Ruboxistaurin

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Ruboxistaurin

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

169939-94-0

LY333531

Ruboxistaurin (LY333531) 是一种具有口服活性，选择性PKC beta抑制剂(K_i=2 nM)，Ruboxistaurin 表现出 ATP 依赖的竞争性抑制 PKC beta I，其IC₅₀为4.7 nM。Ruboxistaurin 对 PKC beta II 的IC₅₀为 5.9 nM。

生物活性

Ruboxistaurin (LY333531) is an orally active, selectivePKCbetainhibitor (K_i=2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition ofPKCbeta I with anIC₅₀of 4.7 nM. Ruboxistaurin inhibitsPKCbeta II with anIC₅₀of 5.9 nM^[1]^[2].

IC₅₀& Target^[1]

PKC-βI

4.7 nM (IC₅₀)

PKC-βII

5.9 nM (IC₅₀)

PKCη

52 nM (IC₅₀)

PKCδ

250 nM (IC₅₀)

PKCγ

300 nM (IC₅₀)

PKCα

360 nM (IC₅₀)

PKCε

600 nM (IC₅₀)

体外研究
(In Vitro)

Ruboxistaurin is a selective and ATP-competitive PKCβ inhibitor, with IC₅₀s of 4.7 and 5.9 nM for PKCβI and PKCβII, shows less potent inhibition on PKCη (IC₅₀, 52 nM), PKCα (IC₅₀, 360 nM), PKCγ (IC₅₀, 300 nM), PKCδ (IC₅₀, 250 nM), and has no effect on PKCζ (IC₅₀, >100 μM)^[1]. Ruboxistaurin (10 and 400 nM) dramatically inhibits glucose-induced monocyte adherence to levels that are not different from baseline adherence of monocytes to endothelial cells under NG conditions. Ruboxistaurin (10 and 400 nM) dose not alter the endothelial expression of adhesion molecules or modify endothelial cell growth^[2]. Ruboxistaurin (LY333531; 10 nM) reduces high-glucose (HG)-induced human renal glomerular endothelial cells (HRGECs) viability, and inhibits the increases in swiprosin-1 in HRGECs incubated with HG^[3].

体内研究
(In Vivo)

Ruboxistaurin (1 mg/kg; 8 weeks) markedly reduces GEC apoptosis as well as swiprosin-1 upregulation, and ameliorates renal glomerular injury in the diabetic mice. Ruboxistaurin also potently attenuates the expression of PARP, cleaved-caspase9, cleaved-caspase3, and the Bax/Bcl-2 ratio, in diabetic mice^[3]. Ruboxistaurin (0.1, 1.0, or 10.0 mg/kg; p.o.) dramatically reduces the number of leukocytes trapped in the retinal microcirculation of diabetic rats^[4].

Animal Model:	Rats^[4]
Dosage:	0.1, 1.0, or 10.0 mg/kg
Administration:	P.o.
Result:	Dramatically reduced the number of leukocytes trapped in the retinal microcirculation of diabetic rats.

Clinical Trial

分子量

468.55

性状

Solid

Formula

C₂₈H₂₈N₄O₃

CAS 号

169939-94-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 25 mg/mL(53.36 mM;ultrasonic and warming and heat to 60℃)

配制储备液

浓度溶剂体积质量

1 mg

5 mg

10 mg

1 mM	2.1342 mL	10.6712 mL	21.3424 mL
5 mM	0.4268 mL	2.1342 mL	4.2685 mL
10 mM	0.2134 mL	1.0671 mL	2.1342 mL

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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.
请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline
Solubility: ≥ 1.67 mg/mL (3.56 mM); Suspended solution
此方案可获得 ≥ 1.67 mg/mL (3.56 mM，饱和度未知) 的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 16.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH2O 中，得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在本网站选购。