SID 26681509 |
| Catalog No.GC10377 |
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 958772-66-2
Sample solution is provided at 25 µL, 10mM.
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IC50: 56 nM
SID 26681509 is a potent and reversible human cathepsin L inhibitor.
The cathepsins have been found to comprise a family of lysosomal protease enzymes whose primary functions, such as protein degradation, play a keyl role in normal cellular homeostasis. Overexpression of cathepsin L and/or abnormal activity has been implicated in a number of disease states.
In vitro: SID 26681509 was found to inhibit human cathepsin L with an IC50 of 56 nM. After preincubation with enzyme for 1, 2, and 4 h before substrate addition, SID 26681509 showed increasing potency, with IC50 values falling to 7.5, 4.2, and 1.0 nM, respectively, indicating a slow onset of inhibition. SID 26681509 was also observed to be nontoxic to human aortic endothelial cells up to 100 μM. SID 26681509 was active in an in vitro propagation assay against P. falciparum with an IC50 of 15.4 μM. Additionally, the thiocarbazate inhibitor was toxic toward L. major promastigotes with an IC50 of 12.5 μM [1].
In vivo: SID 26681509 showed a lack of toxicity to zebrafish in a live organism assay at 100 μM [1].
Clinical trial: N/A
Reference:
[1] Shah PP,Myers MC,Beavers MP,Purvis JE,Jing H,Grieser HJ,Sharlow ER,Napper AD,Huryn DM,Cooperman BS,Smith AB 3rd,Diamond SL. Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L. Mol Pharmacol.2008 Jul;74(1):34-41.
| Cell experiment [1]: | |
|
Cell lines |
human aortic endothelial cells |
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Preparation method |
The solubility of this compound in DMSO is > 10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
|
Reacting condition |
100 μM, 37°C for 24 h |
|
Applications |
SID 26681509 (100 μM) was non-toxic to human aortic endothelial cells. SID 26681509 was active in an in vitro propagation assay against P. falciparum with an IC50 of 15.4 ± 0.6 μM. SID 26681509 was toxic toward L. major promastigotes with an IC50 of 12.5 ± 0.6 μM. |
| Animal experiment [1]: | |
|
Animal models |
zebrafish |
|
Dosage form |
100 μM |
|
Application |
SID 26681509 (100 μM) demonstrated a lack of toxicity to zebrafish in a live organism assay. |
|
Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
|
References: [1]. Shah P P, Myers M C, Beavers M P, et al. Kinetic characterization and molecular docking of a novel, potent, and selective slow-binding inhibitor of human cathepsin L[J]. Molecular pharmacology, 2008, 74(1): 34-41. | |
| Cas No. | 958772-66-2 | SDF | |
| Chemical Name | (S)-S-(2-((2-ethylphenyl)amino)-2-oxoethyl) 2-(2-((tert-butoxycarbonyl)amino)-3-(1H-indol-3-yl)propanoyl)hydrazinecarbothioate | ||
| Canonical SMILES | O=C(NNC(SCC(NC1=CC=CC=C1CC)=O)=O)[C@H](CC2=CNC3=CC=CC=C23)NC(OC(C)(C)C)=O | ||
| Formula | C27H33N5O5S | M.Wt | 539.65 |
| Solubility | <26.98mg/ml in DMSO; <5.4mg/ml in ethanol | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8531 mL | 9.2653 mL | 18.5305 mL |
| 5 mM | 0.3706 mL | 1.8531 mL | 3.7061 mL |
| 10 mM | 0.1853 mL | 0.9265 mL | 1.8531 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 30 reference(s) in Google Scholar.)
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