026 mL | 0.2052 mL | 0.5129 mL |
Fulacimstat Related Classifications
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