NZ-97
Based on 1 Customer Validation
NZ-97 is a locally deliverable, lung-retaining dipeptidyl peptidase 4 (DPP4) inhibitor with an IC50 of 18 nM. It exhibits selectivity for DPP8 and DPP9 (with IC50 values of 1.3 μM and 0.6 μM, respectively). NZ-97 inhibits the DPP4 pool in lung-resident cells and epithelial lining fluid, elevates IL-6 and IGF-1 levels, and induces the expansion of type 2 alveolar epithelial cells (AEC2). NZ-97 reduces protein content in bronchoalveolar lavage fluid (BALF), ameliorates lung injury and alleviates pulmonary fibrosis. NZ-97 shows tolerability in untreated Mus musculus mice after intratracheal administration, and does not alter the proliferation or differentiation of lung fibroblasts. NZ-97 can be used in studies related to idiopathic pulmonary fibrosis, acute lung injury and emphysema.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.43%
- Fòrmula: C43H67N5O9
- Peso molecular:798.02
-
Almacenamiento:
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
-
Actividad biológica
-
Chemical Information
- Pureza y Documentación
- Referencias
-
Help & FAQs
Actividad biológica
Descripciòn
IC50 & Target
[1]|
DPP-4 18 nM (IC50) |
DPP-9 0.6 μM (IC50) |
DPP-8 1.3 μM (IC50) |
In Vitro
NZ-97 potently and selectively inhibits DPP4 (IC50 = 18 nM) relative to DPP8 and DPP9 (IC50s = 1.3 μM and 0.6 μM, respec-
tively) in cell-free biochemical assays[1].
NZ-97 (2 µM; 10-12 days) increases the colony-forming efficiency of AEC2s isolated from IPF lung explants in 3D coculture assays[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NZ-97 (0.5 mg/kg; intratracheal administration; once every 4 days) attenuates bleomycin sulfate (HY-17565)-induced pulmonary fibrosis in male C57BL/6J mice, and the therapeutic efficacy of combined treatment with nintedanib is significantly superior to that of monotherapy[1].
NZ-97 (0.05 mg/kg; intratracheal administration; single dose) increases the proliferation level of AEC2 by approximately 1.5-fold in untreated female C57BL/6J mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:C57BL/6J (female, 9-11 weeks old, LPS-induced acute lung injury)[1]
-
Dosage:0.05 mg/kg
-
Administration:intratracheal administration; every other day
-
Result:Reduced BALF protein levels from a mean of ~600 μg/mL to ~400 μg/mL.
Reduced histological injury scores from a mean of ~0.6 to ~0.4.
Increased the relative percentage of KI-67+ AEC2s by ~1.5-fold compared to vehicle in naive mice.
Increased the relative percentage of KI-67+ AEC2s by ~2-fold compared to vehicle in LPS-challenged mice.
-
Animal Model:C57BL/6J (male, 9-11 weeks old, bleomycin-induced lung fibrosis)[1]
-
Dosage:0.5 mg/kg; 30 mg/kg (nintedanib combination)
-
Administration:intratracheal administration; once every 4 days; p.o.; daily (nintedanib combination)
-
Result:Reduced lung hydroxyproline levels from a mean of ~200 μg/left lobe to ~180 μg/left lobe as a single agent.
Reduced lung hydroxyproline levels to ~150 μg/left lobe when combined with nintedanib, which was significantly more efficacious than either agent alone.
-
Animal Model:C57BL/6J (female, 9-11 weeks old, naive)[1]
-
Dosage:0.05 mg/kg
-
Administration:intratracheal administration; once
-
Result:Increased the relative percentage of KI-67+ AEC2s by ~1.5-fold compared to vehicle-treated naive mice.
Chemical Information
-
Appearance Solid
-
Peso molecular 798.02
-
Fòrmula C43H67N5O9
-
Color White to off-white
-
SMILES
CCCCCCCCN(C[C@@H]([C@H]([C@@H]([C@@H](CO)O)O)O)O)CC1=CC=C(C=C1)CNC(OCCOC23CC4CC(CC(C4)(C3)[C@@H](C(N5[C@@H](C[C@@H]6C[C@@H]65)C#N)=O)N)C2)=O
-
Envío
Room temperature in continental US; may vary elsewhere.
-
Almacenamiento
4°C, sealed storage, away from moisture and light
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Pureza y Documentación
-
Ficha de datos (281 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
Instrucciones de manejo (2659 KB)
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NZ-97 Related Classifications
HY-158315 Related Classifications
Powered by Bioz