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LY 333531 mesylate
- Ruboxistaurin- Parent CAS: 169939-94-0
- Soluble in DMSO
- MF: C28H28N4O3.CH4O3S
- MW: 564.65
Description
LY 333531 mesylate (Ruboxistaurin) is a selective, orally active protein kinase C beta (PKCβ) inhibitor that suppresses PKCβ-dependent vascular and inflammatory signaling.
Ruboxistaurin has been used to study hyperglycemia-driven PKC activation, endothelial dysfunction, vascular permeability and diabetic microvascular complications. Its pharmacology is particularly relevant to retinal, renal and neurovascular disease models. The mesylate salt form is five times more water-soluble than its hydrochloride salt, LY 333531 hydrochloride (Axon 2362).
Key Features
- Selective PKCβ inhibitor
- Orally active small-molecule kinase inhibitor
- Reduces hyperglycemia-associated vascular signaling
- Relevant to diabetic microvascular complications
Applications
- PKCβ kinase activity assays
- Diabetic retinopathy research
- Endothelial permeability and vascular dysfunction models
- Hyperglycemia-induced inflammatory signaling studies
More Information
| Parent CAS No. | 169939-94-0 |
|---|---|
| Chemical Name | 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 |
| MFCD | MFCD09970504 |
| Short Description | PKC-β inhibitor |
References
- Ruboxistaurin: LY 333531. Drug R. D. 2007, 8(3), 193-199.
- LY-333531 mesylate hydrate. Drugs Fut. 2000, 25(10), 1017.
- GL Engel et al. Salt form selection and characterization of LY333531 mesylate monohydrate. Int. J. Pharmaceutics 2000, 198(2), 239-247.
- MR Jirousek 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]oxadiazacy clohexadecene-1,3(2H)-dione (LY333531) and related analogues: isozyme selective inhibitors of protein kinase C beta. J. Med. Chem. 1996, 39, 2664.
- Y Wu et al. Protein kinase C beta inhibitor LY333531 attenuates intercellular adhesion molecule-1 and monocyte chemotactic protein-1 expression in the kidney in diabetic rats. J. Pharmacol. Sci. 2006, 101(4), 335-343.
- List of publications using LY 333531 (Axon 1401) purchased from Axon Medchem
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