Vildagliptin (LAF-237)

Modify Date: 2024-01-02 17:29:43

Vildagliptin (LAF-237) Structure
Vildagliptin (LAF-237) structure
 Common Name Vildagliptin (LAF-237)
CAS Number 274901-16-5 Molecular Weight 303.39900
Density 1.27 g/cm3 Boiling Point 531.3ºC at 760 mmHg
Molecular Formula C17H25N3O2 Melting Point 153-155?C
MSDS N/A Flash Point 275.1ºC

 Use of Vildagliptin (LAF-237)


Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.IC50 Value: 2.3 nM[1]Target: DPP-4in vitro: Vildagliptin is an N-substituted glycyl-2-cyanopyrrolidine (figure 2). It is a potent competitive and reversible inhibitor of human and rodent DPP-4 in vitro, with a median inhibitory concentration (IC50) ~2-3 nmol/L. Importantly, vildagliptin inhibits DPP-4 with high specificity relative to other similar peptidases where its IC50 exceeds 200 mol/L [1].in vivo: Compared to age-, gender-, BMI-matched subjects with normal renal function, the mean AUC of vildagliptin after 14 days in patients with mild, moderate, and severe RI increased by 40%, 71%, and 100%, respectively [2]. The treatment was effective in modulating stress in pancreatic tissue, both by reducing levels of stress markers as well as by increasing activity of SOD and catalase. After analyzing the pancreatic histology, we found that vildagliptin was also able to preserve islets and pancreatic β-cells, especially at the concentration of 5 mg/kg [3].Clinical trial: FDA approved drug.

 Names

Name Vildagliptin
Synonym More Synonyms

 Vildagliptin (LAF-237) Biological Activity

Description Vildagliptin (LAF-237; NVP-LAF 237) inhibits DPP-4 with IC50 of 2.3 nM.IC50 Value: 2.3 nM[1]Target: DPP-4in vitro: Vildagliptin is an N-substituted glycyl-2-cyanopyrrolidine (figure 2). It is a potent competitive and reversible inhibitor of human and rodent DPP-4 in vitro, with a median inhibitory concentration (IC50) ~2-3 nmol/L. Importantly, vildagliptin inhibits DPP-4 with high specificity relative to other similar peptidases where its IC50 exceeds 200 mol/L [1].in vivo: Compared to age-, gender-, BMI-matched subjects with normal renal function, the mean AUC of vildagliptin after 14 days in patients with mild, moderate, and severe RI increased by 40%, 71%, and 100%, respectively [2]. The treatment was effective in modulating stress in pancreatic tissue, both by reducing levels of stress markers as well as by increasing activity of SOD and catalase. After analyzing the pancreatic histology, we found that vildagliptin was also able to preserve islets and pancreatic β-cells, especially at the concentration of 5 mg/kg [3].Clinical trial: FDA approved drug.
Related Catalog
References

[1]. Villhauer EB, Brinkman JA, Naderi GB et al. 1-[[(3-hydroxy-1-adamantyl) amino]acetyl]-2-cyano-(S)-pyrrolidine: a potent, selective, and orally bioavailable dipeptidyl peptidase IV inhibitor with antihyperglycemic properties. J Med Chem 2003;46:2774-89.

[2]. He YL, Kulmatycki K, Zhang Y, Pharmacokinetics of vildagliptin in patients with varying degrees of renal impairment. Int J Clin Pharmacol Ther. 2013 Jun 19.

[3]. Avila Dde L, Araújo GR, Silva M, Vildagliptin ameliorates oxidative stress and pancreatic beta cell destruction in type 1 diabetic rats. Arch Med Res. 2013 Apr;44(3):194-202.

[4]. Qin CJ, et al. Inhibition of dipeptidyl peptidase IV prevents high fat diet-induced liver cancer angiogenesis by downregulating chemokine ligand 2. Cancer Lett. 2018 Jan 31;420:26-37.

 Chemical & Physical Properties

Density 1.27 g/cm3
Boiling Point 531.3ºC at 760 mmHg
Melting Point 153-155?C
Molecular Formula C17H25N3O2
Molecular Weight 303.39900
Flash Point 275.1ºC
Exact Mass 303.19500
PSA 76.36000
LogP 1.50308
Storage condition -20°C Freezer

 Safety Information

Hazard Codes Xi
HS Code 2933990090

 Synthetic Route

 Customs

HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

 Synonyms

2-Pyrrolidinecarbonitrile, 1-[2-[(3-hydroxytricyclo[3.3.1.1]dec-1-yl)amino]acetyl]-, (2S)-
Galvus
(-)-(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1[3,7]]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile
Vildagliptin
Laf 237
(2S)-1-[N-(3-Hydroxyadamantan-1-yl)glycyl]pyrrolidine-2-carbonitrile
(2S)-1-[N-(3-hydroxytricyclo[3.3.1.1]dec-1-yl)glycyl]pyrrolidine-2-carbonitrile
Unii-I6B4B2U96p
(2S)-1-[N-(3-Hydroxyadamantan-1-yl)glycyl]-2-pyrrolidinecarbonitrile
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Related Compounds: More...
vildagliptin Impurity Q
1803168-08-2
Vildagliptin-d7
1133208-42-0
Vildagliptin
1147403-03-9
Vildagliptin Impurity L
1710765-32-4
Vildagliptin impurity M
1844894-70-7
Vildagliptin Impurity ZA6
2246354-69-6
Vildagliptin Related Compound A
741657-02-3
Vildagliptin-Boronic Acid
852331-49-8
Vildagliptin carboxylic acid metabolite (trifluoroacetate salt)
565453-41-0
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