192050-59-2

192050-59-2 structure

Name: Ruboxistaurin mesylate
Chemical Name: Ruboxistaurin mesilate
CAS Number: 192050-59-2
Molecular Formula: C₂₉H₃₂N₄O₆S
Molecular Weight: 564.65300
Catalog: Signaling Pathways Epigenetics PKC
Create Date: 2016-02-12 06:03:13
Modify Date: 2024-01-01 18:35:10
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].

Name	Ruboxistaurin mesilate
Synonyms	9-((Dimethylamino)methyl)-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo(E,k)pyrrolo(3,4-h)(1,4,13)oxadiazacyclohexadecine-18,20(19H)-dione,methanesulfonate,(9S) 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)-DIONE METHANESULFONATE Ruboxistaurin mesylate (S)-9-((dimethylamino)methyl)-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo(e,k)pyrrolo(3,4h)(1,4,13)oxadiazacyclohexadecine-18,20(19H)-dione mesylate UNII-6V860VW8AO

Description	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].
Related Catalog	Signaling Pathways >> Epigenetics >> PKC Research Areas >> Cardiovascular Disease Research Areas >> Metabolic Disease Signaling Pathways >> TGF-beta/Smad >> PKC
Target	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)
In Vitro	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: Male long-evans rats with streptozotocin induced diabetes[4] Dosage: 0.1, 1.0 and 10.0 mg/kg Administration: Oral administration; 0.1, 1.0 and 10.0 mg/kg, once daily for 4 weeks Result: Significantly decreased the number of leukocytes in the retinal microcirculation of rats with streptozotocin induced diabetes.
References	[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.

Molecular Formula	C₂₉H₃₂N₄O₆S
Molecular Weight	564.65300
Exact Mass	564.20400
PSA	134.74000
LogP	4.37440

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