RO5461111 (C007B-415529)

RO5461111 a highly specific and orally active antagonist of Cathepsin S with IC 50 s 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 nephritisIn VitroRO5461111 (16 h) 在 人 (RAJI) ¦Ë†€“©1„4 (A20) 细胞系中具有细胞活性,显著©TM¤1„2Ž¤o€ ¨"3„4¨"¦ '§a§Å ¶§»€ ¨Æ’ž§Å¡"活化以¥Å ©Å¡¥Å½ CD4 T 细胞和 CD4/CD8 ¥Å’© ̃ ́¦‚¬§ T 细胞的扩增和活化€‚ MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoRO5461111 (0.1-100 mg/kg; p.o.; single dose) suppresses T cell priming and antisheep IgG upon vaccination with sheep IgG in BALB/c mice . 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 . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Female MRL-Fas(lpr) mice (12-week-old; with proteinuria/serum creatinine levels up) Dosage: 262.5 mg/kg chow; or 5 mg/mouse with 1.31 mg/mouse Administration: Oral gavage; 8 weeks 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-±.Form:SolidIC50& Target:human Cathepsin S 0.4 nM (IC 50 ) murine Cathepsin S 0.5 nM (IC 50 ). Specification: 0.98 Molecular Formula: C27H24F6N4O4S Molecular Weight: 614.56

UPC:

41181918

Condition:

New

Weight:

1.06 Ounces

HazmatClass:

No

Quantity:

1

Unit of Measurement:

EA

WeightUOM:

LB

MPN:

R646264-10mg

CAS:

1252637-46-9

Product Size:

10mg