產(chǎn)品描述: | CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons. |
靶點(diǎn): |
PI3Kγ:30 nM (IC50, Neurons);Apoptosis;PI3K |
體內(nèi)研究: |
Administration of CAY10505 (0.6 mg/kg, p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly increases serum nitrite and (or) nitrate concentrations in hypertensive rats. Acetylcholine (ACh) and Sodium nitroprusside (SNP) produce endothelium-dependent and-independent relaxation in isolated rat aortic ring precontracted with Phenylephrine (3 μM), in a dose dependent manner. Administration of CAY10505 (0.6 mg/kg,p.o.), Losartan (25 mg/kg, p.o.), or Atorvastatin (30 mg/kg, p.o.) significantly prevents hypertension-induced attenuation of ACh-induced endothelium-dependent relaxation. Deoxycorticosterone acetate salt (DOCA, 40 mg/kg, s.c.) induced hypertension markedly attenuates acetylcholine-induced endothelium-dependent relaxation, but does not affect SNP-induced endotheliumindependent relaxation |
參考文獻(xiàn): |
1. Sun YY, Lin SH et al. Cell type-specific dependency on the PI3K/Akt signaling pathway for the endogenous Epo and VEGF induction by baicalein in neurons versus astrocytes. 2013 Jul 19;8(7):e69019. 2. Tyagi S. Effect of phosphatidylinositol 3-kinase-γ inhibitor CAY10505 in hypertension, and its associated vascular endothelium dysfunction in rats. Can J Physiol Pharmacol. 2012 Jul, 90(7), 881-5. 3. Hofmann C, et al. PI3K-dependent multiple myeloma cell survival is mediated by the PIK3CA isoform. Br J Haematol. 2014 Aug;166(4):529-39. 4. Jingyi Wang, et al. MiR-1976 Knockdown Promotes Epithelial-Mesenchymal Transition and Cancer Stem Cell Properties Inducing Triple-Negative Breast Cancer Metastasis. Cell Death Dis. 2020 Jul 3;11(7):500. |
溶解性: |
DMSO : ≥ 34 mg/mL (117.53 mM) |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
3.457 ml |
17.284 ml |
34.569 ml |
5 mM |
0.691 ml |
3.457 ml |
6.914 ml |
10 mM |
0.346 ml |
1.728 ml |
3.457 ml |
50 mM |
0.069 ml |
0.346 ml |
0.691 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |