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P32/98(hemifumarate)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
P32/98(hemifumarate)图片
CAS NO:251572-86-8
规格:98%
分子量:260.4
包装与价格:
包装价格(元)
1mg电议
5mg电议
10mg电议

产品介绍
competitive transition-state substrate analog inhibitor of DPP IV
CAS:251572-86-8
分子式:C9H18N2OS ? 1/2C4H4O4
分子量:260.4
纯度:98%
存储:Store at -20°C

Background:

Ki: 126 nM


P32/98 (hemifumarate) is an inhibitor of DPP IV.


Glucose-dependent insulinotropic polypeptide (GIP) and glucagon-like peptide 1 (GLP-1) are responsible for >50% of nutrient-stimulated insulin secretion. After being released into the circulation, GIP and GLP-1 are quickly inactivated by the circulating enzyme dipeptidyl peptidase IV (DPP IV).


In vitro: P32/98 was found to be able to block adipogenesis dose-dependently, starting at the concentration of 100 μM, and P32/98 could completely block adipogenesis in 3T3-L1 cell line at 500 μM concentration. In addition, the inhibitory effects of P32/98 was further confirmed by detecting the expression of adipocyte markers at the end of differentiation [1].


In vivo: In previou animal study, two groups of fa/fa Zucker rats were orally treated twice daily for three months with P32/98 at 20 mg/kg/day and monthly oral glucose tolerance tests (OGTTs) were conducted after drug washout. Results showed that after 12 weeks of P32/98 treatment, the peak OGTT blood glucose values in the treated rats averaged 8.5 mmol/l less than in the controls. In addition, the concomitant insulin resulted in an increased early-phase insulin response in the treated group. Moreover, in response to an 8.8 mmol/l glucose perfusion, pancreata from controls showed no increase in insulin secretion, while pancreata from P32/98-treated animals had a 3.2-fold rise in insulin secretion [2].


Clinical trial: Up to now, P32/98 is still in the preclinical development stage.


参考文献:
1.  Han R, Wang X, Bachovchin W, Zukowska Z, Osborn JW. Inhibition of dipeptidyl peptidase 8/9 impairs preadipocyte differentiation. Sci Rep. 2015 Aug 5;5:12348.
2.  J. A. Pospisilik, S. G. Stafford, H. U. Demuth, et al. Long-term treatment with the dipeptidyl peptidase IV inhibitor P32/98 causes sustained improvements in glucose tolerance, insulin sensitivity, hyperinsulinemia, and β-cell glucose responsiveness in VDF (fa/fa) zucker rats. Diabetes 51, 943-950 (2002).