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VTX-27 is a selective inhibitor of protein kinase C θ (PKC θ) (Kis: 0.08 nM and 16 nM for PKC θ and PKC δ).
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $85 | In Stock | |
2 mg | $127 | In Stock | |
5 mg | $256 | In Stock | |
10 mg | $383 | In Stock | |
25 mg | $592 | In Stock | |
50 mg | $822 | In Stock | |
100 mg | $1,090 | In Stock | |
1 mL x 10 mM (in DMSO) | $237 | In Stock |
Description | VTX-27 is a selective inhibitor of protein kinase C θ (PKC θ) (Kis: 0.08 nM and 16 nM for PKC θ and PKC δ). |
Targets&IC50 | PKCθ:0.08 nM (ki), PKCδ:16 nM (ki), PKCα:356 nM (ki) |
In vitro | It has also been found that VTX-27 has good selectivity to other PKC family members, especially the classic isoforms (except for PKCβI, >1000 times, 200 times) and atypical isoforms (>10000 times). As expected, it is more challenging to obtain selectivity for more closely related novel PKC family members, which is 200 times more selective than PKCδ. |
In vivo | VTX-27 demonstrates a superior PK profile characterized by low clearance (7 mL/min/kg), high oral bioavailability (65%), and a prolonged half-life (4.7 h). Following a single oral administration at doses of 6.25, 12.5, 25, and 50 mg/kg (e.g., at 25 mg/kg Cmax concentration 700 ng/mL), it effectively inhibits IL-2 production in a potent dose-dependent manner. |
Molecular Weight | 418.9 |
Formula | C20H24ClFN6O |
Cas No. | 1321924-70-2 |
Smiles | FC1=C(C=2C=3C(NN2)=NC=CC3)N=C(C(Cl)=C1)N4C[C@@]([C@](C(C)C)(C)O)(NCC4)[H] |
Relative Density. | 1.342 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 125 mg/mL (298.40 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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