1. Metabolic Enzyme/Protease
  2. Stearoyl-CoA Desaturase (SCD)

CVT-12012 

Cat. No.: HY-11034 Purity: 98.97%
Handling Instructions

CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.

For research use only. We do not sell to patients.

CVT-12012 Chemical Structure

CVT-12012 Chemical Structure

CAS No. : 1018675-35-8

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 110 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
Estimated Time of Arrival: December 31
10 mg USD 150 In-stock
Estimated Time of Arrival: December 31
25 mg USD 310 In-stock
Estimated Time of Arrival: December 31
50 mg USD 480 In-stock
Estimated Time of Arrival: December 31
100 mg USD 780 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

CVT-12012 is a potent and orally bioavailable stearoyl-coA desaturase (SCD) inhibitor, with IC50s of 38 nM, 6.1 nM for rat microsomal and human HEPG2, respectively.

IC50 & Target

IC50: 38 nM (rat microsomal), 6.1 nM (human HEPG2)[1][2].

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[1].

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[1].

Solvent & Solubility
In Vitro: 

DMSO : 125 mg/mL (287.75 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.3020 mL 11.5099 mL 23.0197 mL
5 mM 0.4604 mL 2.3020 mL 4.6039 mL
10 mM 0.2302 mL 1.1510 mL 2.3020 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (4.79 mM); Clear solution

References
Molecular Weight

434.41

Formula

C₂₁H₂₁F₃N₄O₃

CAS No.

1018675-35-8

SMILES

O=C(NCCN1C(C(C)=NC2=C1C=C(NCC3=CC=CC(C(F)(F)F)=C3)C=C2)=O)CO

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
CVT-12012
Cat. No.:
HY-11034
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CVT-12012

Cat. No.: HY-11034