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(R)-Lisofylline
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
(R)-Lisofylline图片
CAS NO:100324-81-0

(R)-Lisophylline
(R)-Lisofylline ((R)-Lisophylline) 是一种 Pentoxifylline 代谢产物的 (R)-型对映体,具有抗炎特性。(R)-Lisofylline 是一种溶血磷脂酸酰基转移酶 (lysophosphatidic acid acyltransferase) 抑制剂,IC50为 0.6 μM,可中断 IL-12 信号介导的STAT4激活。(R)-Lisofylline 可用于 1 型糖尿病,自身免疫性疾病的研究。
生物活性

(R)-Lisofylline ((R)-Lisophylline) is a (R)-enantiomer of the metabolite of Pentoxifylline with anti-inflammatory properties. (R)-Lisofylline is alysophosphatidic acidacyltransferaseinhibitor with anIC50of 0.6 μM and interruptsIL-12signaling-mediatedSTAT4activation. (R)-Lisofylline has the potential for type 1 diabetes, autoimmune disorders research[1][2].

IC50& Target

IC50: 0.6 μM (Lysophosphatidic acid acyltransferase)[1]
STAT4[1]

体外研究
(In Vitro)

(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[3].

体内研究
(In Vivo)

(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[1].
(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[1].
(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[1].
(R)-Lisofylline also suppresses release of TNF-α in vivo in mice and ex vivo in human blood stimulated with endotoxin derived from Salmonella orEscherichia coli[1].

分子量

280.32

性状

Solid

Formula

C13H20N4O3

CAS 号

100324-81-0

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 100 mg/mL(356.74 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM3.5674 mL17.8368 mL35.6735 mL
5 mM0.7135 mL3.5674 mL7.1347 mL
10 mM0.3567 mL1.7837 mL3.5674 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80℃, 6 months; -20℃, 1 month (stored under nitrogen)。-80℃ 储存时,请在 6 个月内使用,-20℃ 储存时,请在 1 个月内使用。

 
 
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