CVT-12012

SKU: orb1220665

Description

CVT-12012 is an orally bioavailable inhibitor of stearoyl-CoA desaturase (SCD; IC50 = 6.1 nM in HepG2 cells).

Key Properties

• CAS Number: 1018675-35-8
• MW: 434.41
• Purity: >98% (HPLC)
• Formula: C₂₁H₂₁F₃N₄O₃?
• SMILES: Cc1nc2ccc(NCc3cccc(c3)C(F)(F)F)cc2n(CCNC(=O)CO)c1=O
• Target: SCD
• Solubility: DMSO:125 mg/mL (287.75 mM)

Bioactivity

• In Vivo:
  In a rat PK study, CVT-12012 demonstrates good oral bioavailability (78%). It appears that the oral absorption of CVT-12012 is not affected by a significant Pgp efflux, which is expected based on Caco-2 assay result. The plasma clearance of CVT-12012 is high (88 mL/min/kg) with elimination half-life of approximately 1 h.
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• In Vitro:
  CVT-12012 (Compound 5b) displays the highest potency in both the microsomal and the HEPG2 SCD assays (IC50 38 nM and 6.1 nM, respectively) compared to the other methyl-substituted compounds.
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Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Quick Database Links

Gene Symbol

SCD