[CAS NO. 192050-59-2] Ruboxistaurin mesylate
PRODUCTS SPECIFICATIONS [192050-59-2]
DESCRIPTION [192050-59-2]
Overview
| MDL | MFCD09970504 |
|---|---|
| Molecular Weight | 564.65 |
| Molecular Formula | C29H32N4O6S |
| SMILES | O=C1NC(C(C2=CN(C3=CC=CC=C32)CCO[C@H](CN(C)C)CC4)=C1C5=CN4C6=CC=CC=C56)=O.CS(=O)(O)=O |
8 Publications Citing Use of MCE
- [1]Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.
- [2]Acta Pharm Sin B. 2022.
- [3]Cell Biosci. 2021 Feb 8;11(1):32.
- [4]Endocrinology. 2018 May 1;159(5):2253-2263.
- [5]Biosci Rep. 2018 Sep 7;38(5):BSR20171459.
- [6]ACS Omega. 2020 Oct 12;5(41):26551-26561.
- [7]Diabetes Metab Syndr Obes. 2019 Nov 4;12:2289-2302.
- [8]Trop J Pharm Res. 2022; 21(12): 2508.
Summary
IC50 & Target
|
PKC-βI 4.7 nM (IC 50 ) |
PKC-βII 5.9 nM (IC 50 ) |
PKCη 52 nM (IC 50 ) |
PKCδ 250 nM (IC 50 ) |
PKCγ 300 nM (IC 50 ) |
PKCα 360 nM (IC 50 ) |
PKCε 600 nM (IC 50 ) |
In Vitro
Ruboxistaurin mesylate inhibits PKC isozymes with IC
50
values of 0.36, 0.0047, 0.0059, 0.30, 0.25, 0.60 and 0.052 μM for PKCα, PKCβI, PKCβII, PKCγ, PKCδ, PKCε and PKCη, respectively
[1]
.
Ruboxistaurin mesylate inhibits Ca calmodulin and Rat Brain PKC with IC
50
values of 6.2 and 0.32 μM, respectively
[1]
.
Ruboxistaurin mesylate (10 and 400 nM; 4 days) significantly suppresses glucose-induced monocyte adherence under normoglycemic (NG) conditions
[3]
.
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| 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. |
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
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.
