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Fulacimstat  (Synonyms: BAY1142524)

Cat. No.: HY-109059 Purity: 99.92%
COA Handling Instructions

Molarity Calculator

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.

Fulacimstat Chemical Structure

Fulacimstat Chemical Structure

CAS No. : 1488354-15-9

Size Price Stock Quantity
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 375 In-stock
Solution
10 mM * 1 mL in DMSO USD 375 In-stock
Solid
1 mg USD 166 In-stock
5 mg USD 350 In-stock
10 mg USD 500 In-stock
25 mg USD 950 In-stock
50 mg USD 1650 In-stock
100 mg USD 2450 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Fulacimstat Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Fulacimstat

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Fulacimstat is an orally available chymase inhibitor, with IC50s of 4, 3 nM for human and hamster chymase enzyme, respectively.

IC50 & Target

IC50: 4 nM (human chymase enzyme), 3 nM (hamster chymase enzyme)[1][2].
In Vitro

Fulacimstat inhibits human and hamster chymase enzyme with IC50s of 4 nM and 3 nM, respectively[1][2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Fulacimstat Related Antibodies
In Vivo

Isoprenaline induces cardiac fibrosis (24.4±1.8%) in hamsters, which is reduced dose dependently by Fulacimstat (16.4±1.2%, 12.4 ± 1.3%, 10.9±1.4% at 1, 3 and 10 mg/kg respectively) and by enalapril (17.7±1.5% at 20 mg/kg). Four weeks after MI, hamster hearts show an increased end diastolic pressure, and reduce contractility and relaxation. Compared to placebo (19.3±2 mmHg), Fulacimstat at 10 mg/kg reduce significantly the end diastolic pressure (13.2±1.4 mmHg) without any effects on blood pressure or heart rate. Moreover, treatment with Fulacimstat reduce the fibrotic area and improve the cardiac response to adrenergic stimulation[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

487.38

Formula

C23H16F3N3O6
CAS No.
Appearance

Solid

Color

White to off-white

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

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)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the 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.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
  • Protocol 2

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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

Purity: 99.92%

COA (250 KB) HNMR (271 KB) LCMS (94 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, 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 2.0518 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
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Fulacimstat Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Fulacimstat1488354-15-9BAY1142524BAY 1142524BAY-1142524OthersInhibitorinhibitorinhibit

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