Name: Sotrastaurin (AEB071)
Price: 284.00 USD

- Overview
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    Background
    
    AEB071 is an inhibitor of protein kinase C (PKC). The PKC inhibitor which can block the T-cell activation has the ability of immune suppression [1].
    The protein kinase C (PKC) isoforms is very important in cell signaling, proliferation, differentiation, migration, survival, and death. PKC family has many isoforms. Among the PKC isoforms, PKC isoforms have basal effect on the T cells’ activation and other immune cell functions [2,3].
    ABE071 is a potent inhibitor of novel and classical PKC isoforms. Through the inhibition of PKC, AEB071 can depress the activation and proliferation of T-cell and decrease the production of cytokine.ABE071 can also suppress the NK cell activity. Ex vivo stimulation of lymphocytes from subjects exposed to single doses of AEB071 resulted in a dose-dependent inhibition of both lymphocyte proliferation and IL2 mRNA expression
    AEB071 is an effective treatment strategy for the cure of autoimmune diseases. According to the Psoriasis Area Severity Index (PASI) score, after 2 weeks’ treatment with 300 mg bid AEB071, Clinical severity of psoriasis was reduced up to 69% compared with baseline[2,3].
    
    [1]. Weckbecker G1, Pally C, Beerli C, et al. Effects of the novel protein kinase C inhibitor AEB071 (Sotrastaurin) on rat cardiac allograft survival using single agent treatment or combination therapy with cyclosporine, everolimus or FTY720. Transpl Int. 2010 May 1;23(5):543-52
    [2]. Skvara H1, Dawid M, Kleyn E, Wolff B, et al. The PKC inhibitor AEB071 may be a therapeutic option for psoriasis. J Clin Invest. 2008 Sep;118(9):3151-9.
    [3]. Matz M1, Weber U, Mashreghi MF, et al. Effects of the new immunosuppressive agent AEB071 on human immune cells. Nephrol Dial Transplant. 2010 Jul;25(7):2159-67
- Properties
  - Alternative Name
    
    AEB 071;AEB-071; 3-(1H-indol-3-yl)-4-[2-(4-methylpiperazin-1-yl)quinazolin-4-yl]pyrrole-2,5-dione
    
    CAS Number
    
    425637-18-9
    
    Molecular Formula
    
    C25H22N6O2
    
    Molecular Weight
    
    438.48
    
    Appearance
    
    A solid
    
    Purity
    
    99.81%
    
    Solubility
    
    ≥21.9 mg/mL in DMSO; insoluble in H2O; ≥2.55 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only