Product Name :
P32/98 (hemifumarate)
Description:
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 . 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 . Clinical trial: Up to now, P32/98 is still in the preclinical development stage.
CAS:
251572-86-8
Molecular Weight:
318.39
Formula:
C13H22N2O5S
Chemical Name:
(2E)-but-2-enedioic acid; (2S,3S)-2-amino-3-methyl-1-(1,3-thiazolidin-3-yl)pentan-1-one
Smiles :
C[C@@H](CC)[C@H](N)C(=O)N1CSCC1.{{Fluvastatin} web|{Fluvastatin} Apoptosis|{Fluvastatin} Purity & Documentation|{Fluvastatin} Data Sheet|{Fluvastatin} manufacturer|{Fluvastatin} Cancer} OC(=O)/C=C/C(O)=O
InChiKey:
ZSOPWZQRZHWYFY-NUXPJIRBSA-N
InChi :
InChI=1S/C9H18N2OS.{{β-Muricholic acid} web|{β-Muricholic acid} Endogenous Metabolite|{β-Muricholic acid} Activator|{β-Muricholic acid} Biological Activity|{β-Muricholic acid} In Vitro|{β-Muricholic acid} manufacturer} C4H4O4/c1-3-7(2)8(10)9(12)11-4-5-13-6-11;5-3(6)1-2-4(7)8/h7-8H,3-6,10H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t7-,8-;/m0.PMID:23290930 /s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life:
≥12 months if stored properly.
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
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 . 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 . Clinical trial: Up to now, P32/98 is still in the preclinical development stage.|Product information|CAS Number: 251572-86-8|Molecular Weight: 318.39|Formula: C13H22N2O5S|Chemical Name: (2E)-but-2-enedioic acid; (2S,3S)-2-amino-3-methyl-1-(1,3-thiazolidin-3-yl)pentan-1-one|Smiles: C[C@@H](CC)[C@H](N)C(=O)N1CSCC1.OC(=O)/C=C/C(O)=O|InChiKey: ZSOPWZQRZHWYFY-NUXPJIRBSA-N|InChi: InChI=1S/C9H18N2OS.C4H4O4/c1-3-7(2)8(10)9(12)11-4-5-13-6-11;5-3(6)1-2-4(7)8/h7-8H,3-6,10H2,1-2H3;1-2H,(H,5,6)(H,7,8)/b;2-1+/t7-,8-;/m0./s1|Technical Data|Appearance: Solid Power|Purity: ≥98% (or refer to the Certificate of Analysis)|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.|Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined|HS Tariff Code: 382200|Products are for research use only. Not for human use.|
