鲁伯斯塔盐酸盐 - CAS:169939-93-9 - CAS号查询_生物试剂_化学试剂_分析试剂

中文名称:	鲁伯斯塔盐酸盐
英文名称:	Ruboxistaurin hydrochloride
别名:	鲁伯斯塔盐酸盐;芦布妥林 LY333531 hydrochloride
CAS No:	169939-93-9	分子式:	C₂₈H₂₉ClN₄O₃	分子量:	505.01
CAS No:	169939-93-9
分子式:	C₂₈H₂₉ClN₄O₃
分子量:	505.01

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R10286 鲁伯斯塔盐酸盐 ≥98% (psaitong)

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包装规格：

2.5mg in glass bottle

溶解性：

溶于DMSO（6.67mg/mL 超声）

产品描述：

基本信息

产品编号：R10286
产品名称：Ruboxistaurin hydrochloride
CAS:	169939-93-9	储存条件	粉末	-20℃	四年

分子式：	C28H29ClN4O3		溶于液体	-80℃	六个月
分子量：	505.01			-20℃	一个月
化学名：
Solubility (25°C)	体外	DMSO	100mg/mL (198.01mM)
		Ethanol	Insoluble
		Water	Insoluble
	体内（现配现用）
＜1mg/ml表示微溶或不溶。
普西唐提供的所有化合物浓度为内部测试所得，实际溶液度可能与公布值有所偏差，属于正常的批间细微差异现象。
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。

制备储备液

浓度溶液体积质量	1mg	5mg	10mg
1mM	1.9802mL	9.9008mL	19.8016mL
5mM	0.3960mL	1.9802mL	3.9603mL
10mM	0.1980mL	0.9901mL	1.9802mL
50mM	0.0396mL	0.1980mL	0.3960mL

生物活性

产品描述	一种选择性的，ATP-竞争性的 PKCβ 抑制剂对 PKCβI 和 PKCβII 的 IC50 值分别为 4.7nM 和 5.9nM，对 PKCη (IC50，52nM)，PKCα (IC50，360nM)，PKCγ (IC50，300nM) 和 PKCδ (IC50，250nM) 的抑制作用相对较弱，而对 PKCζ (IC50，>100μM) 无作用。
靶点/IC50	PKCβ1 (Cell-free assay)	PKCβ2 (Cell-free assay)	PKCη (Cell-free assay)	PKCδ (Cell-free assay)	PKCγ (Cell-free assay)
靶点/IC50	4.7nM	5.9nM	0.052μM	0.25μM	0.3μM
体外研究	Ruboxistaurin hydrochloride is a selective and ATP-competitive PKCβ inhibitor, with IC50s of 4.7 and 5.9nM for PKCβI and PKCβII,shows less potent inhibition on PKCη (IC50, 52nM),PKCα(IC50,360nM),PKCγ (IC50, 300nM),PKCδ(IC50, 250nM),and has no effect on PKCζ(IC50,>100μM). Ruboxistaurin (10 and 400nM) 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 400nM) dose not alter the endothelial expression of adhesion molecules or modify endothelial cell growth. Ruboxistaurin (LY333531; 10nM) reduces high-glucose (HG)-induced human renal glomerular endothelial cells (HRGECs) viability, and inhibits the increases in swiprosin-1 in HRGECs incubated with HG.
体内研究	Ruboxistaurin (1mg/kg; 8weeks) 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,cleavedcaspase9,cleaved-caspase3,and the Bax/Bcl-2 ratio, in diabetic mice.Ruboxistaurin (0.1,1.0,or 10.0mg/kg;p.o.) dramatically reduces the number of leukocytes trapped in the retinal microcirculation of diabetic rats.

推荐实验方法(仅供参考)

细胞实验:

The second passages of human umbilical vein endothelial cells (HUVEC) are grown to confluence in microtiter plates coated with gelatin. The medium contains 5.5mM glucose. If endothelial cells are stimulated with 27.7mM glucose for 4 days, they are seeded in the well at a calibrated higher cell concentration in order to achieve comparable cell density at the day adhesion assays are performed. Therefore, cell density in the wells is tested thoroughly in control wells of each glucose concentration prior to monocyte adhesion assays. If Ruboxistaurin is used in this assay, it is added to the cultures for the whole period.

动物实验:

Rats

Leukocyte entrapment is evaluated only once after a 4-week diabetic period in both groups of rats with and without Ruboxistaurin treatment, using one eye (right eye) of each rat.Ruboxistaurin is administered orally at dosages of 0.1 (n=8),1.0 (n=16), and 10.0mg/kg/d (n=8) for 4weeks,from the time streptozotocin is injected in the rats.

保存条件：

-20℃

UN码：

HazardClass：

危害声明：

安全说明：

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