| Identification | Back Directory | [Name]
(9S)-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 | [CAS]
192050-59-2 | [Synonyms]
Arxxant
LY 341684
LY-333531 (Mesylate)
Ruboxistaurin mesilate
DUHQBKLTAVUXFF-FERBBOLQSA-N
LY 333531 mesylate - Ruboxistaurin
(9S)-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 | [Molecular Formula]
C28H28N4O3.CH4O3S | [MDL Number]
MFCD09970504 | [MOL File]
192050-59-2.mol | [Molecular Weight]
564.653 |
| Hazard Information | Back Directory | [Uses]
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]. | [in vivo]
Ruboxistaurin mesylate (0.1, 1.0 and 10.0 mg/kg; oral administration, once daily for 4 weeks) decreases the increasing of leukocyte entrapment in the retinal microcirculation during the early diabetes period[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.
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| [IC 50]
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) | [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. DOI:10.1021/jm950588y
[2] Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-199. DOI:10.2165/00126839-200708030-00007
[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. DOI:10.1177/193229680700100620
[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. PMID:10937586 |
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| Company Name: |
SPIRO PHARMA
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| Telephone: |
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| Website: |
www.spiropharma.com.cn |
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