Ruboxistaurin mesylate | LY-333531 | CAS#192050-59-2 | PKC beta inhibitor

MedKoo Cat#: 526554 | Name: Ruboxistaurin mesylate

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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Ruboxistaurin, also known as LY-333531, is a PKC beta inhibitor potentially for the treatment of diabetic nephropathy and diabetic macular edema. Ruboxistaurin attenuates diabetic nephropathy via modulation of TGF-β1/Smad and GRAP pathways. Ruboxistaurin reduces oxidative stress and attenuates left ventricular hypertrophy and dysfunction in rats with streptozotocin-induced diabetes. Ruboxistaurin inhibits retinal neovascularization via suppression of phosphorylation of ERK1/2 and Akt.

Chemical Structure

Ruboxistaurin mesylate

CAS#192050-59-2 (mesylate)

Theoretical Analysis

MedKoo Cat#: 526554

Name: Ruboxistaurin mesylate

CAS#: 192050-59-2 (mesylate)

Chemical Formula: C29H32N4O6S

Exact Mass: 0.0000

Molecular Weight: 564.66

Elemental Analysis: C, 61.69; H, 5.71; N, 9.92; O, 17.00; S, 5.68

Price and Availability

Size	Price	Availability	Quantity
5mg	USD 450.00	2 Weeks

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Related CAS #

169939-94-0 (free base) 202260-21-7 (mesylate hydrate) 169939-93-9 (HCl) 192050-59-2 (mesylate)

Synonym

LY-333531; LY333531; LY 333531; LY-333531 Mesylate; Ruboxistaurin mesylate

IUPAC/Chemical 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 mesylate

InChi Key

DUHQBKLTAVUXFF-FERBBOLQSA-N

InChi Code

InChI=1S/C28H28N4O3.CH4O3S/c1-30(2)15-18-11-12-31-16-21(19-7-3-5-9-23(19)31)25-26(28(34)29-27(25)33)22-17-32(13-14-35-18)24-10-6-4-8-20(22)24;1-5(2,3)4/h3-10,16-18H,11-15H2,1-2H3,(H,29,33,34);1H3,(H,2,3,4)/t18-;/m0./s1

SMILES Code

O=C1NC(C(C2=CN(C3=CC=CC=C32)CCO[C@H](CN(C)C)CC4)=C1C5=CN4C6=CC=CC=C56)=O.OS(=O)(C)=O

Appearance

Solid powder

Purity

>98% (or refer to the Certificate of Analysis)

Shipping Condition

Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition

Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility

Soluble in DMSO

Shelf Life

>2 years if stored properly

Drug Formulation

This drug may be formulated in DMSO

Stock Solution Storage

0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code

2934.99.9001

More Info

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 564.66 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

1: Joy SV, Scates AC, Bearelly S, Dar M, Taulien CA, Goebel JA, Cooney MJ. Ruboxistaurin, a protein kinase C beta inhibitor, as an emerging treatment for diabetes microvascular complications. Ann Pharmacother. 2005 Oct;39(10):1693-9. doi: 10.1345/aph.1E572. Epub 2005 Sep 13. PMID: 16160002. 2: Vinik AI, Bril V, Kempler P, Litchy WJ, Tesfaye S, Price KL, Bastyr EJ 3rd; MBBQ Study Group. Treatment of symptomatic diabetic peripheral neuropathy with the protein kinase C beta-inhibitor ruboxistaurin mesylate during a 1-year, randomized, placebo-controlled, double-blind clinical trial. Clin Ther. 2005 Aug;27(8):1164-80. doi: 10.1016/j.clinthera.2005.08.001. PMID: 16199243. 3: Avignon A, Sultan A. PKC-B inhibition: a new therapeutic approach for diabetic complications? Diabetes Metab. 2006 Jun;32(3):205-13. doi: 10.1016/s1262-3636(07)70270-7. PMID: 16799396. 4: McGill JB, King GL, Berg PH, Price KL, Kles KA, Bastyr EJ, Hyslop DL. Clinical safety of the selective PKC-beta inhibitor, ruboxistaurin. Expert Opin Drug Saf. 2006 Nov;5(6):835-45. doi: 10.1517/14740338.5.6.835. PMID: 17044810. 5: Lang GE. Treatment of diabetic retinopathy with protein kinase C subtype Beta inhibitor. Dev Ophthalmol. 2007;39:157-165. doi: 10.1159/000098506. PMID: 17245085. 6: Lang GE. Pharmacological treatment of diabetic retinopathy. Ophthalmologica. 2007;221(2):112-7. doi: 10.1159/000098256. PMID: 17380065. 7: Casellini CM, Barlow PM, Rice AL, Casey M, Simmons K, Pittenger G, Bastyr EJ 3rd, Wolka AM, Vinik AI. A 6-month, randomized, double-masked, placebo- controlled study evaluating the effects of the protein kinase C-beta inhibitor ruboxistaurin on skin microvascular blood flow and other measures of diabetic peripheral neuropathy. Diabetes Care. 2007 Apr;30(4):896-902. doi: 10.2337/dc06-1699. PMID: 17392551. 8: Anderson PW, McGill JB, Tuttle KR. Protein kinase C beta inhibition: the promise for treatment of diabetic nephropathy. Curr Opin Nephrol Hypertens. 2007 Sep;16(5):397-402. doi: 10.1097/MNH.0b013e3281ead025. PMID: 17693752. 9: Tuttle KR. Protein kinase C-beta inhibition for diabetic kidney disease. Diabetes Res Clin Pract. 2008 Nov 13;82 Suppl 1:S70-4. doi: 10.1016/j.diabres.2008.09.041. PMID: 18977550. 10: Meier M, Menne J, Haller H. Targeting the protein kinase C family in the diabetic kidney: lessons from analysis of mutant mice. Diabetologia. 2009 May;52(5):765-75. doi: 10.1007/s00125-009-1278-y. Epub 2009 Feb 24. PMID: 19238353. 11: Schwartz SG, Flynn HW Jr, Aiello LP. Ruboxistaurin mesilate hydrate for diabetic retinopathy. Drugs Today (Barc). 2009 Apr;45(4):269-74. doi: 10.1358/dot.2009.45.4.1354195. PMID: 19499092. 12: Beckman JA, Goldfine AB, Goldin A, Prsic A, Kim S, Creager MA. Inhibition of protein kinase Cbeta does not improve endothelial function in type 2 diabetes. J Clin Endocrinol Metab. 2010 Aug;95(8):3783-7. doi: 10.1210/jc.2010-0286. Epub 2010 May 5. PMID: 20444914; PMCID: PMC2913029.