5.04044

PrCP Inhibitor

• Sinonimo/i: PrCP Inhibitor, Angiotensinase C Inhibitor, Lysosomal Carboxypeptidase C Inhibitor, Lysosomal Pro-X Carboxypeptidase Inhibitor, PCP Inhibitor, Proline Carboxypeptidase Inhibitor, Prolylcarboxypeptidase Inhibitor, 2-Amino-N-((2 S,3 S)-3-(biphenyl-4-yl)-1-((, Angiotensinase C Inhibitor, Lysosomal Carboxypeptidase C Inhibitor, Lysosomal Pro-X Carboxypeptidase Inhibitor, PCP Inhibitor, Proline Carboxypeptidase Inhibitor, Prolylcarboxypeptidase Inhibitor, 2-Amino-N-((2S,3S)-3-(biphenyl-4-yl)-1-((2
• Formula empirica (notazione di Hill): C₃₁H₃₃Cl₂N₅O₂
• Numero CAS: 1252037-41-4
• Peso molecolare: 578.53
• Codice UNSPSC: 12352200
• NACRES: NA.77

Proprietà

• Saggio: ≥97% (HPLC)
• Livello qualitativo: 100
• Forma fisica: powder
• Produttore/marchio commerciale: Calbiochem^®
• Condizioni di stoccaggio: OK to freeze
• Colore: white
• Solubilità: DMSO: 100 mg/mL
• Temperatura di conservazione: −20°C

Descrizione

Descrizione generale

A dichlorobenzimidazolopyrrolidinamide compound that acts as a highly potent PrCP-selective inhibitor (IC₅₀ = 1 nM against human PrCP; IC₅₀ = 2 and 8 nM against mouse PrCP, respectively, in the absence or presence of 1% mouse serum albumin), presumably via non-covalent catalytic site interaction, while exhibiting no significant potency toward panels of ion channels, receptors, and enzymes, including homologous serine proteases QPP, FAP, PEP, ACE2, DPP4, DPP8, and DPP9 (IC₅₀ >25 µM). Oral administration (100 mg/kg/d for 5 d) is reported to result in significant food intake reduction and body fat loss among high fat diet-induced obese mice in vivo.

A dichlorobenzimidazolopyrrolidinamide compound that acts as a highly potent PrCP-selective inhibitor (IC₅₀ in the absence/presence of 1% mouse serum albumin = 1 nM/1 nM and 2 nM/8 nM, respectively, against human and mouse PrCP-catalyzed Mca-APK(Dnp)-OH hydrolysis; Initial [Substrate] = 25 µM), presumably via non-covalent catalytic site interaction, while exhibiting no significant potency toward panels of ion channels, receptors, and enzymes, including homologous serine proteases QPP, FAP, PEP, ACE2, DPP4, DPP8, and DPP9 (IC₅₀ >25 µM). Despite its being a substrate of P-gp efflux transporters and ineffective CNS delivery across blood-brain barrier, peripheral PrCP inhibition via oral administration (100 mg/kg/d for 5 d; [Drug] = 380 nM and 50 nM, respectively, in blood and brain 24 h after last p.o. dosing) is reported to result in significant food intake reduction and body fat loss among high fat diet-induced obese mice (0.73 g fat reduction vs. 0,73 g fat gain in 5 d, respectively, with drug or vehicle treatment) in vivo. Drug treatment among PrCP^-/- obsese mice in comparison, results in only 1.1% weight loss primarily due to a decreased gain in muscle mass and little change in body fat.

Azioni biochim/fisiol

Cell permeable: yes

Primary Target
PrCP

Reversible: yes

Confezionamento

Packaged under inert gas

Attenzione

Toxicity: Standard Handling (A)

Ricostituzione

Use only fresh DMSO for reconstitution.

Altre note

Wu, Z., et al. 2012. Bioorg. Med. Chem. Lett.22, 1774.
Graham, T.H., et al. 2012. Bioorg. Med. Chem. Lett.22, 658.
Zhou, C., et al. 2010. J. Med. Chem.53, 7251.

Note legali

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): WGK 3
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable