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

L-006235 (Synonyms: L-235)

Cat. No.: HY-103352 Purity: 98.03%
Handling Instructions

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.

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

L-006235 Chemical Structure

L-006235 Chemical Structure

CAS No. : 294623-49-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 123 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 200 In-stock
Estimated Time of Arrival: December 31
25 mg USD 400 In-stock
Estimated Time of Arrival: December 31
50 mg USD 680 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1150 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

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Based on 1 publication(s) in Google Scholar

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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

IC50: 5 nM (cathepsin K)[1]

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].

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

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].

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.

294623-49-7

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 : 83.33 mg/mL (178.59 mM; Need ultrasonic)

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
10 mM 0.2143 mL 1.0716 mL 2.1432 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 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

  • 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

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.46 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

L-006235L-235L006235L 006235L235L 235CathepsincathepsinKboneresorptioncollagendegradationlossInhibitorinhibitorinhibit

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Product Name:
L-006235
Cat. No.:
HY-103352
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