生物活性: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].
体外研究(In Vitro):Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].
瑞禧生物 has not independently confirmed the accuracy of these methods. They are for reference only.
Ruboxistaurin-d6 hydrochloride 相关抗体:
Phospho-PKC alpha (T638) Antibody
Phospho-PKC zeta (T560) Antibody
PKC alpha Antibody
PKC beta 1 Antibody
PKC beta 2 Antibody
PKC delta Antibody
PKC epsilon Antibody
PKC gamma Antibody
Ezrin Antibody (YA767)
PKC eta Antibody
SGK1 Antibody (YA1525)
PKC theta Antibody (YA3162)
Villin Antibody
Phospho-PKC alpha (Ser657) Antibody (YA1023)
Phospho-PKC alpha (Thr638) Antibody (YA1024)
PRKCQ Antibody (YA1106)
AMHR2 Antibody (YA1337)
Phospho-PKC (Ser660) Antibody (YA1394)
Phospho-PKC delta (Ser299) Antibody (YA2628)
Phospho-PKC zeta/lambda (Thr410/Thr412) Antibody (YA2631)
Phospho-PKC zeta (Thr560) Antibody (YA2679)
分子量:511.04
Formula:C28H23D6ClN4O3
CAS 号:1794767-04-6
非标记 CAS:169939-93-9
中文名称:鲁伯斯塔盐酸盐 d6
运输条件:Room temperature in continental US; may vary elsewhere.
储存方式:Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
Data Sheet (534 KB)
产品使用指南 (1538 KB)
参考文献
[1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.
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[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.
[Content Brief]
[3]. Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-199.
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[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.
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[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.
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