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LY 333531 hydrochloride

(Synonyms: LY333531 hydrochloride)

目录号: PC15985 纯度: ≥98%

PKCβ抑制剂，Ruboxistaurin hydrochlorid是蛋白激酶C的抑制剂，是PKCβI 和 PKCβII竞争性可逆的抑制剂，IC50分别是4.7 nM和5.9 nM.

CAS No. :169939-93-9

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中文名称	LY 333531 hydrochloride
中文别名	鲁伯斯塔盐酸盐;芦布妥林
英文名称	LY 333531 hydrochloride
英文别名	Ruboxistaurin Hydrochloride;LY 333531 hydrochloride;LY333531 (hydrochloride);LY-333531HCL;Ruboxistaurin Hydroc;LY-333531 hydrochloride;Ruboxistaurin-d6 Hydrochloride;UNII-6496V4OCZN;(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 hydrochloride;Ruboxistaurin;(S)-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 monohydrochloride;Ruboxistaurin HCl;Ruboxistaurin (hydrochloride);LY333531 HCl;6496V4OCZN;LY333531;Ruboxistaurin(hydrochloride);Ruboxistaurin (LY333531 HCl);s7663;LY 333531-d6
Cas No.	169939-93-9
分子式	C₂₈H₂₉ClN₄O₃
分子量	505.01
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	PKCβ抑制剂，Ruboxistaurin hydrochlorid是蛋白激酶C的抑制剂，是PKCβI 和 PKCβII竞争性可逆的抑制剂，IC50分别是4.7 nM和5.9 nM.

生物活性

Ruboxistaurin (LY333531) hydrochloride is an orally active, selective PKC beta inhibitor (K_i=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.

性状

Solid

IC50 & Target[1][2]

PKCβI

4.7 nM (IC₅₀)

PKCβII

5.9 nM (IC₅₀)

PKCη

52 nM (IC₅₀)

PKCδ

250 nM (IC₅₀)

PKCγ

300 nM (IC₅₀)

PKCα

360 nM (IC₅₀)

PKCε

600 nM (IC₅₀)

体外研究(In Vitro)

Ruboxistaurin hydrochloride is a selective and ATP-competitive PKCβ inhibitor, with IC₅₀s of 4.7 and 5.9 nM for PKCβI and PKCβII, shows less potent inhibition on PKCη (IC₅₀, 52 nM), PKCα (IC₅₀, 360 nM), PKCγ (IC₅₀, 300 nM), PKCδ (IC₅₀, 250 nM), and has no effect on PKCζ (IC₅₀, >100 μM). 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. 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.

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

体内研究(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. 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.

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

运输条件

Room temperature or refrigerated transportation.

储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. 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 kinas [Information]

[2]. Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-199. [Information]

[3]. Kunt T, et al. The beta-specific protein kinase C inhibitor ruboxistaurin (LY333531) suppresses glucose-induced adhesion of human monocytes to endothelial cells 体外研究. J Diabetes Sci Technol. 2007 Nov;1(6):929-35. [Information]

[4]. 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. [Information]

溶解度数据

体外研究:

DMSO : 6.67 mg/mL (13.21 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.9802 mL	9.9008 mL	19.8016 mL
5 mM	0.3960 mL	1.9802 mL	3.9603 mL
10 mM	0.1980 mL	0.9901 mL	1.9802 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 0.67 mg/mL (1.33 mM); Clear solution

此方案可获得 ≥ 0.67 mg/mL (1.33 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH?O 中，得到澄清透明的生理盐水溶液
2.

建议依照次序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 0.67 mg/mL (1.33 mM); Clear solution

此方案可获得 ≥ 0.67 mg/mL (1.33 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 6.7 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明

搜索质检报告(COA)

产品使用指南

Data Sheet

[1]. 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 kinas [Information]

[2]. Ruboxistaurin: LY 333531. Drugs R D. 2007;8(3):193-199. [Information]

[3]. Kunt T, et al. The beta-specific protein kinase C inhibitor ruboxistaurin (LY333531) suppresses glucose-induced adhesion of human monocytes to endothelial cells 体外研究. J Diabetes Sci Technol. 2007 Nov;1(6):929-35. [Information]

[4]. 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. [Information]

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

LY 333531 hydrochloride

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