2. Metabolic Enzyme/Protease
  3. Cathepsin
  4. L-006235

L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss.

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L-006235 Chemical Structure

L-006235 Chemical Structure

CAS No. : 294623-49-7

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 123 In-stock
Solution
10 mM * 1 mL in DMSO USD 123 In-stock
Solid
1 mg USD 40 In-stock
5 mg USD 120 In-stock
10 mg USD 200 In-stock
25 mg USD 400 In-stock
50 mg USD 680 In-stock
100 mg USD 1150 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

L-006235 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

L-006235 (L-235) is a potent, selective, reversible and orally active inhibitor of cathepsin K, with an IC50 of 5 nM in bone resorption assay. L-006235 shows selectivity for cathepsin K (Ki=0.2 nM) over cathepsin B, cathepsin L, and cathepsin S (Ki=1, 6, and 47 μM, respectively). L-006235 can reduce collagen degradation and prevent bone loss[1][2].

IC50 & Target

Cathepsin B

 

cathepsin K

 

In Vitro

L-006235 inhibits bone resorption in the rabbit bone resorption assay, with an IC50 of 5 nM[1].
L-006235 (10 μM; 1 h) show a punctate fluorescence throughout the cytoplasm in HepG2 cells[2].

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

L-006235 Related Antibodies
In Vivo

L-006235 (0.6-15 mg/kg; p.o. qd for 8-11 d) reduces N-telopeptides (NTx) and creatinine (Cre) by up to 76% dose-dependently in rhesus monkey[1].
L-006235 (20 mg/kg; p.o.) exhibits high oral bioavailability (68%), long terminal half-life (204 min) and Cmax (1.4 μM) in rats[1].

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

Animal Model: Rhesus monkey (15 years) receiving oophorectomy (OVX)[1]
Dosage: 0.6, 3, 15 mg/kg
Administration: P.o once daily for 8-11 days
Result: Decreased uNTx/Cre by an average of 76%, 68%, and 31% at the dose of 15, 3, and 0.6 mg/kg, respectively.
Molecular Weight

466.60

Formula

C24H30N6O2S
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(NC1(C(NCC#N)=O)CCCCC1)C2=CC=C(C3=CSC(N4CCN(C)CC4)=N3)C=C2
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 : 31.25 mg/mL (66.97 mM; ultrasonic and warming and heat to 60°C; 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 2.1432 mL 10.7158 mL 21.4316 mL
5 mM 0.4286 mL 2.1432 mL 4.2863 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 (4.46 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 (4.46 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.
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: 99.96%

COA (249 KB) HNMR (277 KB) LCMS (267 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, 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 2.1432 mL 10.7158 mL 21.4316 mL 53.5791 mL
5 mM 0.4286 mL 2.1432 mL 4.2863 mL 10.7158 mL
10 mM 0.2143 mL 1.0716 mL 2.1432 mL 5.3579 mL
15 mM 0.1429 mL 0.7144 mL 1.4288 mL 3.5719 mL
20 mM 0.1072 mL 0.5358 mL 1.0716 mL 2.6790 mL
25 mM 0.0857 mL 0.4286 mL 0.8573 mL 2.1432 mL
30 mM 0.0714 mL 0.3572 mL 0.7144 mL 1.7860 mL
40 mM 0.0536 mL 0.2679 mL 0.5358 mL 1.3395 mL
50 mM 0.0429 mL 0.2143 mL 0.4286 mL 1.0716 mL
60 mM 0.0357 mL 0.1786 mL 0.3572 mL 0.8930 mL
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L-006235 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:

L-006235294623-49-7L-235L006235L 006235L235L 235CathepsincathepsinKboneresorptioncollagendegradationlossInhibitorinhibitorinhibit

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