| Identification | Back Directory | [Name]
RUBOXISTAURIN MESYLATE | [CAS]
169939-94-0 | [Synonyms]
CS-1578
LY 333531
Ruboxistaurin
Unii-721809wqcp
LY 333531; LY 333531
RUBOXISTAURIN MESYLATE
Ruboxistaurin (LY333531)
Ruboxistaurin (LY333531) (HCl salt)
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
(S)-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
9H,18H-5,21:12,17-Dimethenodibenzo(E,K)pyrrolo(3,4-H)(1,4,13)oxadiazacyclohexadecine-18,20(19H)-dione, 9-((dimethylamino)methyl)-6,7,10,11-tetrahydro-, (9S)- | [Molecular Formula]
C28H28N4O3 | [MOL File]
169939-94-0.mol | [Molecular Weight]
468.55 |
| Chemical Properties | Back Directory | [Boiling point ]
744.4±60.0 °C(Predicted) | [density ]
1.34 | [storage temp. ]
Store at -20°C | [solubility ]
DMSO : 50 mg/mL (106.71 mM; ultrasonic and warming and heat to 60°C) | [form ]
Solid | [pka]
8.26±0.40(Predicted) | [color ]
Brown to reddish brown |
| Hazard Information | Back Directory | [Uses]
Ruboxistaurin is a protein kinase C (PKC) β inhibitor, exhibits significant anti-angiogenic activity that reduces the response of vascular endothelial cells to stimulation by vascular endothelial growth factor (VEGF). Ruboxistaurin is used in treatment of diabetic microvascular complications. | [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. |
| [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) | [storage]
Store at -20°C |
|
| Company Name: |
LGM Pharma
|
| Tel: |
1-(800)-881-8210 |
| Website: |
www.lgmpharma.com |
|