S80315 |
Ro 31-8220 Mesylate |
源葉(MedMol) | 99% |
- 提示:詳情請下載說明書。
- 產(chǎn)品描述: Ro 31-8220 mesylate is a potent PKC inhibitor, with IC50s of 5, 24, 14, 27, 24 and 23 nM for PKCα, PKCβI, PKCβII, PKCγ, PKCε and rat brain PKC, respectively. Ro 31-8220 also significantly inhibits MAPKAP-K1b, MSK1, S6K1 and GSK3β (IC50s, 3, 8, 15, and 38 nM, respectively), with no effect on MKK3, MKK4, MKK6 and MKK7.
- 靶點: PKC-α:5 nM (IC50);PKC-βI:24 nM (IC50);PKC-βII:14 nM (IC50);PKC-γ:27 nM (IC50);PKC-ε:24 nM (IC50);Rat Brain PKC:23 nM (IC50);MAPKAP-K1b:3 nM (IC50);MSK1:8 nM (IC50);S6K1:15 nM (IC50);GSK3β:38 nM (IC50);PKC
- 體內(nèi)研究:
Ro 31-8220 (6 mg/kg/d, s.c.) is well tolerated, and has half-life of 5.7 hours in mice. Ro 31-8220-treated MLP?/? mice show a dramatic rescue in fractional shortening after treatment for 6 weeks, but the WT mice shows no change
- 參考文獻:
1. Wilkinson SE, et al. Isoenzyme specificity of bisindolylmaleimides, selective inhibitors of protein kinase C. Biochem J. 1993 Sep 1;294 (Pt 2):335-7. 2. Davies SP, et al. Specificity and mechanism of action of some commonly used protein kinase inhibitors. Biochem J. 2000 Oct 1;351(Pt 1):95-105. 3. Tian F, et al. Inhibition of protein kinase C protects against paraoxon-mediated neuronal cell death. Neurotoxicology. 2007 Jul;28(4):843-9. Epub 2007 Apr 20. 4. Hambleton M, et al. Pharmacological- and gene therapy-based inhibition of protein kinase Calpha/beta enhances cardiac contractility and attenuates heart failure. Circulation. 2006 Aug 8;114(6):574-82.
- 溶解性: DMSO : 35.71 mg/mL (64.50 mM; Need ultrasonic) H2O : < 0.1 mg/mL (insoluble)
- 保存條件: -20℃
- 配置溶液濃度參考:
1mg 5mg 10mg 1 mM 1.806 ml 9.031 ml 18.062 ml 5 mM 0.361 ml 1.806 ml 3.612 ml 10 mM 0.181 ml 0.903 ml 1.806 ml 50 mM 0.036 ml 0.181 ml 0.361 ml
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輸入產(chǎn)品批號:
本計算器可幫助您計算出特定溶液中溶質(zhì)的質(zhì)量、溶液濃度和體積之間的關(guān)系,公式為:
質(zhì)量 (mg) = 濃度 (mM) x 體積 (mL) x 分子摩爾量 (g/mol)