Vildagliptin
Vildagliptin
CAS: 274901-16-5
Molecular Formula: C17H25N3O2
Vildagliptin - Names and Identifiers
| Name | Vildagliptin |
| Synonyms | Galvus Laf 237 Vidagliptin Vildagliptin Unii-I6B4B2U96p Vildagliptin (NVP-LAF 237) Vidagliptin (see vildagliptin) (2S)-1-[N-(3-hydroxytricyclo[3.3.1.1~3,7~]dec-1-yl)glycyl]pyrrolidine-2-carbonitrile 2-Pyrrolidinecarbonitrile, 1-(((3-hydroxytricyclo(3.3.1.13,7)dec-1-yl)amino)acetyl)-, (2S)- (-)-(2S)-1-[[(3-Hydroxytricyclo[3.3.1.1[3,7]]dec-1-yl)amino]acetyl]pyrrolidine-2-carbonitrile |
| CAS | 274901-16-5 |
| EINECS | 630-410-0 |
| InChI | InChI=1/C18H17F6N3O.H3O4P/c19-13-8-15(21)14(20)6-10(13)5-11(25)7-17(28)26-3-4-27-12(9-26)1-2-16(27)18(22,23)24;1-5(2,3)4/h1-2,6,8,11H,3-5,7,9,25H2;(H3,1,2,3,4)/t11-;/m1./s1 |
Vildagliptin - Physico-chemical Properties
| Molecular Formula | C17H25N3O2 |
| Molar Mass | 303.4 |
| Density | 1.27 |
| Melting Point | 153-155?C |
| Boling Point | 531.3±50.0 °C(Predicted) |
| Specific Rotation(α) | -78.3° (c = 9.73 in methanol) |
| Flash Point | 275.1℃ |
| Solubility | Soluble in DMSO and Water |
| Appearance | Solid |
| Color | White |
| pKa | 15.05±0.40(Predicted) |
| Storage Condition | Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
| Stability | Stable for 2 years from date of purchase as supplied. Solutions in DMSO, DMF, or ethanol may be stored at -20°C for up to 3 months |
| Use | A CD26 inhibitor associated with immune response inhibition |
| In vitro study | Vildagliptin is the most stable DPP-IV inhibitor, binding to the DPP-IV S1-and S2-catalytic sites, and is able to mimic the P-1 site transition state. |
| In vivo study | Vildagliptin (administered orally at 10 μmol/kg) is a potent, orally active inhibitor of plasma DPP-IV activity in obese male Zucker rats, increased levels of GLP-1 in the oral glucose tolerance test (OGTT). In obese male Zucker rats, Vildagliptin, administered orally at 10 μmol/kg, significantly reduced blood glucose excursions and stimulated insulin secretion. There was maximal inhibition (95%) of plasma DPP-IV activity approximately 2 h after administration of Vildagliptin (1 μmol/kg, po), whereas within 30 min after administration, the inhibition of DPP-IV was> 50% and the inhibition lasted for more than 10 hours in cynomolgus monkeys. Vildagliptin(60 mg/kg) increased pancreatic β-cell mass by increasing β-cell replication and reducing apoptosis, and the increased β-cell mass was maintained for 12 days after vildagliptin elution. In streptozotocin (STZ)-induced diabetic adult male Sprague Dawley rats, Vildagliptin was administered at a dose of 10 mg/kg for 32 weeks to prevent nerve fiber loss. |
Vildagliptin - Risk and Safety
| Risk Codes | R28 - Very Toxic if swallowed R38 - Irritating to the skin R41 - Risk of serious damage to eyes R48 - Danger of serious damage to health by prolonged exposure |
| Safety Description | S24/25 - Avoid contact with skin and eyes. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S28 - After contact with skin, wash immediately with plenty of soap-suds. S36/37/39 - Wear suitable protective clothing, gloves and eye/face protection. |
| UN IDs | 3077 |
| HS Code | 29339900 |
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