[CAS NO. 169939-94-0] Ruboxistaurin

Name: Ruboxistaurin
Brand: Arctom Scientific
SKU: AS109560

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PRODUCTS SPECIFICATIONS [169939-94-0]

Distributor

Catalog

AS109560

Brand

Arctom Scientific

CAS

169939-94-0

DESCRIPTION [169939-94-0]

Overview

MDL	-
Molecular Weight	468.55
Molecular Formula	C28H28N4O3
SMILES	O=C1NC(C(C2=CN(C3=CC=CC=C32)CCO[C@H](CN(C)C)CC4)=C1C5=CN4C6=CC=CC=C56)=O

For research use only. We do not sell to patients.

8 Publications Citing Use of MCE

Summary

Ruboxistaurin (LY333531) is an orally active, selective PKC beta inhibitor ( K _i =2 nM). Ruboxistaurin exhibits ATP dependent competitive inhibition of PKC beta I with an IC ₅₀ of 4.7 nM. Ruboxistaurin inhibits PKC beta II with an IC ₅₀ of 5.9 nM ^[1] ^[2] .

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 is a selective and ATP-competitive PKCβ inhibitor, with IC ₅₀ s of 4.7 and 5.9 nM for PKCβI and PKCβII, shows less potent inhibition on PKCη (IC ₅₀ , 52 nM), PKCα (IC ₅₀ , 360 nM), PKCγ (IC ₅₀ , 300 nM), PKCδ (IC ₅₀ , 250 nM), and has no effect on PKCζ (IC ₅₀ , >100 μM) ^[1] . Ruboxistaurin (10 and 400 nM) dramatically inhibits glucose-induced monocyte adherence to levels that are not different from baseline adherence of monocytes to endothelial cells under NG conditions. Ruboxistaurin (10 and 400 nM) dose not alter the endothelial expression of adhesion molecules or modify endothelial cell growth ^[2] . Ruboxistaurin (LY333531; 10 nM) reduces high-glucose (HG)-induced human renal glomerular endothelial cells (HRGECs) viability, and inhibits the increases in swiprosin-1 in HRGECs incubated with HG ^[3] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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] .

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

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.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT00190970	Chromaderm, Inc.	Diabetic Neuropathy	October 2004	Phase 2
NCT00482976	Chromaderm, Inc.\|Joslin Diabetes Center	Diabetes Mellitus	December 2003	Phase 2
NCT00044148	Chromaderm, Inc.	Diabetic Nephropathy	July 16, 2002	Phase 2
NCT00604383	Chromaderm, Inc.	Diabetic Retinopathy	March 2001	Phase 3
NCT00090519	Chromaderm, Inc.	Diabetic Retinopathy	February 2004	Phase 3
NCT02769611	University of Tennessee\|The Christ Hospital	Heart Failure	June 28, 2017	Phase 1\|Phase 2
NCT00044395	Eli Lilly and Company	Diabetic Neuropathies\|Diabetes Mellitus, Insulin-Dependent\|Diabetes Mellitus, Non-Insulin-Dependent	July 2002	Phase 3
NCT00761852	Brigham and Women´s Hospital\|Eli Lilly and Company	Type 1 Diabetes Mellitus\|Type 2 Diabetes Mellitus	May 1999	Phase 2\|Phase 3
NCT00297401	Chromaderm, Inc.\|Heart and Stroke Foundation of Canada	Diabetes Mellitus, Type 1	March 2006	Phase 3
NCT00044421	Eli Lilly and Company	Diabetic Neuropathies\|Diabetes Mellitus	July 2002	Phase 3
NCT00133952	Chromaderm, Inc.	Diabetic Macular Edema	August 2005	Phase 3
NCT00266695	Chromaderm, Inc.	Diabetic Retinopathy	January 2006	Phase 3
NCT00552227	Chromaderm, Inc.	Diabetes Mellitus	September 2002	Phase 1
NCT00044408	Chromaderm, Inc.	Diabetic Neuropathies\|Diabetes Mellitus, Insulin-Dependent\|Diabetes Mellitus, Non-Insulin-Dependent	July 2002	Phase 3

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 25 mg/mL ( 53.36 mM ; ultrasonic and warming and heat to 60°C)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1342 mL	10.6712 mL	21.3424 mL
5 mM	0.4268 mL	2.1342 mL	4.2685 mL
10 mM	0.2134 mL	1.0671 mL	2.1342 mL

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

1.

Add each solvent one by one: 10% DMSO >> 40% PEG300 >> 5% Tween-80 >> 45% saline

Solubility: ≥ 1.67 mg/mL (3.56 mM); Suspended solution

* All of the co-solvents are available by MCE.

References

Synonyms

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)-

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-, (S)-

(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

LY 333531

Ruboxistaurin