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| 10mg |
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| 25mg |
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Purity: ≥98%
Fulacimstat (also known as BAY1142524) is a novel, potent and orally bioavailable chymase inhibitor that has IC50 values of 4 and 3 nM for the chymase enzymes in hamsters and humans, respectively. Fulacimstat is being developed as a first-in-class treatment for left-ventricular dysfunction following myocardial infarction. It has the potential to be used as an antifibrotic drug candidate.
| Targets |
human chymase enzyme (IC50 = 4 nM); hamster chymase enzyme (IC50 = 3 nM)
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|---|---|
| ln Vitro |
Fulacimstat inhibits the chymase enzyme in humans and hamsters, with IC50 values of 4 nM and 3 nM, respectively[1][2].
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| ln Vivo |
In hamsters, isoprenaline causes 24.4±1.8% cardiac fibrosis, which is dose-dependently decreased by enalapril (17.7±1.5% at 20 mg/kg) and Fulacimstat (16.4±1.2%, 12.4 ± 1.3%, and 10.9±1.4% at 1, 3 and 10 mg/kg, respectively). The hearts of hamsters exhibit reduced relaxation and contractility, along with an increase in end diastolic pressure, four weeks after MI. Without affecting blood pressure or heart rate, fulacimstat at 10 mg/kg significantly reduced the end diastolic pressure (13.2±1.4 mmHg) in comparison to placebo (19.3±2 mmHg). Additionally, Fulacimstat treatment improves the cardiac response to adrenergic stimulation and reduces the fibrotic area[1].
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| Animal Protocol |
Male Syrian hamstersC
10 mg/kg p.o. |
| References |
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| Molecular Formula |
C23H16F3N3O6
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|---|---|
| Molecular Weight |
487.38485622406
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| Exact Mass |
487.10
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| Elemental Analysis |
C, 56.68; H, 3.31; F, 11.69; N, 8.62; O, 19.70
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| CAS # |
1488354-15-9
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| Related CAS # |
1488354-15-9
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| Appearance |
Solid powder
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| SMILES |
CN1C2=C(C=C(C=C2)N3C=C(C(=O)N(C3=O)[C@@H]4CCC5=C4C=CC=C5C(F)(F)F)C(=O)O)OC1=O
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| InChi Key |
JDARDSVOVYVQST-MRXNPFEDSA-N
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| InChi Code |
InChI=1S/C23H16F3N3O6/c1-27-17-7-5-11(9-18(17)35-22(27)34)28-10-14(20(31)32)19(30)29(21(28)33)16-8-6-12-13(16)3-2-4-15(12)23(24,25)26/h2-5,7,9-10,16H,6,8H2,1H3,(H,31,32)/t16-/m1/s1
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| Chemical Name |
1-(3-methyl-2-oxo-1,3-benzoxazol-6-yl)-2,4-dioxo-3-[(1R)-4-(trifluoromethyl)-2,3-dihydro-1H-inden-1-yl]pyrimidine-5-carboxylic acid
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| Synonyms |
BAY1142524; BAY 1142524; BAY-1142524; Fulacimstat
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 50~97 mg/mL (102.6~199.0 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.13 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (1.03 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (1.03 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0518 mL | 10.2589 mL | 20.5179 mL | |
| 5 mM | 0.4104 mL | 2.0518 mL | 4.1036 mL | |
| 10 mM | 0.2052 mL | 1.0259 mL | 2.0518 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT03412006 | Completed | Drug: Fulacimstat (BAY1142524) Drug: Placebo |
Diabetic Kidney Disease | Bayer | February 2, 2018 | Phase 2 |
| NCT02976467 | Completed | Drug: Fulacimstat (BAY1142524) Drug: Placebo |
Myocardial Infarction | Bayer | December 30, 2016 | Phase 2 |
| NCT03402438 | Completed | Drug: Fulacimstat (BAY1142524) |
Clinical Trial, Phase I | Bayer | February 12, 2018 | Phase 1 |
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