Alogliptin (SYR-322)
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.
Alogliptin (SYR-322)是一种新型可口服的和高选择性的喹唑啉酮类二肽基肽酶-4(DPP-4)抑制剂。DPP-4是一种丝氨酸氨肽酶,催化多肽的裂解。Alogliptin有效抑制人DPP-4,IC50值为6.9 nM,而对密切相关的丝氨酸蛋白酶几乎没有抑制活性,包括DPP-2、DPP-8、DPP-9、成纤维细胞活化蛋白/seprase, 脯氨酰内肽酶和类胰蛋白酶(IC50 > 100,000 nM)。Alogliptin阻止DPP-4催化的GLP-1和GIP的降解,因而被用于2型糖尿病的治疗。GLP-1和GIP通过刺激葡萄糖依赖的胰岛素分泌,从而调控血糖水平。
参考文献:
Bumsup Lee, Lihong Shi, Daniel B. Kassel, Tomoko Asakawa, Koji Takeuchi and Ronald J. Christopher. Pharmacokinetic, pharmacodynamics, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys. European Journal of Pharmacology 589 (2008) 306-314
- 1. Hee Seok Jung, Mi Seon Seo, et al. "The anti-diabetic drug alogliptin induces vasorelaxation via activation of Kv channels and SERCA pumps." Eur J Pharmacol. 2021 May 5;898:173991. PMID:33684451
- 2. Tardif V, Muir R, et al. "Adenosine deaminase-1 delineates human follicular helper T cell function and is altered with HIV." Nat Commun. 2019 Feb 18;10(1):823. PMID:30778076
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 339.39 |
Cas No. | 850649-61-5 |
Formula | C18H21N5O2 |
Synonyms | Alogliptin,SYR322 |
Solubility | insoluble in H2O; ≥100 mg/mL in EtOH with ultrasonic; ≥14.75 mg/mL in DMSO |
Chemical Name | 2-[[6-[(3R)-3-aminopiperidin-1-yl]-3-methyl-2,4-dioxopyrimidin-1-yl]methyl]benzonitrile |
SDF | Download SDF |
Canonical SMILES | CN1C(=O)C=C(N(C1=O)CC2=CC=CC=C2C#N)N3CCCC(C3)N |
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 |
U937 组织细胞 |
溶解方法 |
该化合物在DMSO中的溶解度大于10 mM。若配制更高浓度的溶液,一般步骤如下:请将试管置于37℃加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20℃可放置数月 |
反应条件 |
5 nM,48h,抑制细胞增殖;1 nM,48h,抑制MMP-1分泌 |
实验结果 |
5 nM的Alogliptin抑制53%的细胞增殖。1 nM的Alogliptin显著抑制MMP-1分泌,表明Alogliptin对MMP的抑制作用与细胞增殖不相关。 |
动物实验[2]: | |
动物模型 |
Zucker fa/fa大鼠 |
剂量 |
基于体重和空腹血浆葡萄糖水平将8周龄的雄性Zucker fa/fa大鼠分成5组,即单独口服给予0.3、1、3或10 mg/kg的alogliptin(5 ml/kg剂量体积)或单独的媒介物(0.5%羧甲基纤维素)。在给药后30分钟,给大鼠施用葡萄糖溶液(1 g/kg,2 ml/kg剂量体积)。葡萄糖负荷后90分钟后,使用Accu-Chek血糖仪分析血糖浓度,并使用胰岛素ELISA试剂盒在葡萄糖负荷60分钟后分析血浆胰岛素浓度。 |
实验结果 |
与对照组相比,单次给予alogliptin后早期胰岛素分泌增加。对于0.3、1和3 mg/kg剂量的alogliptin,胰岛素分泌增加约1.5、1.5和1.8倍。在口服葡萄糖后,与对照组相比,alogliptin给药组的血糖波动显著降低。在0.3、1和3 mg/kg剂量组,平均基线调整血糖AUC0–90 min分别降低约31%、37%和41%。 |
注意事项 |
请测试所有化合物在室内的溶解度,实际溶解度和理论值可能略有不同。这是由实验系统的误差引起的,属于正常现象。 |
References: [1] Ta N N, Li Y, Schuyler C A, et al. DPP-4 (CD26) inhibitor alogliptin inhibits TLR4-mediated ERK activation and ERK-dependent MMP-1 expression by U937 histiocytes. Atherosclerosis, 2010, 213(2): 429-435. [2] Lee B, Shi L, Kassel D B, et al. Pharmacokinetic, pharmacodynamic, and efficacy profiles of alogliptin, a novel inhibitor of dipeptidyl peptidase-4, in rats, dogs, and monkeys. European journal of pharmacology, 2008, 589(1): 306-314. |
描述 | Alogliptin是一种有效的和选择性的DPP-4抑制剂,IC50值小于10 nM,比对DPP-8和DPP-9的选择性高10,000倍。 | |||||
靶点 | DPP-4 | |||||
IC50 | < 10 nM |
质量控制和MSDS
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