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Sitagliptin phosphate monohydrate Sale

(Synonyms: 西他列汀磷酸盐一水合物; MK-0431 phosphate monohydrate) 目录号 : GC10298

Sitagliptin phosphate monohydrate (MK-0431 phosphate monohydrate) 是一种有效的 DPP4 抑制剂,在 Caco-2 细胞提取物中的 IC50 为 19 nM。

Sitagliptin phosphate monohydrate Chemical Structure

Cas No.:654671-77-9

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10mM (in 1mL DMSO)
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200mg
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500mg
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Sample solution is provided at 25 µL, 10mM.

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实验参考方法

Cell experiment [1]:

Cell lines

Endothelial progenitor cells (EPCs) and bone marrow mesenchymalstem cells(MSC)

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20°C for several months.

Reaction Conditions

14 d; 25 μmol/L

Applications

To determine whether sitagliptin treatment participated in enhancing the differentiation of EPCs and MSCs and cells expressing its ligand, SDF-1α, adipose tissues were co-cultured with sitagliptin (25 μmol/L) in M199 culture medium for 14 d and examined by flow cytometric analysis. The results show that compared with the 7 d cell culture, the numbers of EPCs [CD31/Sca-1+(double-stained) and CXCR4+ (single-stained)] were remarkably higher at day 14 in both the non-sitagliptin-treated (Si-T) group and the Si-T group

Animal experiment [2]:

Animal models

ApoE−/−mice with the C57BL/6 genetic background

Dosage form

200 mg/kg/day; oral taken

Applications

In ApoE−/−mice, the sitagliptin group showed fewer atherosclerotic plaques than in controls (7.64±1.98% [range 4.62–10.13%] vs 12.91±1.15% [range 11.55–14.37%], p

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1] Chua S, Sheu J J, Chen Y L, et al. Sitagliptin therapy enhances the number of circulating angiogenic cells and angiogenesis—evaluations< i> in vitroand 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.

产品描述

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

Sitagliptin phosphate exhibits a potent inhibitory effect on DPP-4 with IC50 of 19 nM from Caco-2 cell extracts[1]. Sitagliptin reduces in vitro migration of isolated splenic CD4 T-cells through a pathway involving cAMP/PKA/Rac1 activation[2]. A recent study demonstrates that sitagliptin exerts a novel, direct action in order to stimulate GLP-1 secretion by the intestinal L cell through a DPP-4-independent, protein kinase A- and MEK-ERK1/2-dependent pathway. It therefore reduces the effect of autoimmunity on graft survival[3].

In vivo, the ED50 value of sitagliptin phosphate for inhibition of plasma DPP-4 activity is calculated to be 2.3 mg/kg 7 hour postdose and 30 mg/kg 24 hour postdose in freely fed Han-Wistar rats[1]. The streptozotocin-induced type 1 diabetes mouse model exhibits elevated DPP-4 levels in the plasma that can be substantially inhibited in mice on an Sitagliptin phosphate diet. This is achieved by a positive effect on the regulation of hyperglycemia, potentially through prolongation of islet graft survival[4]. The plasma clearance and volume of distribution of Sitagliptin phosphate are higher in rats (40-48 mL/min/kg, 7-9 L/kg) than in dogs (9 mL/min/kg, 3 L/kg); and its half-life is shorter in rats,2 hours compared with 4 hours in dogs[5].

References:
[1]. Thomas, L., et al. (R)-8-(3-amino-piperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylm ethyl)-3,7-dihydro-purine-2,6-dione (BI 1356), a novel xanthine-based dipeptidyl peptidase 4 inhibitor, has a superior potency and longer duration of acti
[2]. Kim, S.J., et al., Dipeptidyl peptidase IV inhibition with MK0431 improves islet graft survival in diabetic NOD mice partially via T-cell modulation. Diabetes, 2009. 58(3): p. 641-51.
[3]. Sangle, G.V., et al., Novel biological action of the dipeptidylpeptidase-IV inhibitor, sitagliptin, as a glucagon-like peptide-1 secretagogue. Endocrinology, 2012. 153(2): p. 564-73.
[4]. Kim, S.J., et al., Inhibition of dipeptidyl peptidase IV with sitagliptin (MK0431) prolongs islet graft survival in streptozotocin-induced diabetic mice. Diabetes, 2008. 57(5): p. 1331-9.
[5]. Beconi, M.G., et al. Disposition of the dipeptidyl peptidase 4 inhibitor sitagliptin in rats and dogs. Drug Metab Dispos, 2007. 35(4): p. 525-32.

Chemical Properties

Cas No. 654671-77-9 SDF
别名 西他列汀磷酸盐一水合物; MK-0431 phosphate monohydrate
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
Canonical 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, ≥ 30.6 mg/mL in Water with ultrasonic 储存条件 Store at -20°C
General tips 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。
为了提高溶解度,请将管子加热至37℃,然后在超声波浴中震荡一段时间。
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 1.9109 mL 9.5547 mL 19.1095 mL
5 mM 0.3822 mL 1.9109 mL 3.8219 mL
10 mM 0.1911 mL 0.9555 mL 1.9109 mL
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Research Update

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.