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CAS No.: 169939-93-9

Ruboxistaurin HCl Catalog No. CSN12991

Synonyms: LY333531 hydrochloride;Ruboxistaurin;Ruboxistaurin HCl

LY333531 is a β-specific protein kinase C inhibitor. It competitively and reversibly inhibits PKCβ1 and PKCβ2 with IC50 values of 4.7 and 5.9 nM respectively.

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述LY333531 is a selective PKCβinhibitor with IC50 values of 4.7nM and 5.9nM for PKCβI and PKCβII isozyme, respectively, 76- and 61-fold selective for inhibition of PKCβI and PKCβII in comparison to PKCα(IC50=360nM). Oral administration of 1mg/kg LY333531 for a duration of 4 weeks prevented excessive PKCβ2 activation induced by hyperglycemia and attenuated cardiac diastolic dysfunction in rats with streptozotocin-induced diabetes. Also it suppressed the decreased expression of myocardial NO, Cav-3, phosphorylated p-Akt, and p-eNOS and also mitigated the augmentation of O₂^-, nitrotyrosine, Cav-1, and iNOS expression).
作用机制LY333531 is an ATP-competitive inhibitor.^[1]
动物研究
剂量
Pig: 0.5 mg/kg^[4] (p.o., twice daily) Rat: 1 mg/kg^[1] (p.o.); 0.1 mg/kg - 10 mg/kg^[5] (i.p.)

给药途径
p.o., i.p.
参考文献

动物研究
剂量	Pig: 0.5 mg/kg^[4] (p.o., twice daily) Rat: 1 mg/kg^[1] (p.o.); 0.1 mg/kg - 10 mg/kg^[5] (i.p.)
给药途径	p.o., i.p.

[1] Jirousek MR, Gillig JR, et al. (S)-13-[(dimethylamino)methyl]-10,11,14,15-tetrahydro-4,9:16, 21-dimetheno-1H, 13H-dibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecene-1,3(2H)-d ione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. J Med Chem. 1996 Jul 5;39(14):2664-71.
[2] Faul MM, Gillig JR, et al. Acyclic N-(azacycloalkyl)bisindolylmaleimides: isozyme selective inhibitors of PKCbeta. Bioorg Med Chem Lett. 2003 Jun 2;13(11):1857-9.
[3] Lei S, Li H, et al. Hyperglycemia-induced protein kinase C β2 activation induces diastolic cardiac dysfunction in diabetic rats by impairing caveolin-3 expression and Akt/eNOS signaling. Diabetes. 2013 Jul;62(7):2318-28.

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
- 1.9802 mL
- 9.9008 mL
- 19.8017 mL
- 5 mM
- 0.3960 mL
- 1.9802 mL
- 3.9603 mL
- 10 mM
- 0.1980 mL
- 0.9901 mL
- 1.9802 mL

技术信息

CAS号

169939-93-9

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C28H29ClN4O3

运输

蓝冰

分子量

505.01

别名

LY333531 hydrochloride;Ruboxistaurin;Ruboxistaurin HCl;LY333531 (hydrochloride);LY-333531

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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