FK614
目录号: PL10040 纯度: ≥99%
CAS No. :193012-35-0
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中文名称
FK614
英文名称
FK614
英文别名
1H-Benzimidazole-6-carboxamide,1-[(2,4-dichlorophenyl)methyl]-2-methyl-N-(pentylsulfonyl)-;3-[(2,4-dichlorophenyl)methyl]-2-methyl-N-pentylsulfonylbenzimidazole-5-carboxamide;FK614
Cas No.
193012-35-0
分子式
C21H23N3O3Scl2
分子量
468.40
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
FK614 是一种口服活性非噻唑烷二酮 (TZD) 型选择性 PPARγ 调节剂 (SPPARM)。FK614 是一种 PPARγ 激动剂,显示出强大的抗糖尿病活性。FK614 在脂肪细胞分化的各个阶段对 PPARγ 的激活有不同的影响。FK614 可用于研究高血糖、高甘油三酯血症、糖耐量异常和 2 型糖尿病。
生物活性
FK614 is an orally active, non-thiazolidinedione (TZD) type, and selective PPARγ modulator (SPPARM). FK614 functions as a PPARγ agonist with potent anti-diabetic activity in vivo. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation. FK614 can be used for the research of hyperglycemia, hypertriglyceridemia, glucose intolerance and type 2 diabetes.
性状
Solid
IC50 & Target[1][2]
PPAR-γ
体外研究(In Vitro)
FK614 (0.1~10000 nM; 24 hours; CV-1 cells) activates PPARγ-dependent transcription in a concentration-dependent manner. FK614 (0~0.1 μM; 5 days; 3T3-L1 adipocytes) makes triglyceride content increased in a concentration-dependent manner. FK614 has different effects on the activation of PPARγ at each stage of adipocyte differentiation.
FK614 is an insulin sensitizer potentially for treatment of postherpetic neuralgia. FK614 is a non-TZD insulin sensitizer. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
FK614 (0.32~3.2 mg/kg; p.o.; 14 days) dose-dependently reduces plasma glucose level.
FK614 (0.1~10 mg/kg; p.o.; 14 days) improves the impaired glucose tolerance. has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Fujimura T, et al. A selective peroxisome proliferator-activated receptor gamma modulator with distinct fat cell regulation properties. J Pharmacol Exp Ther. 2006;318(2):863-871.
[2]. Fujimura T, et al. FK614, a novel peroxisome proliferator-activated receptor gamma modulator, induces differential transactivation through a unique ligand-specific interaction with transcriptional coactivators. J Pharmacol Sci. 2005;99(4):342-352.
溶解度数据
In Vitro: DMSO : 100 mg/mL (213.49 mM; Need ultrasonic)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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