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Sotrastaurin

Cat. No. M3803
Sotrastaurin Structure
Synonym:

AEB071

Size Price Availability Quantity
2mg USD 76.5  USD85 In stock
5mg USD 108  USD120 In stock
10mg USD 180  USD200 In stock
50mg USD 684  USD760 In stock
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

Sotrastaurin is a potent and specific inhibitor of protein kinase C (PKC) with Ki at subnanomolar to low nanomolar range for a variety of PKC isotypes while selective for >200 other kinases. Sotrastaurin is an immunosuppressant that blocks early T-lymphocyte (T-cell) activation via protein kinase C inhibition. Sotrastaurin combined with EVR showed higher efficacy failure rates and some improvement in renal allograft function compared to a CsA-based therapy. Sotrastaurin inhibits nuclear factor (NF)-κB, which directly promotes the transcription of forkhead box protein 3 (FoxP3), the key regulator for the development and function of regulatory T cells (Tregs). Sotrastaurin is a potent inhibitor of alloreactivity in vitro, while it did not affect Treg function in patients after kidney transplantation. Sotrastaurin prevented TCR/CD28-induced T-cell activation and pro-inflammatory cytokine production, but preserved a stable Treg phenotype as evidenced by maintenance of suppressive capacity, high Foxp3 and CD25 expression, and lack of IL-17A and IFNγ production.

Protocol
Cell Experiment
Cell lines
Preparation method
Concentrations
Incubation time
Animal Experiment
Animal models male Wistar/F rats
Formulation Saline
Dosages 10 mg/kg and 30 mg/kg
Administration Orally administrated
Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 438.48
Formula C25H22N6O2
CAS Number 425637-18-9
Purity >98%
Solubility DMSO 50 mg/mL
Storage at -20°C
References

Targeting PKC in human T cells using sotrastaurin (AEB071) preserves regulatory T cells and prevents IL-17 production.
He X, et al. J Invest Dermatol. 2014 Apr;134(4):975-83. PMID: 24192715.

The protein kinase C inhibitor sotrastaurin allows regulatory T cell function.
de Weerd A, et al. Clin Exp Immunol. 2014 Feb;175(2):296-304. PMID: 24131367.

Efficacy of sotrastaurin plus tacrolimus after de novo kidney transplantation: randomized, phase II trial results.
Russ GR, et al. Am J Transplant. 2013 Jul;13(7):1746-56. PMID: 23668931.

Sotrastaurin in calcineurin inhibitor-free regimen using everolimus in de novo kidney transplant recipients.
Tedesco-Silva H, et al. Am J Transplant. 2013 Jul;13(7):1757-68. PMID: 23659755.

Overview of sotrastaurin clinical pharmacokinetics.
Kovarik JM, et al. Ther Drug Monit. 2010 Oct;32(5):540-3. PMID: 20683390.

Sotrastaurin, a protein kinase C inhibitor for the prevention of transplant rejection and treatment of psoriasis.
Manicassamy S. Curr Opin Investig Drugs. 2009 Nov;10(11):1225-35. PMID: 19876790.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Sotrastaurin, AEB071 supplier, PKC, inhibitors

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