Ruboxistaurin mesylate_product_DataBase

Bioactivity	Ruboxistaurin (LY333531) mesylate is an orally active, selective and ATP competitive PKCβ inhibitor with IC50 values of 4.7 and 5.9 nM for PKCβI and PKCβII, respectively. Ruboxistaurin mesylate can be used for the research of eye disorders, heart failure and diabetes[1][2][3][4].
Invitro	Ruboxistaurin mesylate 对 PKCα，PKCβI，PKCβII，PKCγ，PKCδ，PKCε 和 PKCη 的 IC50 值分别为 0.36，0.0047，0.0059，0.30，0.25，0.60 和 0.052 μM[1]。Ruboxistaurin mesylate 抑制 Ca calmodulin 和大鼠脑 PKC 的 IC50 分别为 6.2 和 0.32 μM[1]。Ruboxistaurin mesylate (10 和 400 nM；4 天) 显著抑制正常血糖 (NG) 条件下葡萄糖诱导的单核细胞粘附[3]。
In Vivo	Ruboxistaurin mesylate (0.1, 1.0 和 10.0 mg/kg；口服，每日 1 次，共 3 周) 抑制糖尿病早期视网膜微循环中白细胞滞留的增加[4]。 Animal Model:
Name	Ruboxistaurin mesylate
CAS	192050-59-2
Formula	C29H32N4O6S
Molar Mass	564.65
Transport	Room temperature in continental US; may vary elsewhere.
Storage	Please store the product under the recommended conditions in the Certificate of Analysis.
Reference	[1]. Jirousek MR, 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;39(14):2664-2671. [2]. Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-199. [3]. Kunt T, et al. The beta-specific protein kinase C inhibitor ruboxistaurin (LY333531) suppresses glucose-induced adhesion of human monocytes to endothelial cells in vitro. J Diabetes Sci Technol. 2007 Nov;1(6):929-35. [4]. Nonaka A, et al. PKC-beta inhibitor (LY333531) attenuates leukocyte entrapment in retinal microcirculation of diabetic rats. Invest Ophthalmol Vis Sci. 2000 Aug;41(9):2702-6.

PeptideDB

Ruboxistaurin mesylate

CAS: 192050-59-2 F: C29H32N4O6S W: 564.65