产品
编 号：F077807
分子式：C14H8FNO3S
分子量：289.28
分子式：C14H8FNO3S
分子量：289.28
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规格
价格
是否有货
10mM*1mL in DMSO
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5mg
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10mg
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25mg
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50mg
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100mg
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CAS No: 1218777-13-9
产品详情
生物活性：
CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons.
体内研究：
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.
体外研究：
A class IB PI3Kγ isoform inhibitor CAY10505 at 200 nM (IC50=30 nM) partially reduces the baicalein-induced Akt phosphorylation in neurons. The pharmacological PI3K inhibitor CAY10505 (PIK3CG) is tested on an extended panel of multiple myeloma (MM) cell lines and freshly isolated primary MM samples. MM cells are CAY10505-treated for 3 d (MM cell lines) or 5 d (primary MM cells) respectively, and survival is analysed by flow cytometry (annexin V-FITC/PI staining). Treatment of bone marrow stromal cells (BMSCs)-co-cultured primary MM samples with the PIK3CA inhibitor CAY10505 results in anti-survival effects (mean survival relative to DMSO-treated controls: CAY10505: 84±14%, tested at 10 μM).
CAY10505 is a potent and selective PI3Kγ inhibitor with an IC50 of 30 nM in neurons.
体内研究：
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.
体外研究：
A class IB PI3Kγ isoform inhibitor CAY10505 at 200 nM (IC50=30 nM) partially reduces the baicalein-induced Akt phosphorylation in neurons. The pharmacological PI3K inhibitor CAY10505 (PIK3CG) is tested on an extended panel of multiple myeloma (MM) cell lines and freshly isolated primary MM samples. MM cells are CAY10505-treated for 3 d (MM cell lines) or 5 d (primary MM cells) respectively, and survival is analysed by flow cytometry (annexin V-FITC/PI staining). Treatment of bone marrow stromal cells (BMSCs)-co-cultured primary MM samples with the PIK3CA inhibitor CAY10505 results in anti-survival effects (mean survival relative to DMSO-treated controls: CAY10505: 84±14%, tested at 10 μM).
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