Teneligliptin hydrobromide
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.
Teneligliptin hydrobromide是一种新型有效和持久的二肽基肽酶-4(DPP-4)抑制剂,具有抗氧化特性;在体外竞争性抑制人血浆、大鼠血浆和人重组DPP-4,IC50值约1 nM [1]。
DPP4也称为腺苷脱氨酶复合蛋白2或CD26。DPP4是在大多数细胞类型表面表达的抗原性酶,与免疫调节、信号转导和细胞凋亡有关[2]。
体外实验:在人脐静脉内皮细胞中,Teneligliptin促进抗氧化反应,降低ROS水平以及诱导Nrf2靶基因信使核糖核酸表达。在暴露于高葡萄糖的HUVEC中,Teneligliptin提高增殖速率,调节细胞周期抑制剂标志物P53、P21和P27的表达,减少促凋亡基因BAX和CASP3的表达,而促进BCL2表达。Teneligliptin改善高葡萄糖诱导的内质网应激。Teneligliptin具有抗氧化性能并克服HUVEC缓慢暴露于高葡萄糖诱导的代谢记忆效应[3]。
在体实验:在teneligliptin治疗的小鼠中,血清丙氨酸转氨酶和肝内甘油三酯水平显著降低(p < 0.05)。Teneligliptin还显著下调参与从头脂肪生成的基因的肝mRNA水平(p < 0.05)。此外,Teneligliptin上调磷酸化的AMP活化蛋白激酶(AMPK)的肝表达水平[4]。在维持高脂肪饮食的卵巢切除(OVX)成年小鼠中,每日一次口服20 mg,Teneligliptin有效地改善与绝经后肥胖相关的代谢异常特征。Teneligliptin改善黑暗和明亮阶段的能量消耗,减少黑暗阶段的运动活动,并降低OVX-HF中的核心体温 [5]
参考文献:
Kishimoto M. Teneligliptin: a DPP-4 inhibitor for the treatment of type 2 diabetes[J]. Diabetes, metabolic syndrome and obesity: targets and therapy, 2013, 6: 187.
Kameoka J, Tanaka T, Nojima Y, et al. Direct association of adenosine deaminase with a T cell activation antigen, CD26[J]. Science, 1993, 261(5120): 466-469.
Pujadas G, De Nigris V, Prattichizzo F, et al. The dipeptidyl peptidase-4 (DPP-4) inhibitor teneligliptin functions as antioxidant on human endothelial cells exposed to chronic hyperglycemia and metabolic high-glucose memory[J]. Endocrine, 2016: 1-12.
Ideta T, Shirakami Y, Miyazaki T, et al. The Dipeptidyl Peptidase-4 Inhibitor Teneligliptin Attenuates Hepatic Lipogenesis via AMPK Activation in Non-Alcoholic Fatty Liver Disease Model Mice[J]. International journal of molecular sciences, 2015, 16(12): 29207-29218.
Sameshima A, Wada T, Ito T, et al. Teneligliptin improves metabolic abnormalities in a mouse model of postmenopausal obesity[J]. Journal of Endocrinology, 2015, 227(1): 25-36.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 1257.72 |
Cas No. | 906093-29-6 |
Formula | C44H65Br5N12O2S2 |
Solubility | ≥62.9 mg/mL in DMSO; ≥104.8 mg/mL in H2O; ≥12.1 mg/mL in EtOH with gentle warming and ultrasonic |
Chemical Name | [(2S,4S)-4-[4-(5-methyl-2-phenylpyrazol-3-yl)piperazin-1-yl]pyrrolidin-2-yl]-(1,3-thiazolidin-3-yl)methanone;pentahydrobromide |
SDF | Download SDF |
Canonical SMILES | CC1=NN(C(=C1)N2CCN(CC2)C3CC(NC3)C(=O)N4CCSC4)C5=CC=CC=C5.CC1=NN(C(=C1)N2CCN(CC2)C3CC(NC3)C(=O)N4CCSC4)C5=CC=CC=C5.Br.Br.Br.Br.Br |
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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