PKC-IN-1

PKC-IN-1是一种有效的，ATP-竞争性的，可逆的PKC抑制剂，对人PKCβ和PKCα的Ki值分别为5.3和10.4nM，对人PKCα，PKCβI，PKCβII，PKCθ，PKCγ，PKCmu和PKCε的IC50值分别为2.3，8.1，7.6，25.6，57.5，314，808nM。

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库存: 现货

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数量
2mg

￥2512.00

2010.00

- +
5mg

￥3737.00

2990.00

- +
10mg

￥5350.00

4280.00

- +
50mg

￥15887.00

12710.00

- +
100mg

￥22250.00

17800.00

- +

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货号: ajce47664
CAS: 1046787-18-1
别名: [(2S,5R)-2,5-二甲基-4-[(四氢-2H-吡喃-4-基)甲基]-1-哌嗪基][3-[(5-氟-2-甲基-4-嘧啶基)氨基]-4,6-二氢-6,6-二甲基吡咯并[3,4-C]吡唑-5(1H)-基]甲酮
分子式: C25H37FN8O2
分子量: 500.61
纯度: ＞98%
溶解度: DMSO : ≥ 25 mg/mL (49.94 mM)
储存: Store at -20°C
库存: 现货

Background

PKC-IN-1 is a potent, ATP-competitive and reversible inhibitor of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively.

PKC-IN-1 (Compound A) is a potent, ATP-competitive and reversible of conventional PKC enzymes with Kis of 5.3 and 10.4 nM for human PKCβ and PKCα, and IC50s of 2.3, 8.1, 7.6, 25.6, 57.5, 314, 808 nM for PKCα, PKCβI, PKCβII, PKCθ, PKCγ, PKC mu and PKCε, respectively[1].

PKC-IN-1 (Compound A; 15 and 30 mg/kg, p.o., bid (twice a day)) dose-dependently and significantly reduces maximum EAE severity and end severity in autoimmune encephalitis (EAE) model in Lewis rats[1].

[1]. Michael Niesman, et al. Treatment of autoimmune disease. WO2015179847A1.

Protocol

Animal experiment:

Rats[1]PKC-IN-1 is tested in the experimental autoimmune encephalitis (EAE) model in Lewis rats. EAE is induced by MBP69-88/CFA immunization and pertussis toxin injection in Lewis rats. PKC-IN-1 is prepared as an oral suspension and dosed orally, twice per day (BID) at three doses, 7.5 and 15 and 30 mg/kg for total daily doses of 15, 30 and 60 mg/kg. The efficacy is compared to animals that receive the positive control FTY720 dosed once per day at a dose of 0.5 mg/kg. The treatment starts on Day 8, when 48% of the rats have signs of EAE[1].

参考文献:

[1]. Michael Niesman, et al. Treatment of autoimmune disease. WO2015179847A1.