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SID 26681509 is a highly potent, reversible, competitive, and specific inhibitor of human cathepsin L with an IC50 of 56 nM. SID 26681509 inhibits in vitro propagation of malaria parasite Plasmodium falciparum and inhibits Leishmania major with IC50s of 15.4 μM and 12.5 μM, respectively. SID 26681509 shows no inhibitory activity against cathepsin G.
| ln Vitro |
After four hours of preincubation with cathepsin L, SID 26681509's IC50 of 1.0 nM increased in potency. It was discovered that SID 26681509 is a slowly reversible and slowly binding competitive inhibitor. The inhibitory rate constants, determined by single-step reversibility transient kinetic analysis, are kon = 24,000 M-1s-1 and koff = 2.2 × 10-5 s-1 (Ki = 0.89 nM). Using the papain/CLIK-148 experimentally obtained X-ray crystal structure, molecular docking investigations were carried out [1]. After an hour, SID 26681509 was shown to inhibit papain and cathepsins B, K, S, and V, with IC50 values ranging from 618 nM to 8.442 μM. The inhibitory action of SID 26681509 against the serine protease cathepsin G is nonexistent[1]. At 0.5 μM, SID 26681509 suppresses the activity of cathepsin V. Without affecting cell viability, SID 26681509 (1–30 μM) dose-dependently inhibits TNF-α production caused by high mobility group box 1 (HMGB1) [2].
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| ln Vivo |
SID 26681509 therapy significantly enhances the survival rate of sepsis animal models and lowers liver injury following warm hepatic ischemia/reperfusion (I/R) model [2].
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| References |
[1]. Shah PP, et al. 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.
[2]. Pribis JP, et al. The HIV Protease Inhibitor Saquinavir Inhibits HMGB1-Driven Inflammation by Targeting the Interaction of Cathepsin V with TLR4/MyD88. Mol Med. 2015 Dec;21(1):749-757. |
| Molecular Formula |
C₂₇H₃₃N₅O₅S
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|---|---|
| Molecular Weight |
539.646425008774
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| CAS # |
958772-66-2
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| Related CAS # |
SID 26681509 quarterhydrate
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| SMILES |
O=C(NNC(SCC(NC1=CC=CC=C1CC)=O)=O)[C@H](CC2=CNC3=CC=CC=C23)NC(OC(C)(C)C)=O
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| InChi Key |
OTIWAYTTYNFEKL-QFIPXVFZSA-N
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| InChi Code |
InChI=1S/C27H33N5O5S/c1-5-17-10-6-8-12-20(17)29-23(33)16-38-26(36)32-31-24(34)22(30-25(35)37-27(2,3)4)14-18-15-28-21-13-9-7-11-19(18)21/h6-13,15,22,28H,5,14,16H2,1-4H3,(H,29,33)(H,30,35)(H,31,34)(H,32,36)/t22-/m0/s1
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| Chemical Name |
S-(2-((2-ethylphenyl)amino)-2-oxoethyl) 2-((tert-butoxycarbonyl)-L-tryptophyl)hydrazine-1-carbothioate
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| Synonyms |
SID-26681509 SID26681509 SID 26681509
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~50 mg/mL (~92.65 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.32 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 (2.32 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 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 (2.32 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 | 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 |
*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.
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