Vildagliptin (LAF-237) inhibits DPP−4 with IC50 of 2.3 nM.
Pharmacology. 2023;108(2):166-175.
DPP4 Inhibitor Sitagliptin Reduces Inflammatory Responses and Mast Cell Activation in Allergic Rhinitis
Vildagliptin purchased from AbMole
Cell Experiment | |
---|---|
Cell lines | |
Preparation method | |
Concentrations | |
Incubation time |
Animal Experiment | |
---|---|
Animal models | Obese male Zucker rats |
Formulation | 0.5% carboxymethylcellulose (CMC) and 0.2% Tween 80 |
Dosages | 10 μmol/kg |
Administration | Orally administrated at a single dose |
Molecular Weight | 303.4 |
Formula | C17H25N3O2 |
CAS Number | 274901-16-5 |
Solubility (25°C) | DMSO 50 mg/mL |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
[1] Michał Wiciński, et al. Vasculoprotective Effects of Vildagliptin. Focus on Atherogenesis
Related DPP Products |
---|
Saikogenin A
Saikogenin A, extracted from a Chinese herbal plant called Tsai-Fu, is a dipeptidyl peptidase-IV (DPP-IV) inhibitor. |
16-Hydroxycleroda-3,13-dien-15,16-olide
16-Hydroxycleroda-3,13-dien-15,16-olide is a potent serine protease dipeptidyl peptidase 4 (DPP-4) inhibitor. 16-Hydroxycleroda-3,13-dien-15,16-olide down-regulates LPS-induced ERK phosphorylation in myocyte but blocks GLP-1 induced PKA expression. |
Gosogliptin
Gosogliptin is a potent and selective inhibitor of dipeptidyl peptidase-IV (DPP-IV). |
1G244
1G244 is a potent DPP8/9 inhibitor with IC50s of 12 nM and 84 nM, respectively. 1G244 does not inhibit DPPIV and DPPII. 1G244 induces apoptosis in multiple myeloma cells and has anti-myeloma effects. |
Saxagliptin hydrochloride
Saxagliptin hydrochloride (BMS-477118 hydrochloride) is a potent, selective, reversible, competitive and orally active dipeptidyl peptidase-4 (DPP-4) (Ki = 0.6-1.3 nM) inhibitor. Saxagliptin hydrochloride has the peotential for type 2 diabetes mellitus research. |
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2023 AbMole BioScience. All Rights Reserved.