RO5461111
Based on 1 Customer Validation
RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC50s of 0.4 nM (human Cathepsin S) and 0.5 nM (murine Cathepsin S), respectively. RO5461111 can effectively inhibit the activation of antigen-specific T cells and B cells. RO5461111 can improve pulmonary inflammation and lupus nephritis.
For research use only. We do not sell to patients.
- Purity: 98.01%
- CAS No.: 1252637-46-9
- Formula: C27H24F6N4O4S
- Molecular Weight:614.56
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Storage:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
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All Cathepsin Isoforms
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Biological Activity
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human Cathepsin S 0.4 nM (IC50) |
murine Cathepsin S 0.5 nM (IC50) |
RO5461111 (16 h) is cytoactive in cell lines of human (RAJI) or mouse (A20), and significantly reduces splenic dendritic cell activation and subsequent expansion and activation of CD4 T cells and CD4/CD8 double negative T cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
RO5461111 (1.31 mg/mouse or 30 mg/kg; p.o.; 8 weeks) disrupts germinal centres (as CXCL12) and reduces hypergammaglobulinemia and lupus autoantibody production F in MRL-Fas(lpr) mice. And RO5461111 reduces lung inflammation and improves lupus nephritis[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female MRL-Fas(lpr) mice (12-week-old; with proteinuria/serum creatinine levels up)[1]
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Dosage:262.5 mg/kg chow; or 5 mg/mouse with 1.31 mg/mouse
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Administration:Oral gavage; 8 weeks
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Result:Reduced the activation and expansion of spleen dendritic cells, CD4, double-negative T cells and plasma cells.
Reduced plasma levels of IL-10 and TNF-α.
Chemical Information
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CAS No. 1252637-46-9
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Appearance Solid
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Molecular Weight 614.56
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Formula C27H24F6N4O4S
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Color White to off-white
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SMILES
O=C([C@H]1N(C(C2(C(F)(F)F)CC2)=O)C[C@H](S(=O)(C3=CC=C(C4=CC(C)=NC=C4)C=C3C(F)(F)F)=O)C1)NC5(C#N)CC5
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Purity & Documentation
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Data Sheet (276 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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