(R)-Lisofylline
CAS No. 100324-81-0
(R)-Lisofylline ( —— )
产品货号. M27451 CAS No. 100324-81-0
(R)-Lisofylline 是一种溶血磷脂酸酰基转移酶抑制剂 (IC50 = 0.6 μM)。
纯度: >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| 规格 | 价格/人民币 | 库存 | 数量 |
| 500MG | 获取报价 | 有现货 |
|
| 1G | 获取报价 | 有现货 |
|
生物学信息
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产品名称(R)-Lisofylline
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注意事项本公司产品仅用于科研实验,不得用于人体或动物的临床与诊断
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产品简述(R)-Lisofylline 是一种溶血磷脂酸酰基转移酶抑制剂 (IC50 = 0.6 μM)。
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产品描述(R)-Lisofylline is an inhibitor of lysophosphatidic acid acyltransferase (IC50 = 0.6 μM). (R)-Lisofylline interrupts IL-12 signaling-mediated STAT4 activation and can be used in studies about the treatment of type 1 diabetes and autoimmune disorders.(In Vitro):(R)-Lisofylline blocks IL-12-driven T cell proliferation and Th1 differentiation yet has no effect on IL-12 secretion.(In Vivo):In NOD mice, (R)-Lisofylline prevents β cell dysfunction by inhibition of STAT4 phosphorylation and ameliorates experimental allergic encephalomyelitis. (R)-Lisofylline reduces the impairment of insulin secretion induced by IL-1β in cultured rat islet cells, suppresses IFN-γ production, the onset of diabetes, and macrophage infiltration into islets. (R)-Lisofylline improves insulin response and lowers glucose levels in Streptozotocin-treated rats after the oral glucose tolerance test. In rats given IL-1 intratracheally (R)-Lisofylline pretreatment reduces lung leak but does not decrease neutrophil accumulation in lungs. (R)-Lisofylline improves survival in mice injected with a lethal dose of LPS and ameliorates sepsis-induced lung injury in minipigs.
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体外实验(R)-Lisofylline blocks IL-12-driven Th1 differentiation and T cell proliferation in vitro, yet has no effect on IL-12 secretion from APCs ex vivo or in vitro.
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体内实验(R)-Lisofylline reduces the impairment of insulin secretion induced by IL-1β in cultured rat islet cells, suppresses IFN-γ production, the onset of diabetes, and macrophage infiltration into islets from NOD mice, as well as Lisofylline improves insulin response and lowers glucose levels in Streptozotocin-treated rats after the oral glucose tolerance test.(R)-Lisofylline prevents β cell dysfunction in NOD mice by inhibition of STAT4 phosphorylation which interrupts IL-12 signaling. (R)-Lisofylline ameliorates experimental allergic encephalomyelitis in mice. (R)-Lisofylline also improves survival in mice injected with a lethal dose of LPS and ameliorates sepsis-induced lung injury in minipigs. In rats given IL-1 intratracheally (R)-Lisofylline pretreatment reduces lung leak but does not decrease neutrophil accumulation in lungs. (R)-Lisofylline also suppresses release of TNF-α in vivo in mice and ex vivo in human blood stimulated with endotoxin derived from Salmonella or Escherichia coli.
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同义词——
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通路JAK/STAT Signaling
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靶点STAT
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受体Cereblon|PEGs
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研究领域——
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适应症——
化学信息
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CAS Number100324-81-0
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分子量280.32
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分子式C13H20N4O3
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纯度>98% (HPLC)
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溶解度In Vitro:?DMSO : 100 mg/mL (356.74 mM)
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SMILESO=C1C2=C(N(C)C(=O)N1CCCC[C@@H](C)O)N=CN2C
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化学全称——
运输与储存
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储存条件(-20℃)
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运输条件With Ice Pack
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稳定性≥ 2 years
参考文献
1.Li Y, et al. Discovery of MD-224 as a First-in-Class, Highly Potent, and Efficacious Proteolysis Targeting Chimera Murine Double Minute 2 Degrader Capable of Achieving Complete and Durable Tumor Regression. J Med Chem. 2019 Jan 24;62(2):448-466.
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