TUG-770
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50: 6 nM
TU-770是一种强效的游离脂肪酸受体1(FFA1/GPR40)激动剂。游离脂肪酸受体1(FFA1或GPR40)增强葡萄糖刺激的胰腺β细胞胰岛素分泌,作为治疗2型糖尿病的新靶点引起了极大关注。
体外实验:TU-770对FFA1表现出显著增加的效力,EC50 = 6 nM,选择性优于FFA4 150倍。 TUG-770显示出优于FFA2、FFA3、PPARγ以及54种不同转运蛋白、受体和酶的高选择性。在大鼠INS-1E细胞系中,TU-770在高葡萄糖浓度下引起显著的胰岛素分泌增加,在低葡萄糖浓度下如预期没有效果[1]。
体内:TU-770在小鼠中的药代动力学研究显示出快速口服吸收、较高血浆浓度、较长半衰期、较低清除率和增加的生物利用度。每天口服20 mg/kg治疗4周以及250 mg/kg剂量急性治疗后,未出现小鼠不良反应。在正常小鼠的急性腹膜内葡萄糖耐受性试验中,TUG-770的体内检查显示出良好的剂量依赖性反应,血糖水平最大降低50 mg/kg。随后进行的DIO小鼠慢性口服葡萄糖耐受性试验表明,TU-770比其类似物更为有效。在大鼠中的进一步评估确认了高剂量TUG-770显著的降低葡萄糖作用[1]。
临床试验:N/A
参考文献:
[1] Christiansen E,Hansen SV,Urban C,Hudson BD,Wargent ET,Grundmann M,Jenkins L,Zaibi M,Stocker CJ,Ullrich S,Kostenis E,Kassack MU,μMilligan G,Cawthorne MA,Ulven T. Discovery of TUG-770: A Highly Potent Free Fatty Acid Receptor 1 (FFA1/GPR40) Agonist for Treatment of Type 2 Diabetes. ACS Med Chem Lett.2013 May 9;4(5):441-445.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 307.32 |
Cas No. | 1402601-82-4 |
Formula | C19H14FNO2 |
Synonyms | TUG770;TUG 770 |
Solubility | insoluble in H2O; ≥11.85 mg/mL in DMSO; ≥9.5 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | 3-[4-[2-[2-(cyanomethyl)phenyl]ethynyl]-2-fluorophenyl]propanoic acid |
SDF | Download SDF |
Canonical SMILES | C1=CC=C(C(=C1)CC#N)C#CC2=CC(=C(C=C2)CCC(=O)O)F |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
质量控制和MSDS
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