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Sitagliptin phosphate monohydrateDPP-4抑制剂

Sitagliptin phosphate monohydrate

产品编号:A4036
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规格 单价 库存 订购数量
10mM (in 1mL DMSO) ¥550.00 现货
200mg ¥600.00 现货
500mg ¥1,100.00 现货

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Sample solution is provided at 25 µL, 10mM.

引用文献

1. Mansur SA, Mieczkowska A, et al. "Sitagliptin Alters Bone Composition in High-Fat-Fed Mice." Calcif Tissue Int. 2018 Dec 18. PMID:30564859
2. Ghorpade DS, Ozcan L, et al. "Hepatocyte-secreted DPP4 in obesity promotes adipose inflammation and insulin resistance." Nature. 2018 Mar 29;555(7698):673-677. PMID:29562231
3.Mroz PA, Perez-Tilve D, et al. "Native Design of Soluble, Aggregation-Resistant Bioactive Peptides: Chemical Evolution of Human Glucagon." ACS Chem Biol. 2016 Dec 16;11(12):3412-3420. PMID:27797473
4.Khan D, Vasu S, et al. "Islet distribution of Peptide YY and its regulatory role in primary mouse islets and immortalised rodent and human beta-cell function and survival." Mol Cell Endocrinol. 2016 Jul 25;436:102-113. PMID:27465830
5.Gault, V. A., R. Lennox, and P. R. Flatt. "Sitagliptin, a DPP‐4 inhibitor, improves recognition memory, oxidative stress, hippocampal neurogenesis and up‐regulates key genes involved in cognitive decline." Diabetes, Obesity and Metabolism (2015). PMID:25580570

质量控制

化学结构

Sitagliptin phosphate monohydrate

相关生物数据

Sitagliptin phosphate monohydrate

相关生物数据

Sitagliptin phosphate monohydrate

相关生物数据

Sitagliptin phosphate monohydrate

相关生物数据

Sitagliptin phosphate monohydrate

相关生物数据

Sitagliptin phosphate monohydrate

相关生物数据

Sitagliptin phosphate monohydrate

相关生物数据

Sitagliptin phosphate monohydrate

Sitagliptin phosphate monohydrate Dilution Calculator

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Sitagliptin phosphate monohydrate Molarity Calculator

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化学性质

CAS号 654671-77-9 SDF Download SDF
别名 Tesavel, MK-0431,MK0431
化学名 (3R)-3-amino-1-[3-(trifluoromethyl)-6,8-dihydro-5H-[1,2,4]triazolo[4,3-a]pyrazin-7-yl]-4-(2,4,5-trifluorophenyl)butan-1-one;phosphoric acid;hydrate
SMILES [HH].C1CN2C(=NN=C2C(F)(F)F)CN1C(=O)CC(CC3=CC(=C(C=C3F)F)F)N.O.OOP(=O)=O
分子式 C16H15F6N5O.H3PO4.H2O 分子量 523.3
溶解度 ≥23.8 mg/mL in DMSO, <2.41 mg/mL in EtOH, ≥30.6 mg/mL in H2O with ultrasonic 储存条件 Store at -20°C
物理性状 A solid 运输条件 试用装:蓝冰运输。
其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议 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。

生物活性

描述 Sitagliptin phosphate是一种有效的DPP-IV抑制剂,在Caco-2细胞提取物中的IC50值为19 nM。
靶点 DPP-4          
IC50 19 nM          

实验操作

细胞实验 [1]:

细胞系

内皮祖细胞(EPC)和骨髓间充质干细胞(MSC)

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

14 d,25 μmol/L

实验结果

为了确定sitagliptin是否参与增强EPC和MSC的分化以及细胞表达配体SDF-1α,将脂肪组织与sitagliptin(25 μmol/L)在M199培养基中共培养14天,并通过流式细胞术分析。结果显示,与第7天的细胞培养物相比,在非sitagliptin处理(Si-T)和sitagliptin处理(Si-)T的第14天, EPCs [CD31/Sca-1+(双染色的)和CXCR4+(单染色的)]的数目显著增加。

