31314-39-3
31314-39-3 structure
- Name: Prodipine hydrochloride
- Chemical Name: 4,4-diphenyl-1-propan-2-ylpiperidine,hydrochloride
- CAS Number: 31314-39-3
- Molecular Formula: C20H26ClN
- Molecular Weight: 315.88000
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Dipeptidyl Peptidase
- Create Date: 2017-12-19 04:52:52
- Modify Date: 2024-01-10 14:17:22
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Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively.
| Name | 4,4-diphenyl-1-propan-2-ylpiperidine,hydrochloride |
|---|---|
| Synonyms |
Prodipine hydrochloride
Piperidine,4,4-diphenyl-1-isopropyl-,hydrochloride BY-101 ANTHEN prodipin hydrochloride UNII-89CCP8Z2PS |
| Description | Prodipine, a diphenyl-phosphonate derivative. The IC50s of Prodipine for purified and plasma Dipeptidyl peptidase IV (DPP IV) from the rabbit are 4.5 μM and 30 μM, respectively. |
|---|---|
| Related Catalog | |
| Target |
IC50: 4.5 μM (purified DPP IV), 30 μM (plasma DPP IV)[1] |
| In Vitro | Prodipine, a diphenyl-phosphonate derivative selected from a group of slow-binding irreversible inhibitors of this enzyme. The IC50 values of Prodipine for purified and plasma DPP IV from the rabbit are 4.5 μM and 30 μM, respectively[1]. |
| In Vivo | Male rabbits weighing 3-4 kg receive a single intravenous injection with 10 mg Prodipine or saline. After 1 hr, plasma DPP IV activity has decreased to less than 20% of the preinjection value and remaines unchanged during a 24 hr observation period. A profound and long-lasting inhibition of plasma DPP IV activity is observed in the treated animals (1, 5 or 10 mg). It takes 5 to 8 days to reach half of the pretreatment DPP IV activity and generally more than 20 days for a complete recovery[1]. |
| Kinase Assay | Dipeptidyl peptidase IV activity is determined using the fluorogenic substrate Gly-Pro-4-methoxy-2-naphthylamide. Hydrolysis of L-Ala-4-methoxy-2-naphthylamide in 60 mM phosphate buffer pH 7.4 is chosen for the determination of aminopeptidase M activity. The intramolecularly quenched fluorogenic substrate Lys (2,4 dinitrophenyl)-Pro-Pro-NH-CH2-CH,-NH,-aminobenzoyl-2HCl is used to assay aminopeptidase P activity. Prolyl oligopeptidase (PO) is measured with N-benzyloxycarbonyl-Gly-Pro-7-amino-4-methylcoumarin. One unit of enzymatic activity is defined as the amount of enzyme catalyzing the formation of 1 μmol of assay product per minute under the conditions used[1]. |
| Animal Admin | Rabbits[1] Male New Zealand white rabbits (3-4 kg) are used. EXPERIMENT 1 The rabbits (n=1 for each condition) receive a single iv. injection of 10 mg Prodipine or saline. Blood samples are taken 5 min before injection and 30 min, 1 hr, 2 hr, and 24 hr after the treatment. EXPERIMENT 2 The rabbits (n=1 for each condition) receive a single i.v. bolus injection of saline or are treated with 1, 5, or 10 mg Prodipine (also in a single i.v. bolus) at time 0. The animals are kept under observation for 40 days. At several time points (-5 min, 4 hr, and at days 1, 2, 3, 6, 12, 21, and 40), blood samples are taken and body weight determined. Rabbits are killed with pentobarbital after termination of the observation period. |
| References |
| Molecular Formula | C20H26ClN |
|---|---|
| Molecular Weight | 315.88000 |
| Exact Mass | 315.17500 |
| PSA | 3.24000 |
| LogP | 5.21680 |