AH 7614
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.
靶点:FFA4/GPR120
IC50: N/A
AH7614是游离脂肪酸受体4(FFA4/GPR120)的有效选择性拮抗剂,对人、小鼠和大鼠受体的pIC50值分别为7.1、8.1和8.1[1]。游离脂肪酸受体4(FFA4/GPR120)属于G蛋白偶联受体家族的成员,是一种潜在的7TM受体,参与长链脂肪酸刺激的胰高血糖素样肽-1(GLP-1)的分泌。FFA4在肠内分泌细胞系STC-1和肠中高表达。GLP-1调节多种生理功能,包括饮食行为[2]。
体外实验:在表达FFA4受体的U2OS骨肉瘤细胞中,AH7614(0.063、0.25和1 μM)阻断亚油酸和GSK137647A诱导的细胞内钙增加[1]。另外,在MIN6小鼠胰岛细胞系中,在选择性FFA4拮抗剂AH7614(100 μM)存在下,50 μM的GSK137647A诱导的葡萄糖刺激的胰岛素分泌的增加被废除。此外,在NCIH716细胞中,AH7614(100 μM)阻断GSK137647A(100 μM)介导的GLP-1分泌的适度增加[1]。
体内实验:N / A
参考文献:
1. Sparks SM, Chen G, Collins JL, Danger D, Dock ST, Jayawickreme C, et al. Identification of diarylsulfonamides as agonists of the free fatty acid receptor 4 (FFA4/GPR120). Bioorg Med Chem Lett. 2014;24(14):3100-3.
2. Martin C, Passilly-Degrace P, Chevrot M, Ancel D, Sparks SM, Drucker DJ, et al. Lipid-mediated release of GLP-1 by mouse taste buds from circumvallate papillae: putative involvement of GPR120 and impact on taste sensitivity. J Lipid Res. 2012;53(11):2256-65.
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 351.42 |
Cas No. | 6326-06-3 |
Formula | C20H17NO3S |
Solubility | ≥35.1 mg/mL in DMSO; insoluble in EtOH; insoluble in H2O |
Chemical Name | 4-methyl-N-(9H-xanthen-9-yl)benzenesulfonamide |
SDF | Download SDF |
Canonical SMILES | O=S(NC1C2=C(C=CC=C2)OC3=CC=CC=C31)(C4=CC=C(C)C=C4)=O |
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。 |
细胞实验[1]: | |
细胞系 |
Flp-In T-REx 293细胞 |
溶解方法 |
在DMSO中的溶解度> 10 mM。为了获得更高浓度,可以将离心管在37℃加热10分钟和/或在超声波浴中震荡一段时间。原液可以在-20℃以下储存几个月。 |
反应条件 |
10-10 ~10-5 M,15分钟 |
应用 |
AH-7614可以强效和浓度依赖的方式抑制表达hFFA4-eYFP的Flp-In T-REx 293细胞中由ω-3脂肪酸aLA引发的Ca2 +动员的能力。作为FFA4的拮抗剂,AH-7614能够阻断多不饱和ω-6脂肪酸亚油酸的作用。 |
References: [1] Watterson KR, Hansen SVF, Hudson BD, et al. Probe-Dependent Negative Allosteric Modulators of the Long-Chain Free Fatty Acid Receptor FFA4. Mol Pharmacol. 2017 Jun;91(6):630-641. |
质量控制和MSDS
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