GlpBio

PKC-IN-1

目录号: GC31711纯度: >98.50%同义词: [(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
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。
PKC-IN-1
Cas No.: 1046787-18-1
规格价格库存数量操作
2mg¥2,082.00现货
1
5mg¥3,124.00现货
1
10mg¥4,463.00现货
1
50mg¥13,388.00现货
1
100mg¥18,743.00现货
1
10mM (in 1mL DMSO)¥3,441.00现货
1
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文献被引

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    183(7):1867-1883 (2020)
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    33, 904–922 (2023)
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    31, 1291–1307 (2021)

产品描述 Description

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.

实验参考方法 Experimental Reference Method

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].

References:

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

产品文档 Product Documents

Purity:>98.50%

化学性质Chemical Properties

CAS 号
1046787-18-1
同义词
[(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
SMILES
O=C(N1[C@@H](C)CN(CC2CCOCC2)[C@H](C)C1)N(C3)C(C)(C)C4=C3C(NC5=NC(C)=NC=C5F)=NN4
分子式
C25H37FN8O2
分子量
500.61 g/mol
溶解性
DMSO : ≥ 25 mg/mL (49.94 mM)
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol