VTX-27

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

VTX-27 是蛋白激酶 C θ (PKC θ) 的选择性抑制剂（Kis：PKC θ 和 PKC δ 的 Kis：0.08 nM 和 16 nM）。

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).(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 shows the best PK profile with low clearance (7 mL/min/kg), good oral bioavailability (65%), and long half-life (4.7 h). A single dose of VTX-27 is administered orally at 6.25, 12.5, 25, and 50 mg/kg (e.g., at 25 mg/kg Cmax concentration 700 ng/mL) and demonstrates potent dose-dependent inhibition of IL-2 production.

VTX-27 (Compound 27) possesses excellent overall characteristics. Good selectivity of VTX-27 is also seen against other PKC family members, particularly classical isoforms (>1000-fold except PKCβ I, 200-fold) and atypical isoforms (>10000-fold). As anticipated, attaining selectivity over the more closely related novel PKC family members is more challenging, with a good 200-fold being achieved over PKC δ.

VTX-27 shows the best PK profile with a low clearance (7 mL min-1 kg-1), long half-life (4.7 h), and good oral bioavailability (65%). A single dose of VTX-27 is administered orally at 6.25, 12.5, 25, and 50 mg/kg (e.g., at 25 mg/kg Cmax concentration 700 ng/mL) and demonstrates potent dose dependent inhibition of IL-2 production.

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Angiogenesis

PKC

D2

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1321924-70-2

418.9

C20H24ClFN6O

>98% (HPLC)

In Vitro:?DMSO : 125 mg/mL (298.40 mM)

[H][C@]1(CN(CCN1)c1nc(-c2n[nH]c3ncccc23)c(F)cc1Cl)[C@](C)(O)C(C)C

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(-20℃)

With Ice Pack

≥ 2 years