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> Camostat (mesylate) [59721-29-8]

Camostat (mesylate) [59721-29-8]

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Katalog-Nummer HY-13512-100mg

Size : 100mg

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Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase.

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Camostat mesylate Chemische Struktur

Camostat mesylate Chemische Struktur

CAS. Nr. : 59721-29-8

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

Based on 28 publication(s) in Google Scholar

Beschreibung

Camostat mesylate (Camostat mesilate) is an orally active, synthetic serine protease inhibitor for chronic pancreatitis. Camostat mesylate, an inhibitor of TMPRSS2, shows antiviral activity against SARS-CoV-2. Camostat mesylate also inhibits the activity of prostasin, trypsin, and matriptase[1][2][3].

In Vitro

Camostat mesylate (Camostat mesilate) inhibits both monocyte chemoattractant protein-1 (MCP-1) and TNF-α production from monocytes, and proliferation and MCP-1 production from PSCs[1].
? Camostat mesylate, a trypsin-like protease inhibitor, provides a potent (IC50=50 nM) and prolongs attenuation of ENaC function in human airway epithelial cell models that is reversible upon the addition of excess trypsin[3].

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

Camostat mesylate Related Antibodies
In Vivo

Camostat mesilate (30 mg/kg; p.o.; twice a day for 9 days) blocks the spread and pathogenesis of SARS-CoV in a pathogenic mouse model[4].

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

Animal Model: 6-8 week old female BALB/c mice (lethal SARS-CoV infection model)[4]
Dosage: 30 mg/kg
Administration: P.o.; twice a day for 9 days
Result: Effective in protecting mice against death due to a lethal infection by SARS-CoV, with a survival rate of ∼60%.
Klinische Studie
Molekulargewicht

494.52

Formel

C21H26N4O8S
CAS. Nr.

59721-29-8
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCC(N(C)C)=O)CC1=CC=C(OC(C2=CC=C(NC(N)=N)C=C2)=O)C=C1.CS(=O)(O)=O
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, sealed storage, away from moisture

*In solvent : -80°C, 1 year; -20°C, 6 months (sealed storage, away from moisture)

Lösungsmittel & Löslichkeit
In Vitro: 

DMSO : 125 mg/mL (252.77 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H2O : ≥ 50 mg/mL (101.11 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0222 mL 10.1108 mL 20.2216 mL
5 mM 0.4044 mL 2.0222 mL 4.0443 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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

  • Molaritätsrechner

  • Verdünnungsrechner

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: ≥ 2.08 mg/mL (4.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.21 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.

For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
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:  PBS

    Solubility: 12.5 mg/mL (25.28 mM); Clear solution; Need ultrasonic

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.
Calculation results:
Working solution concentration: mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
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).
Reinheit & Dokumentation

Purity: 99.93%

COA (246 KB) LCMS (93 KB)

Handling Instructions (2659 KB)
Verweise

  • [1]. Gibo J, et al. Camostat mesilate attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity. Lab Invest. 2005;85(1):75‐89.  [Content Brief]

    [2]. Uno Y. Camostat mesilate therapy for COVID-19 [published online ahead of print, 2020 Apr 29]. Intern Emerg Med. 2020;1‐2.  [Content Brief]

    [3]. Coote K, et al. Camostat attenuates airway epithelial sodium channel function in vivo through the inhibition of a channel-activating protease. J Pharmacol Exp Ther. 2009;329(2):764‐774.  [Content Brief]

    [4]. Zhou Y, Vedantham P, Lu K, et al. Protease inhibitors targeting coronavirus and filovirus entry. Antiviral Res. 2015;116:76‐84.  [Content Brief]

  • [1]. Gibo J, et al. Camostat mesilate attenuates pancreatic fibrosis via inhibition of monocytes and pancreatic stellate cells activity. Lab Invest. 2005;85(1):75‐89.

    [2]. Uno Y. Camostat mesilate therapy for COVID-19 [published online ahead of print, 2020 Apr 29]. Intern Emerg Med. 2020;1‐2.

    [3]. Coote K, et al. Camostat attenuates airway epithelial sodium channel function in vivo through the inhibition of a channel-activating protease. J Pharmacol Exp Ther. 2009;329(2):764‐774.

    [4]. Zhou Y, Vedantham P, Lu K, et al. Protease inhibitors targeting coronavirus and filovirus entry. Antiviral Res. 2015;116:76‐84.

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, 1 year; -20°C, 6 months (sealed storage, away from moisture). When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
H2O / DMSO 1 mM 2.0222 mL 10.1108 mL 20.2216 mL 50.5541 mL
5 mM 0.4044 mL 2.0222 mL 4.0443 mL 10.1108 mL
10 mM 0.2022 mL 1.0111 mL 2.0222 mL 5.0554 mL
15 mM 0.1348 mL 0.6741 mL 1.3481 mL 3.3703 mL
20 mM 0.1011 mL 0.5055 mL 1.0111 mL 2.5277 mL
25 mM 0.0809 mL 0.4044 mL 0.8089 mL 2.0222 mL
30 mM 0.0674 mL 0.3370 mL 0.6741 mL 1.6851 mL
40 mM 0.0506 mL 0.2528 mL 0.5055 mL 1.2639 mL
50 mM 0.0404 mL 0.2022 mL 0.4044 mL 1.0111 mL
60 mM 0.0337 mL 0.1685 mL 0.3370 mL 0.8426 mL
80 mM 0.0253 mL 0.1264 mL 0.2528 mL 0.6319 mL
100 mM 0.0202 mL 0.1011 mL 0.2022 mL 0.5055 mL

* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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Camostat mesylate Related Classifications

Help & FAQs

Keywords:

Camostat59721-29-8Camostat mesilate FOY305 FOY-S980FOY305FOY 305FOY-305Ser/Thr ProteaseSARS-CoVSerine proteasesSerine endopeptidasesThreonine proteasesSARS coronavirusoralchronicpancreatitisTMPRSS2virusSARS-CoV-2coronavirusInhibitorinhibitorinhibit

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