| Identification | Back Directory | [Name]
Thiazolidine,3-[(2S,3S)-2-aMino-3-Methyl-1-oxopentyl]-, (2E)-2-butenedioate (2:1) | [CAS]
251572-86-8 | [Synonyms]
P32/98 (hemifumarate)
WEOXCUQGVBLKQX-CXOKTDEKSA-N
Thiazolidine,3-[(2S,3S)-2-aMino-3-Methyl-1-oxopentyl]-, (2E)-2-butenedioate (2:1) | [Molecular Formula]
C13H22N2O5S | [MDL Number]
MFCD27976627 | [MOL File]
251572-86-8.mol | [Molecular Weight]
318.39 |
| Hazard Information | Back Directory | [Uses]
P32/98 is a dipeptidyl peptidase IV inhibitor which is used in hypertensive patients treated with antihpertensive drugs. | [Biological Activity]
ki: 126 nmp32/98 (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]. | [IC 50]
DPP-4: 130 nM (Ki) | [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). |
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Energy Chemical
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