Detail of "274901-16-5"

CAS Number:
274901-16-5
Name:
2-Pyrrolidinecarbonitrile,1-[2-[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-, (2S)-
Superlist Name:
Vildagliptin
Molecular Structure:
Formula:
C₁₇H₂₅N₃O₂
Molecular Weight:
303.40
Synonyms:
2-Pyrrolidinecarbonitrile,1-[[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-, (2S)- (9CI);Galvus;LAF 237;NVP-LAF 237;(-)-(2s)-1-(((3-hydroxytricyclo(3.3.1.1(3,7))dec-1-yl)amino)acetyl)pyrrolidine-2-carbonitrile;
Density:
1.27 g/cm³
Boiling Point:
531.3 °C at 760 mmHg
Flash Point:
275.1 °C
Appearance:
white crystalline powder

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Liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does not: All Rights Reserved. Liraglutide, a long-acting glucagon-like peptide-1 analog, reduces body weight and food intake in obese candy-fed rats, whereas a dipeptidyl peptidase-IV inhibitor, vildagliptin, does not. Raun, Kirsten; von Voss, Pia; Gotfredsen, Carsten F.; Golozoubova, Valeria; Rolin, Bidda; Knudsen, Lotte Bjerre (Department of Pharmacology Research 3, Novo Nordisk A/S, Maaloev, Den.).In this study， 274901-16-5 and 204656-20-2 are also used. Diabetes, 56(1), 8-15 (English) 2007 American Diabetes Association. CODEN: DIAEAZ. ISSN: 0012-1797. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) Metabolic effects of the glucagon-like peptide-1 analog liraglutide and the dipeptidyl peptidase-IV inhibitor vildagliptin were compared in rats made obese by supplementary candy feeding. Female Sprague-Dawley rats were randomized to 12-wk diets of chow or chow plus candy. The latter were randomized for 12 further weeks to continue their diet while receiving 0.2 mg/kg liraglutide twice daily s.c., 10 mg/kg vildagliptin twice daily orally, or vehicle or to revert to chow-only diet. Energy expenditure was measured, and oral glucose tolerance tests (OGTTs) were performed. Body compn. was detd. by dual-energy x-ray absorptiometry scanning, and pancreatic b-cell mass was detd. by histol. Candy feeding increased wt., fat mass, and feeding-assocd. energy expenditure. Liraglutide or reversal to chow diet fully reversed wt. and fat gains. Liraglutide was assocd. with decreased calorie intake and shifted food preference (increased chow/decreased candy consumption). Despite wt. loss, liraglutide-treated rats did not decrease energy expenditure compared with candy-fed controls. Vildagliptin affected neither wt., food intake, nor energy expenditure. OGTTs, histol., and blood analyses indirectly suggested that both drugs increased insulin sensitivity. Liraglutide and vildagliptin inhibited obesity-assocd. increases in b-cell mass. This was assocd. with wt. and fat mass normalization with liraglutide, but not vildagliptin, where the ratio of b-cell to body mass was low. .

Vildagliptin therapy reduces postprandial intestinal triglyceride-rich lipoprotein particles in patients with type 2 diabetes: All Rights Reserved. Vildagliptin therapy reduces postprandial intestinal triglyceride-rich lipoprotein particles in patients with type 2 diabetes. Matikainen, N.; Maenttaeri, S.; Schweizer, A.; Ulvestad, A.; Mills, D.; Dunning, B. E.; Foley, J. E.; Taskinen, M.-R. (Division of Cardiology, Department of Medicine, Helsinki University Central Hospital and Biomedicum, Helsinki, Finland). Diabetologia, 49(9), 2049-2057 (English) 2006 Springer GmbH. CODEN: DBTGAJ. ISSN: 0012-186X. DOCUMENT TYPE: Journal CA Section: 1 (Pharmacology) We assessed the effects of vildagliptin, a novel dipeptidyl peptidase IV inhibitor, on postprandial lipid and lipoprotein metab. in patients with type 2 diabetes. Subjects, materials and methods: This was a single-center, randomized, double-blind study in drug-naive patients with type 2 diabetes. Patients received vildagliptin (50 mg twice daily, n=15) or placebo (n=16) for 4 wk. Triglyceride, cholesterol, lipoprotein, glucose, insulin, glucagon and glucagon-like peptide-1 (GLP-1) responses to a fat-rich mixed meal were detd. for 8 h postprandially before and after 4 wk of treatment. Relative to placebo, 4 wk of treatment with vildagliptin decreased the AUC0-8h for total triglyceride by 22±11% (p=0.037), the incremental AUC0-8h (IAUC0-8h) for total triglyceride by 85±47% (p=0.065), the AUC0-8h for chylomicron triglyceride by 65±19% (p=0.001) and the IAUC0-8h for chylomicron triglyceride by 91±28% (p=0.002). This was assocd. 9007-92-5 and 274901-16-5 are cas registry numbers of chemicals which are used as reagents here. with a decrease in chylomicron apolipoprotein B-48 (AUC0-8h, -1.0±0.5 mg l-1 h, p=0.037) and chylomicron cholesterol (AUC0-8h, -0.14±0.07 mmol l-1 h, p=0.046). Consistent with previous studies, 4 wk of treatment with vildagliptin also increased intact GLP-1, suppressed inappropriate glucagon secretion, decreased fasting and postprandial glucose, and decreased HbA1c from a baseline of 6.7% (change, -0.4±0.1%, p<0.001), all relative to placebo. Treatment with vildagliptin for 4 wk improves postprandial plasma triglyceride and apolipoprotein B-48-contg. triglyceride-rich lipoprotein particle metab. after a fat-rich meal. The mechanisms underlying the effects of this dipeptidyl peptidase IV inhibitor on postprandial lipid metab. remain to be explored. .

Detail of "274901-16-5"

2-Pyrrolidinecarbonitrile,1-[2-[(3-hydroxytricyclo[3.3.1.13,7]dec-1-yl)amino]acetyl]-, (2S)-

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Reference