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VTX-27

VTX-27 是蛋白激酶 C θ (PKC θ) 的一种选择性抑制剂，对 PKC θ 和 PKC δ 的 Ki 值分别为 0.08 nM 和 16 nM。

CAS号

1321924-70-2

分子式

C20H24ClFN6O

主要靶点

PKC

仅限科研使用

Cat No : CM06025

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Synonyms

验证数据展示

  • CAS No.: 1321924-70-2

    VTX-27
    CAS#: 1321924-70-2

产品信息

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).

CAS号 1321924-70-2
分子式 C20H24ClFN6O
主要靶点 PKC
主要通路 表观遗传|细胞骨架
分子量 418.9
纯度 99.49%， 此纯度可做参考，具体纯度与批次有关系，可咨询客服
储存条件 Powder: -20°C for 3 years | In solvent: -80°C for 1 year
别名

靶点活性

PKCδ:16 nM (ki)|PKCθ:0.08 nM (ki)|PKCα:356 nM (ki)

体内活性

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.

体外活性

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.

溶解度

DMSO:125 mg/mL (298.40 mM),Sonification is recommended.

参考文献

1.Jimenez JM, et al. Design and optimization of selective protein kinase C θ (PKCθ) inhibitors for the treatment of autoimmune diseases. J Med Chem. 2013 Mar 14;56(5):1799-810.

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