中文名 | 鲁伯斯塔 |
英文名 | RUBOXISTAURIN MESYLATE |
别名 | 鲁伯斯塔 |
英文别名 | LY-333531 LY 333531 Ruboxistaurin Unii-721809wqcp UNII-721809WQCP Ruboxistaurin [INN] RUBOXISTAURIN MESYLATE Ruboxistaurin (LY333531) Ruboxistaurin (LY333531) (HCl salt) |
CAS | 169939-94-0 |
化学式 | C28H28N4O3 |
分子量 | 468.55 |
InChI | InChI=1/C28H28N4O3/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/h3-10,16-18H,11-15H2,1-2H3,(H,29,33,34)/t18-/m0/s1 |
密度 | 1.34 |
沸点 | 744.4±60.0 °C(Predicted) |
闪点 | 404°C |
蒸汽压 | 4.93E-22mmHg at 25°C |
折射率 | 1.695 |
酸度系数 | 8.26±0.40(Predicted) |
存储条件 | -20℃ |
产品用途 | 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. |
参考资料 展开查看 | 1: Pang C, Wen L, Lu X, Luo S, Qin H, Zhang X, Zhu B, Luo S. Ruboxistaurin maintains the bone mass of subchondral bone for blunting osteoarthritis progression by inhibition of osteoclastogenesis and bone resorption activity. Biomed Pharmacother. 2020 Sep 1;131:110650. doi: 10.1016/j.biopha.2020.110650. Epub ahead of print. PMID: 32882584. 2: Zestos AG, Carpenter C, Kim Y, Low MJ, Kennedy RT, Gnegy ME. Ruboxistaurin Reduces Cocaine-Stimulated Increases in Extracellular Dopamine by Modifying Dopamine-Autoreceptor Activity. ACS Chem Neurosci. 2019 Apr 17;10(4):1960-1969. doi: 10.1021/acschemneuro.8b00259. Epub 2018 Nov 8. PMID: 30384585; PMCID: PMC6470047. 3: Lewin AH, Brieaddy L, Deschamps JR, Imler GH, Mascarella SW, Reddy PA, Carroll FI. Synthesis and Characterization of the Selective, Reversible PKCβ Inhibitor (9 S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9 H,18 H-5,21:12,17-dimethenodibenzo[ e,k]pyrrolo[3,4- h][1,4,13]oxadiazacyclohexadecine-18,20(19 H)-dione, Ruboxistaurin (LY333531). ACS Chem Neurosci. 2019 Jan 16;10(1):246-251. doi: 10.1021/acschemneuro.8b00196. Epub 2018 Sep 11. PMID: 30156829. 4: Sharp TE 3rd, Kubo H, Berretta RM, Starosta T, Wallner M, Schena GJ, Hobby AR, Yu D, Trappanese DM, George JC, Molkentin JD, Houser SR. Protein Kinase C Inhibition With Ruboxistaurin Increases Contractility and Reduces Heart Size in a Swine Model of Heart Failure With Reduced Ejection Fraction. JACC Basic Transl Sci. 2017 Dec 25;2(6):669-683. doi: 10.1016/j.jacbts.2017.06.007. PMID: 3 |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 2.134 ml | 10.671 ml | 21.342 ml |
5 mM | 0.427 ml | 2.134 ml | 4.268 ml |
10 mM | 0.213 ml | 1.067 ml | 2.134 ml |
5 mM | 0.043 ml | 0.213 ml | 0.427 ml |
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