L-873724

Cat. No.: HY-50887 Purity: 98.93%: FAQs
Data Sheet SDS COA Handling Instructions

Molarity Calculator

L-873724 is a potent, orally bioavailable, selective and reversible non-basic cathepsin K inhibitor, with IC₅₀s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also exhibits an IC₅₀ of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption.

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

L-873724 Chemical Structure

CAS No. : 603139-12-4

Size	Price	Stock	Quantity
1 mg	USD 850	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 1650	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 2850	In-stock	Estimated Time of Arrival: December 31
50 mg		Get quote
100 mg		Get quote

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Cathepsin B Cathepsin C Cathepsin D Cathepsin E Cathepsin K Cathepsin L Cathepsin S

Biological Activity
Purity & Documentation
References
Customer Review

Description

L-873724 is a potent, orally bioavailable, selective and reversible^[2] non-basic cathepsin K inhibitor, with IC₅₀s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively^[1]. L-873724 also exhibits an IC₅₀ of 0.5 nM for rabbit cathepsin K. L-873724 inhibits bone resorption^[2].

IC₅₀ & Target

IC50: 0.2 nM (Cathepsin K), 178 nM (Cathepsin S), 264 nM (Cathepsin B), 5239 nM (Cathepsin B)^[1], 0.5 nM (Rabbit cathepsin K)^[2]

In Vitro

L-873724 (Compound 22) is a potent and selective non-basic cathepsin K inhibitor, with IC₅₀s of 0.2, 178, 264, and 5239 nM for cathepsin K, cathepsin S, cathepsin L, cathepsin B, respectively. L-873724 also shows IC₅₀s of 95, 1221 and 4807 nM for Ramos cathepsin S, Hep G2 cathepsin L, Hep G2 cathepsin B^[1]. L-873724 exhibits an IC₅₀ of 0.5 nM for rabbit cathepsin K^[2].

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

In Vivo

L-873724 is orally bioavailable, non-lysosomotropic, and efficacious in the rhesus monkey bone resorption model^[1].

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

Molecular Weight

481.53

Formula

C₂₃H₂₆F₃N₃O₃S

CAS No.

603139-12-4

Appearance

Solid

Color

White to off-white

SMILES

O=S(C1=CC=C(C2=CC=C([C@@H](C(F)(F)F)N[C@@H](CC(C)C)C(NCC#N)=O)C=C2)C=C1)(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

4°C, sealed storage, away from moisture and light

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (207.67 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	2.0767 mL	10.3836 mL	20.7671 mL
5 mM	0.4153 mL	2.0767 mL	4.1534 mL
10 mM	0.2077 mL	1.0384 mL	2.0767 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 (sealed storage, away from moisture and light). 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)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (5.19 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% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.19 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 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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.19 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)

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).

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

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: 98.93%

Select Batch:

Data Sheet (272 KB) SDS (252 KB)

COA (248 KB) HNMR (260 KB) CNMR (263 KB) RP-HPLC (253 KB) MS (73 KB)

Handling Instructions (2659 KB)

References

[1]. Li CS, et al. Identification of a potent and selective non-basic cathepsin K inhibitor. Bioorg Med Chem Lett. 2006 Apr 1;16(7):1985-9. [Content Brief]

[2]. Zhuo Y, et al. Inhibition of bone resorption by the cathepsin K inhibitor odanacatib is fully reversible. Bone. 2014 Oct;67:269-80. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.0767 mL	10.3836 mL	20.7671 mL	51.9178 mL
	5 mM	0.4153 mL	2.0767 mL	4.1534 mL	10.3836 mL
	10 mM	0.2077 mL	1.0384 mL	2.0767 mL	5.1918 mL
	15 mM	0.1384 mL	0.6922 mL	1.3845 mL	3.4612 mL
	20 mM	0.1038 mL	0.5192 mL	1.0384 mL	2.5959 mL
	25 mM	0.0831 mL	0.4153 mL	0.8307 mL	2.0767 mL
	30 mM	0.0692 mL	0.3461 mL	0.6922 mL	1.7306 mL
	40 mM	0.0519 mL	0.2596 mL	0.5192 mL	1.2979 mL
	50 mM	0.0415 mL	0.2077 mL	0.4153 mL	1.0384 mL
	60 mM	0.0346 mL	0.1731 mL	0.3461 mL	0.8653 mL
	80 mM	0.0260 mL	0.1298 mL	0.2596 mL	0.6490 mL
	100 mM	0.0208 mL	0.1038 mL	0.2077 mL	0.5192 mL

L-873724 Related Classifications

Metabolic Disease

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-873724603139-12-4L873724L 873724CathepsinInhibitorinhibitorinhibit

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