MIV-247( MIV 247 | MIV247 )

Catalog No. M11433 CAS No. 1352817-76-5

COA

Datasheet

HNMR

HPLC

MSDS

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Product Name

MIV-247
Note

Research use only, not for human use.
Brief Description

MIV-247 (MIV247) is a potent, selective, orally active inhibitor of cathepsin S with Ki of 2.1 nM (human cathepsin S).
Description

MIV-247 (MIV247) is a potent, selective, orally active inhibitor of cathepsin S with Ki of 2.1 nM (human cathepsin S); displays high selectivity (>200-fold) overs other related cathepsins, inhibits mouse and cynomolgus monkey cathepsin S with Ki of 4.5 and 7.2 nM, respectively; attenuates mechanical allodynia alone, and also enhances the effect of gabapentin and pregabalin without increasing side effects in mouse model of neuropathic pain.Asthma Discontinued.
In Vitro

——
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.
Synonyms

MIV 247 | MIV247
Pathway

Metabolic Enzyme/Protease
Target

Cathepsin
Recptor

Cathepsin
Research Area

Inflammation/Immunology
Indication

Asthma

CAS Number

1352817-76-5
Formula Weight

391.391
Molecular Formula

C17H24F3N3O4
Purity

>98% (HPLC)
Solubility

——
SMILES

CC(C(=O)NC(CC1(CCCC1)F)C(=O)NC2(CCC2)C(=O)C(=O)N)(F)F
Chemical Name

(S)-N-(1-(2-amino-2-oxoacetyl)cyclobutyl)-2-(2,2-difluoropropanamido)-3-(1-fluorocyclopentyl)propanamide

1. Hewitt E, et al. J Pharmacol Exp Ther. 2016 Sep;358(3):387-96.

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