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Ruboxistaurin-d6 (hydrochloride)

Ruboxistaurin-d6 (hydrochloride) is the deuterium labeled Ruboxistaurin hydrochloride. Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (Ki=2 nM) . Ruboxistaurin hydrochloride exhibits ATP dependent competitive inhibition of PKC beta I with an IC50 of 4.7 nM. Ruboxistaurin hydrochloride inhibits PKC beta II with an IC50 of 5.9 nM[1][2].

Product Specifications

CAS Number

1794767-04-6

UNSPSC

12352005

Target

Isotope-Labeled Compounds; PKC

Type

Isotope-Labeled Compounds

Related Pathways

Epigenetics; Others; TGF-beta/Smad

Applications

Metabolism-sugar/lipid metabolism

Field of Research

Metabolic Disease

Solubility

10 mM in DMSO

Smiles

O=C1C2=C(C=3C=4C(N(C3)CCO[C@H](CN(C([2H])([2H])[2H])C([2H])([2H])[2H])CCN5C=C2C=6C5=CC=CC6)=CC=CC4)C(=O)N1.Cl

Molecular Formula

C28H23D6ClN4O3

Molecular Weight

511.04

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216.|[2]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.|[3]Ruboxistaurin: LY 333531. Drugs R D. 2007;8 (3) :193-199.|[4]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.|[5]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.

Shipping Conditions

Room temperature

Scientific Category

Isotope-Labeled Compounds

Clinical Information

No Development Reported

Available Sizes

Frequently Asked Questions

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