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P32/98 (hemifumarate) Sale

(Synonyms: 异亮氨酸噻唑烷半富马酸盐) 目录号 : GC14786

A DPP IV inhibitor

P32/98 (hemifumarate) Chemical Structure

Cas No.:251572-86-8

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Sample solution is provided at 25 µL, 10mM.


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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.

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).

Chemical Properties

Cas No. 251572-86-8 SDF
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 • 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°C
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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。
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1 mg 5 mg 10 mg
1 mM 3.8402 mL 19.2012 mL 38.4025 mL
5 mM 0.768 mL 3.8402 mL 7.6805 mL
10 mM 0.384 mL 1.9201 mL 3.8402 mL
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给药剂量 mg/kg 动物平均体重 g 每只动物给药体积 ul 动物数量
% DMSO % % Tween 80 % saline