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> Calpeptin [117591-20-5]

Calpeptin [117591-20-5]

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Referentie HY-100223-5mg

Formaat : 5mg

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Calpeptine est un inhibiteur puissant de la calpaïne pénétrant dans les cellules, avec un ID50 de 40 nM pour la Calpain I dans les plaquettes humaines. Calpeptine est également un inhibiteur de la cathepsine K.

Calpeptin ist ein starker, zelldurchdringender calpain-Inhibitor mit einer ID50 von 40 nM für Calpain I in menschlichen Blutplättchen. Calpeptin ist auch ein Inhibitor von cathepsin K.

Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets. Calpeptin is also an inhibitor of cathepsin K.

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Calpeptin Chemical Structure

Calpeptin Chemical Structure

CAS No. : 117591-20-5

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

Based on 22 publication(s) in Google Scholar

Voir tous les produits spécifiques à Isoform Cathepsin:

Voir toutes les isoformes
Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S
Description

Calpeptin is a potent, cell penetrating calpain inhibitor, with an ID50 of 40 nM for Calpain I in human platelets[1]. Calpeptin is also an inhibitor of cathepsin K[2].

IC50 & Target

cathepsin K

 

In Vitro

Calpeptin (0-100 nM, 24 hours) treatment suppresses the proliferation of both WI38 VA13 and IMR90 cells in a dose-dependent manner. Calpeptin (1000 pg/ml, 24 hours) inhibits IL-6-induced cell proliferation of lung fibroblasts[3].

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

Calpeptin Related Antibodies

Cell Proliferation Assay[3]

Cell Line: WI38 VA13 and IMR90 cells
Concentration: 0-100 nM
Incubation Time: 24 hours
Result: Suppressed the proliferation in a dose-dependent manner.
In Vivo

Calpeptin with Bleo (0.04 mg/mouse, i.p., 3 times weekly, 28 days) administration significantly inhibits the collagen deposition and increases of calpain activity in the NSC-125066 treated mouse lung tissues[3].

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

Animal Model: C57BL/6 female mice (Eight-week-old)[3].
Dosage: 0.04 mg/mouse.
Administration: Intraperitoneally three times weekly for 28 days (together with Bleo).
Result: Inhibited the collagen deposition and increase of calpain activity in the NSC-125066 treated mouse lung tissues.
Masse moléculaire

362.46

Formule

C20H30N2O4
CAS No.

117591-20-5
Appearance

Solid

Color

White to off-white

SMILES

O=C(OCC1=CC=CC=C1)N[C@H](C(N[C@H](C=O)CCCC)=O)CC(C)C
Livraison

Room temperature in continental US; may vary elsewhere.
Stockage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvant et solubilité
In Vitro: 

DMSO : 100 mg/mL (275.89 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 2.7589 mL 13.7946 mL 27.5893 mL
5 mM 0.5518 mL 2.7589 mL 5.5179 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, 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.

  • Calculateur de molarité

  • Calculateur de dilution

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 (6.90 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% Corn Oil

    Solubility: ≥ 2.5 mg/mL (6.90 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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.
Pureté et documentation

Purity: ≥98.0%

SDS (393 KB)

COA (245 KB) HNMR (137 KB)

Instruction de manipulation (2659 KB)
Références

  • [1]. Tsujinaka T, et al. Synthesis of a new cell penetrating calpain inhibitor (calpeptin). Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8.  [Content Brief]

    [2]. Catalano JG, et al. Design of small molecule ketoamide-based inhibitors of cathepsin K. Bioorg Med Chem Lett. 2004 Feb 9;14(3):719-22.  [Content Brief]

    [3]. Tabata C, et al. The calpain inhibitor calpeptin prevents pulmonary fibrosis in mice. Clin Exp Immunol. 2010 Dec;162(3):560-7.  [Content Brief]

  • [1]. Tsujinaka T, et al. Synthesis of a new cell penetrating calpain inhibitor (calpeptin). Biochem Biophys Res Commun. 1988 Jun 30;153(3):1201-8.

    [2]. Catalano JG, et al. Design of small molecule ketoamide-based inhibitors of cathepsin K. Bioorg Med Chem Lett. 2004 Feb 9;14(3):719-22.

    [3]. Tabata C, et al. The calpain inhibitor calpeptin prevents pulmonary fibrosis in mice. Clin Exp Immunol. 2010 Dec;162(3):560-7.

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 2.7589 mL 13.7946 mL 27.5893 mL 68.9731 mL
5 mM 0.5518 mL 2.7589 mL 5.5179 mL 13.7946 mL
10 mM 0.2759 mL 1.3795 mL 2.7589 mL 6.8973 mL
15 mM 0.1839 mL 0.9196 mL 1.8393 mL 4.5982 mL
20 mM 0.1379 mL 0.6897 mL 1.3795 mL 3.4487 mL
25 mM 0.1104 mL 0.5518 mL 1.1036 mL 2.7589 mL
30 mM 0.0920 mL 0.4598 mL 0.9196 mL 2.2991 mL
40 mM 0.0690 mL 0.3449 mL 0.6897 mL 1.7243 mL
50 mM 0.0552 mL 0.2759 mL 0.5518 mL 1.3795 mL
60 mM 0.0460 mL 0.2299 mL 0.4598 mL 1.1496 mL
80 mM 0.0345 mL 0.1724 mL 0.3449 mL 0.8622 mL
100 mM 0.0276 mL 0.1379 mL 0.2759 mL 0.6897 mL
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Calpeptin Related Classifications

  • Metabolic Enzyme/Protease Apoptosis
  • Cathepsin Proteasome Apoptosis
Help & FAQs

Keywords:

Calpeptin117591-20-5CathepsinProteasomeApoptosisInhibitorinhibitorinhibit

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