| CAS NO: | 251572-86-8 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| Cas No. | 251572-86-8 |
| 别名 | 异亮氨酸噻唑烷半富马酸盐 |
| 化学名 | (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 |
| 分子式 | C9H18N2OS o 1/2C4H4O4 |
| 分子量 | 260.4 |
| 溶解度 | ≤1mg/ml in ethanol;15mg/ml in DMSO;5mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | 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: |
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