| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
SC 57461 targets leukotriene A4 (LTA4) hydrolase, a bifunctional zinc metalloenzyme that catalyzes the conversion of LTA4 to leukotriene B4 (LTB4), a potent pro-inflammatory lipid mediator involved in chemotaxis, leukocyte activation, and inflammatory responses. By inhibiting LTA4 hydrolase with low-nanomolar IC50 values (2.5-3 nM), SC 57461 blocks LTB4 production. This inhibition reduces inflammation by decreasing the recruitment and activation of neutrophils and other immune cells. The compound shows selectivity for LTA4 hydrolase over other enzymes.
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| ln Vitro |
In whole blood, SC-57461A suppresses the synthesis of LTB4 induced by ionophores with IC50 values of 49, 166, and 466 nM for human, mouse, and topovirus, respectively [1]. The LTA4 fine-tuned enzyme (IC50=2.5 nM) and entire cells (IC50=49 nM) are both effectively inhibited by SC-57461A [2].
In vitro, SC 57461 acts as a potent and selective inhibitor of LTA4 hydrolase with IC50 values of 2.5 nM, 3 nM, and 3 nM for recombinant human, mouse, and mouse LTA4 hydrolase, respectively. It inhibits calcium ionophore-induced LTB4 production in human whole blood with an IC50 of 49 nM. The compound's ability to inhibit LTA4 hydrolase and reduce LTB4 production has been demonstrated in enzymatic and cell-based assays. SC 57461 is a non-peptide inhibitor, making it suitable for oral administration. |
| ln Vivo |
SC-57461A also showed excellent effects in in vitro mouse experiments, inhibiting the production of LTB4 with ED50=0.2 mg/kg and ED90=1 mg/kg. SC-57461A also inhibits LTB4 production in the peritoneal model with ED50=1 mg/kg[2]. SC-57461A is a potent, selective, competitive inhibitor of the LTA4 disinfecting enzyme with excellent activity in whole animals. SC-57461A in mice and mice
In vivo, SC 57461 is an orally bioactive LTA4 hydrolase inhibitor. It has been used in research studies to investigate the role of LTB4 in inflammatory diseases. However, specific in vivo efficacy data in animal models are not extensively detailed in the available literature. The compound's potent inhibition of LTA4 hydrolase and reduction of LTB4 production suggest potential therapeutic applications in inflammatory diseases such as asthma, rheumatoid arthritis, and inflammatory bowel disease. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for SC 57461 are LTA4 hydrolase inhibition assays using purified recombinant human, mouse, or rat LTA4 hydrolase. The enzyme is incubated with LTA4 substrate and varying concentrations of SC 57461, and the production of LTB4 is measured by ELISA or HPLC. The IC50 for inhibition of LTA4 hydrolase activity is determined from dose-response curves. These assays confirm the compound's direct inhibition of LTA4 hydrolase.
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| Cell Assay |
In vitro cellular assays for SC 57461 are performed using human whole blood or isolated leukocytes. Cells are treated with SC 57461 and stimulated with calcium ionophore (e.g., A23187) to induce LTB4 production. LTB4 levels in the supernatant are measured by ELISA. The IC50 for inhibition of LTB4 production is determined from dose-response curves. Cell viability is evaluated using appropriate assays to ensure that the observed effects are not due to cytotoxicity. These assays confirm the compound's ability to inhibit LTB4 production in a cellular context.
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| Animal Protocol |
Animal/Disease Models: Fasted CD rat [3]
Doses: 0.01, 0.1, 1 and 10 mg/kg Route of Administration: Oral Experimental Results: ED50 value at 1.0 is 0.2 mg/kg . h and 0.8 mg/kg at 3.0 h. A single dose of 10 mg/kg prevented 79%, 67% and 44% of LTB4 production at 6 hrs (hrs (hours)), 18 hrs (hrs (hours)) and 24 hrs (hrs (hours)), respectively. In vivo animal experiments for SC 57461 are conducted in animal models of inflammatory diseases. Rats or mice are administered SC 57461 via oral administration, and inflammation is induced using appropriate stimuli (e.g., carrageenan-induced paw edema, zymosan-induced peritonitis). LTB4 levels in inflammatory exudates or tissues are measured by ELISA. Inflammatory parameters such as edema, leukocyte infiltration, and cytokine levels are assessed. These studies evaluate the compound's efficacy in reducing inflammation. |
| ADME/Pharmacokinetics |
SC 57461 has a molecular weight of 363.88 g/mol and a molecular formula of C20H26ClNO3. The compound is orally active and is supplied as a purified solid for laboratory studies. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability have not been extensively reported. As a non-peptide LTA4 hydrolase inhibitor, SC 57461 is expected to have favorable pharmacokinetic properties for oral administration.
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| Toxicity/Toxicokinetics |
SC 57461 has been evaluated in preclinical studies and has been reported to be well-tolerated at effective doses. No significant toxicity has been reported in the available literature. As a selective LTA4 hydrolase inhibitor, SC 57461 may have a favorable safety profile with reduced risk of off-target effects. However, comprehensive toxicology studies would be necessary to fully assess the compound's safety for clinical development.
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| References |
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| Additional Infomation |
SC 57461 is a potent, orally active, non-peptide, and selective inhibitor of leukotriene A4 (LTA4) hydrolase. It has IC50 values of 2.5 nM, 3 nM, and 3 nM for recombinant human, mouse, and mouse LTA4 hydrolase, respectively. SC 57461 inhibits calcium ionophore-induced LTB4 production in human whole blood with an IC50 of 49 nM. The compound is a research tool for studying the role of LTB4 in inflammatory diseases.
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| Molecular Formula |
C20H25NO3
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| Molecular Weight |
327.42
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| Exact Mass |
363.16
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| CAS # |
423169-68-0
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| PubChem CID |
9820433
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| Appearance |
White to off-white solid powder
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| Density |
1.115g/cm3
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| Boiling Point |
499.7ºC at 760 mmHg
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| Flash Point |
256.01ºC
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| Index of Refraction |
1.562
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| LogP |
4.254
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
25
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| Complexity |
347
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| Defined Atom Stereocenter Count |
0
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| Synonyms |
SC57461; SC-57461; SC 57461
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| HS Tariff Code |
2934.99.9001
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| 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)
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| Solubility (In Vitro) |
DMSO : ~250 mg/mL (~687.04 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.72 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 20.8 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: ≥ 2.08 mg/mL (5.72 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 20.8 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: ≥ 2.08 mg/mL (5.72 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 | 3.0542 mL | 15.2709 mL | 30.5418 mL | |
| 5 mM | 0.6108 mL | 3.0542 mL | 6.1084 mL | |
| 10 mM | 0.3054 mL | 1.5271 mL | 3.0542 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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