动物实验 [2]:

动物模型

具有C57BL/6遗传背景的ApoE-/-小鼠

剂量

200 mg/kg/day,口服

实验结果

在ApoE-/-小鼠中,与对照组相比,sitagliptin组动脉粥样硬化斑块较少,为7.64±1.98%[范围4.62-10.13%],对照组为12.91±1.15%[范围11.55-14.37%],p < 0.001。与对照小鼠相比,给予sitagliptin的小鼠的主动脉根部和腹主动脉中的动脉粥样硬化斑块区域分别降低1.92和2.74倍(p = 0.011和p = 0.006)。数据显示,在ApoE-/-小鼠中,sitagliptin可以抑制整个主动脉、主动脉根和腹主动脉区域的动脉粥样硬化形成。

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] Chua S, Sheu J J, Chen Y L, et al. Sitagliptin therapy enhances the number of circulating angiogenic cells and angiogenesis—evaluations in vitro and in the rat critical limb ischemia model[J]. Cytotherapy, 2013, 15(9): 1148-1163.

[2] Zeng Y, Li C, Guan M, et al. The DPP-4 inhibitor sitagliptin attenuates the progress of atherosclerosis in apolipoprotein-E-knockout mice via AMPK-and MAPK-dependent mechanisms[J]. Cardiovascular diabetology, 2014, 13(1): 32.

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研究更新

1. Simultaneous Determination of Sitagliptin Phosphate Monohydrate and Metformin Hydrochloride in Tablets by a Validated UPLC Method. Sci Pharm. 2012;80(1):139-52. doi: 10.3797/scipharm.1110-13. Epub 2011 Dec 12.
Abstract
The reverse phase UPLC is a method to simultaneously measure Sitagliptin phosphate monohydrate and Metformin hydrochloride in pharmaceutical dosage forms with LOD and LOQ of 0.2 μg/mL and 0.7 μg/mL respectively for Sitagliptin phosphate monohydrate.
3. Efficacy and safety of initial combination treatment with sitagliptin and pioglitazone-a factorial study. Diabetes Obes Metab. 2014 Mar;16(3):223-30. doi: 10.1111/dom.12194. Epub 2013 Aug 29.
Abstract
The combination of sitagliptin and pioglitazone has been assessed for safety and efficacy in patients with type 2 diabetes.
4. Effects of short-term sitagliptin treatment on immune parameters in healthy individuals, a randomized placebo-controlled study. Clin Exp Immunol. 2013 Oct;174(1):120-8. doi: 10.1111/cei.12144.
Abstract
Sitagliptin is a DPP-4 inhibitor that inhibits the cleavage of GLP-1 leading to improved blood glucose control in patients with type 2 diabetes. Although it initially increased the percentage of cells expressing high levels of CD26, sitagliptin failed to alter systemic immune function in healthy volunteers at the end of 28-day treatment.

产品描述

Sitagliptin phosphate monohydrate是其活性成分西他列汀(sitagliptin)的磷酸盐加上一分子的水。Sitagliptin是二肽基肽酶(DPP-4)的有效抑制剂,选择性抑制DPP-4,IC50值为18 nM,而对其它的DDP酶(如DDP-8和DDP-9)没有亲和性。DPP-4是一种酶,催化N端为丙氨酸或脯氨酸残基的多肽水解。据报道,sitagliptin通过增加两种DPP-4底物的水平,包括胰高血糖素样肽-1(GLP-1)和肠抑胃肽(GIP),从而抑制DPP4。Sitagliptin目前正用于治疗II型糖尿病的研究。

参考文献:
Gallwitz B.  Review of sitagliptin phosphate: a novel treatment for type 2 diabetes. Vasc Health Risk Manag. 2007;3(2):203-10.