Sitagliptin (phosphate)
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.
Sitagliptin is a dipeptidyl peptidase-4 (DPP4) inhibitor [1].
DPP4 is an antigenic enzyme expressed on the surface of most cell types associated with immune regulation, signal transduction and apoptosis. DPP4 is an intrinsic membrane glycoprotein and a serine exopeptidase that cleaves X-proline dipeptides from the N-terminus of polypeptides [2].
In vitro: Sitagliptin was a potent inhibitor for DPP-4 with an IC50 of 18 nM [1]. Sitagliptin inhibited DPP-8 with an IC50 of 48 μM. Sitagliptin showed no effect on several related peptidases, including DPP-9, DPP-II, and amino peptidase P [1].
Clinical trials: In patients with type 2 diabetes, once-daily sitagliptin monotherapy improved glycemic control in the fasting and postprandial states, improved measures of β-cell function. Sitagliptin was well tolerated [3]. Sitagliptin did not increase the risk of major adverse cardiovascular events, hospitalization for heart failure, or other adverse events [4].
References:
[1] Biftu T, Feng D, Qian X, et al. (3R)-4-[(3R)-3-Amino-4-(2, 4, 5-trifluorophenyl) butanoyl]-3-(2, 2, 2-trifluoroethyl)-1, 4-diazepan-2-one, a selective dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes[J]. Bioorganic & medicinal chemistry letters, 2007, 17(1): 49-52.
[2] Fleischer B. CD26: a surface protease involved in T-cell activation[J]. Immunology today, 1994, 15(4): 180-184.
[3] Aschner P, Kipnes M S, Lunceford J K, et al. Effect of the dipeptidyl peptidase-4 inhibitor sitagliptin as monotherapy on glycemic control in patients with type 2 diabetes[J]. Diabetes care, 2006, 29(12): 2632-2637.
[4] Green J B, Bethel M A, Armstrong P W, et al. Effect of sitagliptin on cardiovascular outcomes in type 2 diabetes[J]. New England Journal of Medicine, 2015, 373(3): 232-242.
Storage | Store at -20°C |
M.Wt | 505.3 |
Cas No. | 654671-78-0 |
Formula | C16H15F6N5O·H3PO4 |
Synonyms | INN,MK-431,ONO-5435 |
Solubility | ≥24.4 mg/mL in DMSO; insoluble in EtOH; ≥10.38 mg/mL in H2O with ultrasonic |
Chemical Name | (3R)-3-amino-1-[5,6-dihydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazin-7(8H)-yl]-4-(2,4,5-trifluorophenyl)-1-butanone, monophosphate |
SDF | Download SDF |
Canonical SMILES | FC1=CC(C[C@H](CC(N2CC3=NN=C(N3CC2)C(F)(F)F)=O)N)=C(C=C1F)F.O=P(OO)=O.[HH] |
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
- 批次: