| P32/98 (hemifumarate)competitive transition-state substrate analog inhibitor of DPP IV |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
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Chemical structure
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| Cas No. | 251572-86-8 | SDF | Download SDF |
| Chemical Name | (2S,3S)-2-amino-3-methyl-1-(3-thiazolidinyl)-1-pentanone, (2E)-2-butenedioate | ||
| Canonical SMILES | O=C([C@@H](N)[C@@H](C)CC)N1CCSC1.OC(/C=C/C(O)=O)=O | ||
| Formula | C9H18N2OS • 1/2C4H4O4 | M.Wt | 260.4 |
| Solubility | ≤1mg/ml in ethanol;15mg/ml in DMSO;5mg/ml in dimethyl formamide | Storage | Store at -20°C |
| Physical Appearance | A crystalline solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
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.
References: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).
