1352817-76-5
1352817-76-5 structure
- Name: MIV-247
- Chemical Name: MIV-247
- CAS Number: 1352817-76-5
- Molecular Formula: C17H24F3N3O4
- Molecular Weight: 391.39
- Catalog: Signaling Pathways Metabolic Enzyme/Protease Cathepsin
- Create Date: 2019-02-09 12:05:02
- Modify Date: 2024-01-23 16:10:00
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MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively.
| Name | MIV-247 |
|---|
| Description | MIV-247 is a selective cathepsin S inhibitor with Kis of 2.1, 4.2 and 7.5 nM for human, mouse and cynomolgus monkey cathepsin S, respectively. |
|---|---|
| Related Catalog | |
| Target |
IC50: 2.1 nM (Human Cathepsin S), 4.2 nM (Mouse Cathepsin S), 7.5 nM (Cynomolgus monkey Cathepsin S)[1] |
| In Vivo | Oral administration of MIV-247 (100-200 µmol/kg) dose-dependently attenuates mechanical allodynia by up to approximately 50% reversal when given as a single dose or when given twice daily for 5 days. Cathepsin S inhibition with MIV-247 exerts significant antiallodynic efficacy alone, and also enhances the effect of gabapentin and pregabalin without increasing side effects or inducing pharmacokinetic interactions[1]. |
| Animal Admin | Mice[1] MIV-247 is administered via oral gavage to Male C57BL/6 mice (20-30 g) at a dose volume of 5 ml/kg at doses up to 200 µmol/kg. In the PK studies, seven blood samples (20 µL) are drawn from the lateral saphenous vein of each mouse at 15 minutes, 30 minutes, 1 hour, 2 hours, 3 hours, 5 hours, and 7 hours postdose[1]. |
| References |
| Molecular Formula | C17H24F3N3O4 |
|---|---|
| Molecular Weight | 391.39 |