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VTX-27

Cat. No. M9547
VTX-27 Structure
Synonym:

VTX27

Size Price Availability Quantity
5mg USD 459  USD510 In stock
10mg USD 747  USD830 In stock
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Quality Control
  • Current batch:
  • Purity >98.5%
  • COA
  • MSDS
Biological Activity

VTX-27 is a novel potent and selective PKCθ inhibitor, with Kis of 0.08 nM and 16 nM for PKC θ and PKC δ. In vivo, VTX-27 shows the best PK profile with a low clearance (7 mL/min/kg), long half-life (4.7 h), and good oral bioavailability (65%).

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 418.90
Formula C20H24ClFN6O
CAS Number 1321924-70-2
Purity >98.5%
Solubility DMSO ≥ 60 mg/mL
Storage at -20°C
References

Design and Optimization of Selective Protein Kinase C θ (PKCθ) Inhibitors for the Treatment of Autoimmune Diseases
Juan-Miguel Jimenez, et al. J Med Chem. 2013 Mar 14;56(5):1799-810. PMID: 23398373.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: VTX-27, VTX27 supplier, PKC, inhibitors

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