Size | Price | Stock | Qty |
---|---|---|---|
5mg |
|
||
10mg |
|
||
50mg |
|
||
100mg |
|
||
Other Sizes |
|
Targets |
cathepsin L
|
---|---|
ln Vitro |
Pretreatment with Z-FY-CHO (10 μM) for one hour reduced the amount of cell death caused by 6-OHDA. Z-FY-CHO prevents 6-OHDA-treated SH-SY5Y cells from expressing more CTSL protein. In SH-SY5Y cells treated with 6-OHDA, Z-FY-CHO treatment increased LC3-II and decreased P62 expression, suggesting increased autophagy activity. Z-FY-CHO also inhibits the activation of caspase-3 and PARP[1]. ?U251 cells' radiosensitivity was greatly enhanced by transfection with cathepsin L shRNA or treatment with the particular cathepsin L inhibitor Z-FY-CHO (10 μM). In U251 cells, cathepsin L knockdown and suppression both exacerbated irradiation-induced DNA damage and G2/M phase cell cycle arrest. Increased levels of Bax and decreased levels of Bcl-2 demonstrate that irradiation-induced apoptosis was enhanced in U251 cells by both cathepsin L suppression and knockdown[2].
|
ln Vivo |
In an experimental model of osteoporosis involving ovariectomized mice, intraperitoneal injection of Z-FY-CHO (2.5-10 mg/kg) for 4 weeks inhibits bone weight loss in a dose-dependent manner. Z-FY-CHO suppresses bone resorption by preventing the breakdown of collagen[3].
|
References |
[1]. Lingyun Li, et al. Activated cathepsin L is associated with the switch from autophagy to apoptotic death of SH-SY5Y cells exposed to 6-hydroxydopamine. Biochem Biophys Res Commun. 2016 Feb 12;470(3):579-585.
[2]. Qing-qing Zhang, et al. Cathepsin L suppression increases the radiosensitivity of human glioma U251 cells via G2/M cell cycle arrest and DNA damage. Acta Pharmacol Sin. 2015 Sep;36(9):1113-25. [3]. J T Woo, et al. Suppressive effect of N-(benzyloxycarbonyl)-L-phenylalanyl-L-tyrosinal on bone resorption in vitro and in vivo. Eur J Pharmacol. 1996 Apr 4;300(1-2):131-5. |
Molecular Formula |
C26H26N2O5
|
---|---|
Molecular Weight |
446.50
|
CAS # |
167498-29-5
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
OC=1C=CC(=CC1)C[C@@H](C=O)NC([C@@H](NC(OCC2=CC=CC=C2)=O)CC3=CC=CC=C3)=O
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: 100 mg/mL (223.96 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.80 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 1.25 mg/mL (2.80 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (2.80 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.2396 mL | 11.1982 mL | 22.3964 mL | |
5 mM | 0.4479 mL | 2.2396 mL | 4.4793 mL | |
10 mM | 0.2240 mL | 1.1198 mL | 2.2396 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.