1. Metabolic Enzyme/Protease
  2. Cathepsin
  3. VBY-825

VBY-825 is an orally available novel reversible cathepsin inhibitor that has high inhibitory potency against cathepsin B, L, S and V, and possesses anti-tumor, anti-inflammatory and analgesic effects.

For research use only. We do not sell to patients.

VBY-825 Chemical Structure

VBY-825 Chemical Structure

CAS No. : 1310340-58-9

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1 mg USD 340 In-stock
5 mg USD 850 In-stock
10 mg USD 1450 In-stock
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100 mg   Get quote  

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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of VBY-825:

Top Publications Citing Use of Products

1 Publications Citing Use of MCE VBY-825

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

VBY-825 is an orally available novel reversible cathepsin inhibitor that has high inhibitory potency against cathepsin B, L, S and V, and possesses anti-tumor, anti-inflammatory and analgesic effects[1][2][3].

IC50 & Target

cathepsin K

 

cathepsin S

 

Cellular Effect
Cell Line Type Value Description References
Vero C1008 EC50
0.3 μM
Compound: VBY-825
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
Determination of antiviral efficacy in high-content imaging assay in Vero E6 cells infected with SARS-CoV-2 (USA-WA1/2020 isolate) at MOI 0.75 after 24 hrs
[PMID: 32511357]
In Vitro

VBY-825 (0-300 nM) inhibits both heavy chain isoforms of cathepsin L and cathepsin B with IC50 values of 0.5, 3.3 and 4.3 nM in HUVEC cells[1].

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

In Vivo

VBY-825 (10 mg/kg, via gavage, once daily, 14 days) reduces pain behaviors in a mouse bone cancer model[2].
VBY-825 inhibits inflammation in mouse models of gout, peritonitis, and arthritis[3].

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

Animal Model: Mouse bone cancer model[2]
Dosage: 10 mg/kg; daily; 14 days
Administration: i.g.
Result: Reduced withdrawal and guarding of spontaneous bone cancer-induced pain.
Molecular Weight

535.55

Formula

C23H29F4N3O5S

CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CC[C@H](NC([C@@H](N[C@@H](C1=CC=C(F)C=C1)C(F)(F)F)CS(=O)(CC2CC2)=O)=O)C(C(NC3CC3)=O)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (233.40 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 1.8672 mL 9.3362 mL 18.6724 mL
5 mM 0.3734 mL 1.8672 mL 3.7345 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.

  • 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: ≥ 2.08 mg/mL (3.88 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 (3.88 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    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.
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: 99.81%

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, 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 1.8672 mL 9.3362 mL 18.6724 mL 46.6810 mL
5 mM 0.3734 mL 1.8672 mL 3.7345 mL 9.3362 mL
10 mM 0.1867 mL 0.9336 mL 1.8672 mL 4.6681 mL
15 mM 0.1245 mL 0.6224 mL 1.2448 mL 3.1121 mL
20 mM 0.0934 mL 0.4668 mL 0.9336 mL 2.3340 mL
25 mM 0.0747 mL 0.3734 mL 0.7469 mL 1.8672 mL
30 mM 0.0622 mL 0.3112 mL 0.6224 mL 1.5560 mL
40 mM 0.0467 mL 0.2334 mL 0.4668 mL 1.1670 mL
50 mM 0.0373 mL 0.1867 mL 0.3734 mL 0.9336 mL
60 mM 0.0311 mL 0.1556 mL 0.3112 mL 0.7780 mL
80 mM 0.0233 mL 0.1167 mL 0.2334 mL 0.5835 mL
100 mM 0.0187 mL 0.0934 mL 0.1867 mL 0.4668 mL
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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.

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Product Name:
VBY-825
Cat. No.:
HY-15958
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