MDL 101146
MDL 101146 is an orally active neutrophil elastase inhibitor. MDL 101146 inhibits neutrophil elastase for human with a Ki value of 25 nM. MDL 101146 can be used for the research of arthritis.
For research use only. We do not sell to patients.
- CAS No.: 149859-17-6
- Formula: C29H37F5N4O6
- Molecular Weight:632.62
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
Ki for neutrophil elastase: 25 nM (human); 18 nM (rat)[1][2]
In Vitro
MDL 101,146 inhibits human neutrophil elastase with a Ki value of 25 nM[1].
MDL 101,146 inhibits rat neutrophil elastase activity in a dose-related manner with a Ki value of 18 nM[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Rats[2]
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Dosage:200 mg/kg
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Administration:Oral, 200 mg/kg/day
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Result:Inhibited the severity of collagen-induced arthritis.
Had a bone and cartilage sparing effect in the tibio-tarsal joint of animals with collagen-induced arthritis.
Chemical Information
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CAS No. 149859-17-6
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Molecular Weight 632.62
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Formula C29H37F5N4O6
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SMILES
O=C(N(CCC1)[C@@H]1C(NC(C(C)C)C(C(F)(F)C(F)(F)F)=O)=O)[C@H](C(C)C)NC(C(C=C2)=CC=C2C(N3CCOCC3)=O)=O
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Phagocytosis Functional Assay
A phagocytosis functional assay measures the ability of phagocytic cells, such as neutrophils, macrophages, monocytes, or microglia/macrophages, to bind and internalize particulate targets including bacteria, yeast particles, beads, or myelin particles. Fluorescent flow-cytometry assays detect target uptake as fluorescence associated with gated phagocytes, while pH-sensitive dyes such as pHrodo increase signal in acidic phagosomal compartments and therefore preferentially report internalized particles rather than particles remaining outside the cell. Microscopy or high-content imaging can be used to confirm intracellular localization and, in some protocols, to follow uptake kinetics.
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Collagen-Induced Arthritis
Collagen-induced arthritis (CIA) is an autoimmune murine model of rheumatoid arthritis in which immunization with type II collagen (CII) emulsified in an adjuvant induces a T cell- and autoantibody-driven inflammatory arthritis characterized by synovial hyperplasia, immune cell infiltration, and joint destruction. The model typically relies on genetically susceptible mouse strains (e. g. , DBA/1) and reproduces key features of human rheumatoid arthritis, including anti-collagen immune responses and progressive joint inflammation. Disease onset generally occurs within ~3-4 weeks after immunization, depending on antigen/adjuvant combinations and protocol variation. The immunopathology is driven by adaptive immune activation against CII, leading to systemic and local joint inflammation mediated by pro-inflammatory cytokines and effector immune cells, making CIA a standard preclinical platform for evaluating immunomodulatory and anti-arthritic interventions.
Purity & Documentation
References
[1]. Angelastro M, et al. Inhibition of human neutrophil elastase with peptidyl [Content Brief]
[2]. M J Janusz, et al. Inhibition of cartilage degradation in rat collagen-induced arthritis but not adjuvant arthritis by the neutrophil elastase inhibitor MDL 101,146. Inflamm Res. 1997 Dec;46(12):503-8. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)