2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. Balicatib

Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis.

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

Balicatib Chemical Structure

Balicatib Chemical Structure

CAS No. : 354813-19-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 79 In-stock
Solution
10 mM * 1 mL in DMSO USD 79 In-stock
Solid
5 mg USD 72 In-stock
10 mg USD 132 In-stock
25 mg USD 277 In-stock
50 mg USD 470 In-stock
100 mg USD 750 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Balicatib Related Antibodies

Top Publications Citing Use of Products

View All Cathepsin Isoform Specific Products:

View All Isoforms
Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Balicatib (AAE581) is a potent, orally active and selective cathepsin K inhibitor with IC50 values of 22, 61, 48, 2900 nM for cathepsin K, cathepsin B, cathepsin L, cathepsin S, respectively. Balicatib inhibits bone turnover, decreases bone formation rates. Balicatib has the potential for the research of osteoporosis[1][2].

IC50 & Target[2]

cathepsin K

22 nM (IC50)

cathepsin L

48 nM (IC50)

Cathepsin B

61 nM (IC50)

cathepsin S

2900 nM (IC50)

In Vitro

Balicatib (0-10 µM) shows less than 1.5-fold accumulation of Type I collagen at concentrations up to 10 µM in human dermal fibroblasts[2].

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

Balicatib Related Antibodies
In Vivo

Balicatib (0, 3, 10, 50 mg/kg; Oral gavage; twice daily for 18 months) partially prevented ovariectomyinduced changes in bone mass, inhibited bone turnover at most sites, and had an stimulatory effect on periosteal bone formation in cynomolgus monkeys[1].

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

Animal Model: 11-13 years, female cynomolgus monkeys (Macaca fascicularis)[1]
Dosage: 0, 3, 10, 50 mg/kg
Administration: Oral gavage; twice daily for 18 months
Result: Completely prevented ovariectomy-induced increases in BFR/BS in cancellous bone of vertebra and femur and in osteonal and endocortical bone of vertebra, significantly decreased bone formation rates.
Clinical Trial
Molecular Weight

411.54

Formula

C23H33N5O2
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

CCCN1CCN(C2=CC=C(C(NC3(C(NCC#N)=O)CCCCC3)=O)C=C2)CC1
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 : 75 mg/mL (182.24 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 2.4299 mL 12.1495 mL 24.2990 mL
5 mM 0.4860 mL 2.4299 mL 4.8598 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: ≥ 3.75 mg/mL (9.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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: ≥ 3.75 mg/mL (9.11 mM); Clear solution

    This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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
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 2.4299 mL 12.1495 mL 24.2990 mL 60.7474 mL
5 mM 0.4860 mL 2.4299 mL 4.8598 mL 12.1495 mL
10 mM 0.2430 mL 1.2149 mL 2.4299 mL 6.0747 mL
15 mM 0.1620 mL 0.8100 mL 1.6199 mL 4.0498 mL
20 mM 0.1215 mL 0.6075 mL 1.2149 mL 3.0374 mL
25 mM 0.0972 mL 0.4860 mL 0.9720 mL 2.4299 mL
30 mM 0.0810 mL 0.4050 mL 0.8100 mL 2.0249 mL
40 mM 0.0607 mL 0.3037 mL 0.6075 mL 1.5187 mL
50 mM 0.0486 mL 0.2430 mL 0.4860 mL 1.2149 mL
60 mM 0.0405 mL 0.2025 mL 0.4050 mL 1.0125 mL
80 mM 0.0304 mL 0.1519 mL 0.3037 mL 0.7593 mL
100 mM 0.0243 mL 0.1215 mL 0.2430 mL 0.6075 mL
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Balicatib 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:

Balicatib354813-19-7AAE581AAE 581AAE-581Cathepsinbone turnoverbone formationosteoporosisdermal fibroblastsInhibitorinhibitorinhibit

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