|(R)-2-((S)-4-(3-氯-5-氟-6-(1H-吡唑并[3,4-b]吡啶-3-基)吡啶-2-基)哌嗪-2-基)-3-甲基丁-2-醇|CsnPharm

CAS No.: 1321924-70-2

VTX-27 Catalog No. CSN23775

Synonyms: Vtx-27

VTX-27 is an inhibitor of protein kinase C θ (PKC θ) and PKC δ with Kis of 0.08 nM and 16 nM, respectively.

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纯度 & 质量文件批次:

靶点选择性

生物活性

实验方案

技术信息

生物活性

描述PKCθ has a central role in T cell activation and survival. VTX-27 is a selective PKCθ inhibitor with Ki value of 0.08nM, but also inhibits PKC δ, ϵ and η less potently with IC50 values of 16, 1 and 3.5nM, respectively. VTX-27 exhibited impressive potency in PBMC T cell IL-2 assays with IC50 value of 11nM and IL-2 level in human whole blood with IC50 value of 70nM. A single oral dose of VTX-27 at doses of 12.5, 25 and 50mg/kg significantly (but not in a dose-dependent manner) reduced level of IL-2 release induced by staphylococcal enterotoxin B in a murine model.

动物研究

剂量

Mice: 6.25 mg/kg - 50 mg/kg^[1] (p.o.) Rat: 3 mg/kg^[1] (i.v.); 10 mg//kg^[1] (p.o.)

给药途径

p.o., i.v.

动物药代数据

Animal	Rats^[1]
Dose	3 mg/kg (i.v.) 10 mg/kg (p.o.)
Administration	i.v. p.o.
F	36% (p.o.)
T_1/2	4.7 h (p.o.)
CL	7 ml/min/kg (i.v.)

参考文献

[1] Jimenez JM, Boyall D, 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3872 mL
- 11.9361 mL
- 23.8723 mL
- 5 mM
- 0.4774 mL
- 2.3872 mL
- 4.7745 mL
- 10 mM
- 0.2387 mL
- 1.1936 mL
- 2.3872 mL

技术信息

CAS号

1321924-70-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H24ClFN6O

运输

蓝冰

分子量

418.90

别名

Vtx-27

溶解度

DMSO	84.0 mg/mL (200.5 mM)
Water	Insoluble
Ethanol	5.0 mg/mL (11.9 mM)

动物实验配方

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