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VTX-27

Cat. No. M9547
VTX-27 Structure
Synonym:

VTX27

Size Price Availability Quantity
5mg USD 510  USD510 In stock
10mg USD 840  USD840 In stock
25mg USD 1700  USD1700 In stock
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Quality Control & Documentation
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%).

Chemical Information
Molecular Weight 418.90
Formula C20H24ClFN6O
CAS Number 1321924-70-2
Solubility (25°C) DMSO ≥ 60 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Juan-Miguel Jimenez, et al. J Med Chem. Design and Optimization of Selective Protein Kinase C θ (PKCθ) Inhibitors for the Treatment of Autoimmune Diseases

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


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