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CVT-12012

Catalog No. T6412 CAS 1018675-35-8

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

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CVT-12012, CAS 1018675-35-8

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	CVT-12012 is an orally bioavailable inhibitor of stearoyl-CoA desaturase (SCD; IC50 = 6.1 nM in HepG2 cells).
Targets&IC50	human HEPG2:6.1 nM, rat microsomal:38 nM
In vivo	CVT-12012 is highly potent in a human cell-based (HEPG2) SCD assay (IC(50)=6nM). This compound has 78% oral bioavailability in rats and is preferentially distributed into liver (76 times vs plasma) with relatively low brain penetration[1].

Molecular Weight	434.41
Formula	C21H21F3N4O3?
CAS No.	1018675-35-8

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 125 mg/mL (287.75 mM)

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Koltun D O , Vasilevich N I , Parkhill E Q , et al. Orally bioavailable, liver-selective stearoyl-CoA desaturase (SCD) inhibitors[J]. Bioorganic and Medicinal Chemistry Letters, 2009, 19(11):3050-3053. 2. Atkinson KA, Beretta EE, Brown JA,et al.N-benzylimidazole carboxamides as potent, orally active stearoylCoA desaturase-1 inhibitors[J].Bioorg Med Chem Lett. 2011 Mar 15;21(6):1621-5.

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO (Master liquid concentration mg/mL)，Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation：Take μL DMSO master liquid, next add μL PEG300， mix and clarify, next add μL Tween 80，mix and clarify, next add μL ddH₂O, mix and clarify.

Note:

Be sure to add the solvent(s) in order. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.

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What is the mass of compound required to make a 10 mM stock solution in 10 ml of water given that the molecular weight of the compound is 197.13 g/mol?
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An example of a dilution calculation using the Tocris dilution calculator
What volume of a given 10 mM stock solution is required to make 20ml of a 50 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=50 μM, V2=20 ml and V1 is the unknown:
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The answer of 100 microliter (0.1 ml) appears in the Volume (start) box

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Definitions of molecular mass, molecular weight, molar mass and molar weight:
Molecular mass (molecular weight) is the mass of one molecule of a substance and is expressed n the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

CVT-12012 1018675-35-8 Metabolism Stearoyl-CoA Desaturase (SCD) CVT 12012 inhibit CVT12012 Inhibitor inhibitor

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