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磷酸西他列汀 /Sitagliptin phosphate {[allProObj[0].p_purity_real_show]}

货号：A111654 同义名： MK-0431 phosphate;(–)-Sitagliptin (phosphate)

Sitagliptin phosphate is a potent inhibitor of DPP4 with IC50 of 19 nM in Caco-2 cell extracts.

Sitagliptin phosphate 化学结构 CAS号：654671-78-0
Sitagliptin phosphate 化学结构
CAS号：654671-78-0
Sitagliptin phosphate 3D分子结构
CAS号：654671-78-0
Sitagliptin phosphate 化学结构 CAS号：654671-78-0
Sitagliptin phosphate 3D分子结构 CAS号：654671-78-0
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Sitagliptin phosphate 纯度/质量文件 产品仅供科研

货号：A111654 标准纯度： {[allProObj[0].p_purity_real_show]}
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Sitagliptin phosphate 生物活性

描述 The dipeptidyl peptidase 4 (DPP4) is a protein that presenting in various cells of the body and is associated with immune regulation, glucose metabolism and cardiovascular function[4]. Sitagliptin Phosphate is the phosphate form of Sitagliptin. Sitagliptin, which is used to treat diabetes, is a DPP4 inhibitor with IC50 value of 19 nM[5]. HLMVECs were treated with sitagliptin with 1000 μM for one hour and the DPP4 activity measured using a CD26/DPPIV Assay kit after four hours of PBS incubation was decreased significantly compared with the control group. The secreated cytokine levels detected by ELISA after LPS (1 μg/ml) for four hours was decreased significantly compared with the cells without sitagliptin treatment[6]. When sitagliptin was treated with LPS treated (10 μg/ml) H9c2 cells with concentration of 1 μM and above, the cytokines level measured by PCR and ELISA also decreased siginificantly compared with control. The NF-kB level measured by western blotting assay also decreased significantly[7]. In high salt diet Dahl salt-sensitive rats, sitagliptin was given to the rats orally daily with 10 mg/ kg for eight weeks. The survival rate of the sitagliptin treated group was higher than the control group, and the in situ assessment of DPP4 activity was reduced coupled with an increased expression of GLP-1 receptors from sitagliptin treated group, measured by immunofluorescence labelling and confocal microscopy[8].
作用机制 The sitagliptin is a competitive, tight and fast binding inhibitor to the DPP4. It can prolong the bioactivity of the native GLP-1 by inhibiting the proteolytic activity of the DPP4 enzyme[9].

Sitagliptin phosphate 动物研究

Dose Rat: 2 mg/kg - 180 mg/kg[3] (p.o.); 0.5 mg/kg - 5 mg/kg[3] (i.v.)
Administration p.o., i.v.
Pharmacokinetics
Animal Rats[3] Dogs[3]
Dose 2 mg/kg (i.v.) 1.5 mg/kg (i.v.)
1.6 mg/kg (p.o.)
Administration i.v. or p.o. i.v. or p.o.
T1/2 1.8 ± 0.3 h (i.v.)
2.6 ± 0.6 h (p.o.) 		4.4 ± 0.1 h (i.v.)
4.5 ± 0.7 h (p.o.)
Tmax 2.2 ± 1.8 h (p.o.) 0.8 ± 0.3 h (p.o.)
CLp 43 ± 1.3 ml/min/kg (i.v.) 8.9 ± 1.5 ml/min/kg (i.v.)
Cmax 0.21 ± 0.13 μM (p.o.) 1.32 ± 0.24 μM (p.o.)
Vdss 8.7 ± 3.1 L/kg (i.v.) 3.9 ± 0.8 L/kg (i.v.)
AUC0→∞ 1.93 ± 0.06 μM·h (i.v.)
1.17 ± 0.14 μM·h (p.o.) 		7.07 ± 1.37 μM·h (i.v.)
7.08 ± 1.52 μM·h (p.o.)

Sitagliptin phosphate 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00372060 Type 2 Diabetes Mellitus Phase 3 Completed - -
NCT00372060 - Completed - -
NCT01100125 Diabetes Phase 4 Completed - Korea, Republic of ... 展开 >> Seoul National University Bundang Hospital Seongnam, Gyeonggi, Korea, Republic of, 463-707 Seoul National University Bundang Hospital Seongnam, Korea, Republic of 收起 <<

Sitagliptin phosphate 参考文献

[1]Sangle GV, Lauffer LM, et al. Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology. 2012 Feb;153(2):564-73.

[2]Kim SJ, Nian C, et al. Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes. 2009 Mar;58(3):641-51.

[3]JANUVIA

[4]Salles TA, dos Santos L, Barauna VG, Girardi AC. Potential role of dipeptidyl peptidase IV in the pathophysiology of heart failure. Int J Mol Sci. 2015 Feb 16;16(2):4226-49.

[5]Röhrborn D, Wronkowitz N, Eckel J. DPP4 in Diabetes. Front Immunol. 2015 Jul 27;6:386.

[6]Kawasaki T, Chen W, Htwe YM, Tatsumi K, Dudek SM. DPP4 inhibition by sitagliptin attenuates LPS-induced lung injury in mice. Am J Physiol Lung Cell Mol Physiol. 2018 Nov 1;315(5):L834-L845.

[7]Lin CH, Lin CC. Sitagliptin attenuates inflammatory responses in lipopolysaccharide-stimulated cardiomyocytes via nuclear factor-κB pathway inhibition. Exp Ther Med. 2016 Jun;11(6):2609-2615.

[8]Esposito G, Cappetta D, Russo R, Rivellino A, Ciuffreda LP, Roviezzo F, Piegari E, Berrino L, Rossi F, De Angelis A, Urbanek K. Sitagliptin reduces inflammation, fibrosis and preserves diastolic function in a rat model of heart failure with preserved ejection fraction. Br J Pharmacol. 2017 Nov;174(22):4070-4086.

[9]Davis JA, Singh S, Sethi S, Roy S, Mittra S, Rayasam G, Bansal V, Sattigeri J, Ray A. Nature of action of Sitagliptin, the dipeptidyl peptidase-IV inhibitor in diabetic animals. Indian J Pharmacol. 2010 Aug;42(4):229-33.

Sitagliptin phosphate 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

1.98mL

0.40mL

0.20mL

9.89mL

1.98mL

0.99mL

19.79mL

3.96mL

1.98mL

Sitagliptin phosphate 技术信息

CAS号654671-78-0
分子式C16H18F6N5O5P
分子量 505.309
别名 MK-0431 phosphate;(–)-Sitagliptin (phosphate);(R)-Sitagliptin;ONO-5435;MK-431;INN
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,2-8°C
溶解度

DMSO: 105 mg/mL(207.79 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO

H2O: 50 mg/mL(98.95 mM)，配合低频超声助溶
动物实验配方

Tags: Sitagliptin | 654671-78-0 | MK-0431 | MK0431 | MK 0431 | Dipeptidyl Peptidase Inhibitor | Metabolic Enzyme/Protease | Autophagy | Dipeptidyl Peptidase | Autophagy | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Sitagliptin phosphate 纯度/质量文件 | Sitagliptin phosphate 生物活性 | Sitagliptin phosphate 动物研究 | Sitagliptin phosphate 临床数据 | Sitagliptin phosphate 参考文献 | Sitagliptin phosphate 实验方案 | Sitagliptin phosphate 技术信息

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