NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research
In Vitro
NDB induces rearrangements of helix 11 (H11) and helix 12 (H12, AF-2) by forming a homodimer of hFXRα-LBD, totally different from the active conformation in monomer state. NDB (25 μM) effectively antagonizes the GW4064-stimulated FXR/RXR interaction and FXRα target gene expression in primary mouse hepatocytes, including the small heterodimer partner (SHP) and bile-salt export pump (BSEP). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
NDB (24 mg/kg; intraperitoneal injection; once a day; for 4 weeks) efficiently decreases the gene expressions of phosphoenolpyruvate carboxykinase (PEPCK), glucose 6-phosphatase (G6-pase), small heterodimer partner, and BSEP in db/db mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Male C57BL/6J db/db mice (8 weeks of age) Dosage: 24 mg/kg Administration: Intraperitoneal injection; once a day; for 4 weeks Result: Decreased the gene expressions of PEPCK, G6-pase, small heterodimer partner, and BSEP.
Form:Solid
IC50& Target:Human FXRα (hFXRα)
Spezifikationen
Spezifikationen & Reinheit
≥98%
Biochemische und physiologische Mechanismen
NDB is a selective human FXRα (hFXRα) antagonist that is effective in modulating transcription of FXRα downstream genes. NDB can be used in anti-diabetes research.
Storage
Store at -20°C
Verschickt in
Ice chest + Ice pads
Dieses Produkt erfordert Kühlkettenversand. Grundversand und andere Economy-Optionen sind nicht verfügbar.
Aktionsart
ANTAGONIST
Reinheit
≥98%
Namen und Kennungen
Molekulargewicht
471.42
Erweiterte Daten
Zertifikate (CoA, COO, BSE/TSE und Analyse-Diagramm)
C of A & Other Certificates(BSE/TSE, COO):
Analytical Chart:
Chemische und physikalische Eigenschaften
Löslichkeit
DMSO : 100 mg/mL (212.13 mM; Need ultrasonic)
Lösungsrechner
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